Information on EC 3.4.21.59 - Tryptase

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The expected taxonomic range for this enzyme is: Eutheria

EC NUMBER
COMMENTARY
3.4.21.59
-
RECOMMENDED NAME
GeneOntology No.
Tryptase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Preferential cleavage: Arg-/-, Lys-/-, but with more restricted specificity than trypsin
show the reaction diagram
preferential cleavage: Arg-, Lys-, but with more restricted specificity than trypsin
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Lung tryptase
-
-
-
-
Mast cell neutral proteinase
-
-
-
-
Mast cell protease II
-
-
-
-
Mast cell proteinase II
-
-
-
-
Mast cell tryptase
-
-
-
-
Pituitary tryptase
-
-
-
-
Proteinase, mast cell neutral
-
-
-
-
Proteinase, mast cell serine, II
-
-
-
-
Proteinase, mast cell serine, tryptase
-
-
-
-
Rat mast cell protease II
-
-
-
-
Skin tryptase
-
-
-
-
tryptase
-
-
-
-
Tryptase M
-
-
-
-
Tryptase, skin
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
97501-93-4
-
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
gene mtc1; gene mtc1
SwissProt
Manually annotated by BRENDA team
genes TPSAB 1 and TPSB2
-
-
Manually annotated by BRENDA team
several enzyme forms
-
-
Manually annotated by BRENDA team
three distinct catalytic forms of human tryptase-beta
-
-
Manually annotated by BRENDA team
C57BL/6 mice, no TMT activity in but not BALB/c or 129/Sv mice
-
-
Manually annotated by BRENDA team
C57BL/6 mice, several enzyme forms
-
-
Manually annotated by BRENDA team
pig
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
physiological function
-
tryptase does not alter paracellular permeability in human airway cells over min or hours, and tryptase does not alter the structure of the cell tight junction
physiological function
-
tryptase increases the lipid accumulation in human monocyte THP-1-derived macrophages and promotes foam cell formation in vitro via suppressing LXRalpha activation
physiological function
-
tryptase plays an important role in the control of human colonic mucosal permeability, and enhanced tryptase activity is responsible for the increased permeability of rectal mucosa in irritable bowel syndrome patients
physiological function
-
tryptase promotes the invasion and migration of breast cancer cells along with activation of matrix metalloproteinase-2. Tryptase does not affect the proliferation of the cells. Tryptase promotes breast cancer migration and invasion
physiological function
-
tryptase-positive mast cells play a role in breast cancer angiogenesis
physiological function
-
activates isolated adult cardiac fibroblasts (Mus musculus) via protease activated receptor-2 (PAR-2)
physiological function
-
an essential mast cell-restricted mediator in chemically induced colitis, acts upstream of many of the factors implicated in inflammatory bowel disease
physiological function
-
angiogenic activity (shown in a chick embryo chorioallantoic membrane in vivo assay)
physiological function
-
can induce microvascular leakage via prostaglandins in a mast cell-independent manner and may contribute to the development of basophil-mediated inflammatory responses
physiological function
-
up-regulates vascular endothelial growth factor production in acute myeloid leukemia bone marrow stromal cells via the proteinase-activated receptor-2, ERK1/2, and p38MAPK signaling pathways
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
Ac-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate
-
-
?
Ac-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate
-
-
?
Ac-PANKAAC + H2O
Ac-PANK + Ala-Ala-Cys
show the reaction diagram
-
betaI and betaII tryptase
-
?
Ac-PRNKAAC + H2O
Ac-PRNK + Ala-Ala-Cys
show the reaction diagram
-
betaI and betaII tryptase
-
?
Ac-PRNRAAC + H2O
Ac-PRNR + Ala-Ala-Cys
show the reaction diagram
-
betaI and betaII tryptase
-
?
Ac-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate, best peptide substrate
-
-
?
Ac-PRTKAAC + H2O
Ac-PRTK + Ala-Ala-Cys
show the reaction diagram
-
betaI and betaII tryptase
-
?
Ac-Ser-Ile-Gln-Ser-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 51.2%
-
?
Ala-Ala-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate, high activity
-
-
?
Ala-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate
-
-
?
alpha2-antiplasmin + H2O
?
show the reaction diagram
-
substrate binding and interaction with the enzyme, overview
-
-
?
Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate
-
-
?
Benzoyl-Arg 4-nitroanilide + H2O
Benzoyl-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
-
Benzoyl-L-Lys-Gly-L-Arg 4-nitroanilide + H2O
Benzoyl-L-Lys-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
best of the substrates screened
-
-
-
Benzoyl-L-Lys-Gly-L-Arg 4-nitroanilide + H2O
Benzoyl-L-Lys-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
best of the substrates screened
-
-
-
benzoyl-L-Phe-L-Val-L-Arg-4-nitroanilide + H2O
benzoyl-L-Phe-L-Val-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Benzyloxycarbonyl-Ala-Ala-Lys 4-methoxy-2-naphthylamide + H2O
?
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-Ala-Arg-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Ala-Arg-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Arg + 7-amino-4-methylcoumarine
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-Arg 4-nitroanilide + H2O
Benzyloxycarbonyl-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
Benzyloxycarbonyl-Glu-Phe-Arg 4-nitroanilide + H2O
Benzyloxycarbonyl-Glu-Phe-Arg + 4-nitroaniline
show the reaction diagram
-
best substrate for lung enzyme
-
-
-
Benzyloxycarbonyl-Gly-Arg 4-trifluoromethylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Gly-Arg + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-Gly-Pro-Arg 4-nitroanilide + H2O
Benzyloxycarbonyl-Gly-Pro-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-L-Ala-L-Arg-L-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-L-Ala-L-Arg-L-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-L-Ala-L-Lys-L-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-L-Ala-L-Lys-L-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-L-Ala-L-Lys-L-Lys 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-L-Ala-L-Lys-L-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-Lys-Arg 4-trifluoromethylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Lys-Arg + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-Lys-Arg-S-CH2(CH3)2 + H2O
Benzyloxycarbonyl-Lys-Arg + S-CH2(CH3)2
show the reaction diagram
-
best substrate for skin enzyme
-
-
-
Boc-Phe-Ser-Arg-methyl-coumarin + H2O
?
show the reaction diagram
-
synthetic substrate
-
?
Bz-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
complement component 3 + H2O
?
show the reaction diagram
-
digestion
-
-
?
D-Ile-Pro-Arg-4-nitroanilide + H2O
D-Ile-Pro-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
D-Ile-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
D-Phe-Pip-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
D-Phe-piperocolyl-L-Arg 4-nitroanilide + H2O
D-Phe-piperocolyl-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
-
D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide + H2O
D-phenylalanyl-pipecolyl-L-arginine + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide + H2O
D-phenylalanyl-pipecolyl-L-arginine-4-nitroaniline
show the reaction diagram
-
-
-
-
?
D-Pro-Phe-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
D-Val-Leu-Arg 4-methoxy-2-naphthylamide + H2O
?
show the reaction diagram
-
-
-
-
-
D-Val-Leu-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
Fibrinogen + H2O
?
show the reaction diagram
-
-
-
-
?
Fibrinogen + H2O
?
show the reaction diagram
-
digestion
-
-
?
fibrinogen + H2O
fibrin + ?
show the reaction diagram
Q7YS62
-
-
-
?
fibrinogen + H2O
fibrinogen fragments
show the reaction diagram
-
-
-
?
fibrinogen + H2O
fibrinogen fragments
show the reaction diagram
-
-
-
?
fibrinogen + H2O
fibrinogen fragments
show the reaction diagram
-
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
-
-
-
-
Fibronectin + H2O
?
show the reaction diagram
-
digestion
-
-
?
Gelatinase + H2O
?
show the reaction diagram
-
digestion of the 72000 MW form to a 62000 MW form
-
-
-
Glu-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
Glu-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
High-molecular mass kininogen + H2O
?
show the reaction diagram
-
-
-
-
-
high-molecular-weight kininogen + H2O
?
show the reaction diagram
-
-
-
-
?
human influenza virus HA + H2O
HA1 + HA2
show the reaction diagram
-
-
-
?
Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate
-
-
?
L-pyroGlu-Gly-Arg 4-nitroanilide + H2O
L-pyroGlu-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
-
LL-37 + H2O
LL-37 fragments
show the reaction diagram
-
the platelet-derived chemokine CXCL4 protects LL-37 from cleavage by beta-tryptase
-
-
?
N-(p-tosyl)-Gly-Pro-Arg-4-nitroanilide + H2O
N-(p-tosyl)-Gly-Pro-Arg + 4-nitroaniline
show the reaction diagram
Q7YS62
-
-
-
?
N-(p-tosyl)-Gly-Pro-Lys-4-nitroanilide + H2O
N-(p-tosyl)-Gly-Pro-Lys + 4-nitroaniline
show the reaction diagram
Q7YS62
-
-
-
?
N-Benzoyl-Arg ethyl ester + H2O
?
show the reaction diagram
-
-
-
-
-
N-benzoyl-DL-Arg-p-nitroanilide + H2O
N-benzoyl-DL-Arg + p-nitroaniline
show the reaction diagram
-
measurements of tryptase activity in sputum of chronic obstructive pulmonary disease patiens
-
-
?
N-benzoyl-DL-arginine-4-nitroanilide + H2O
N-benzoyl-DL-arginine + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
N-Carbobenzoxy-Arg-Arg 4-methylcoumarin 7-amide + H2O
N-Carbobenzoxy-Arg-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
N-carbobenzoxy-GPR-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
N-Carbobenzoxy-Phe-Arg 4-methylcoumarin 7-amide + H2O
N-Carbobenzoxy-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
N-p-tosyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
N-p-tosyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
synthetic peptide substrate, mutant enzyme, expressed in insect cells
-
?
N-p-tosyl-Gly-Pro-Arg-p-nitroanilide + H2O
N-p-tosyl-Gly-Pro-Arg + p-nitroaniline
show the reaction diagram
-
-
-
-
?
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
show the reaction diagram
-
synthetic peptide substrate
-
?
N-tert-Butyloxycarbonyl-Ile-Glu-Gly-Arg 4-methylcoumarin 7-amide + H2O
N-tert-Butyloxycarbonyl-Ile-Glu-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
rapid hydrolysis by free enzyme, scarcely hydrolyzed by the enzyme associated with trypstatin
-
-
-
N-tert-Butyloxycarbonyl-Phe-Ser-Arg 4-methylcoumarin 7-amide + H2O
N-tert-Butyloxycarbonyl-Phe-Ser-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
N-tert-Butyloxycarbonyl-Phe-Ser-Arg 4-methylcoumarin 7-amide + H2O
N-tert-Butyloxycarbonyl-Phe-Ser-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
N-tert-Butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide + H2O
N-tert-Butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
N-tert-Butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide + H2O
N-tert-Butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Nalpha-benzoyl-DL-arginine-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
Nalpha-benzoyl-L-arginine-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
neurotensin + H2O
?
show the reaction diagram
-
-
-
-
-
Oxidized B-chain of insulin + H2O
?
show the reaction diagram
-
cleavage at Arg8-Gly9-NH2, Arg8-Arg9- and Arg22-Gly23-bonds
-
-
-
Precursor of matrix metalloproteinase 1 + H2O
?
show the reaction diagram
-
conversion of the 52000 MW precursor into a 41000 MW protein, generation of new N-termini, namely Gln80 and Val82
-
-
-
Precursor of matrix metalloproteinase 3 + H2O
?
show the reaction diagram
-
conversion of the 57000 MW precursor to a 45000 MW polypeptide, N-terminal amino acid is Phe83
-
-
-
Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide + H2O
?
show the reaction diagram
-
chromogenic substrate, best peptide substrate
-
-
?
pro-matrix metalloprotease-3 + H2O
?
show the reaction diagram
-
digestion
-
-
?
pro-matrix metalloproteinase-2 + H2O
matrix metalloproteinase-2 + ?
show the reaction diagram
-
-
-
-
?
pro-nerve growth factor + H2O
mature nerve growth factor and smaller fragments
show the reaction diagram
-
-
analyzed by MS/MS
-
?
Pro-Phe-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 3.9%
-
?
Pro-urokinase + H2O
?
show the reaction diagram
-
digestion
-
-
?
protease-activated receptor-2 + H2O
?
show the reaction diagram
-
digestion
-
-
?
proteinase-activated receptor-2 + H2O
?
show the reaction diagram
-
tryptase may contribute to cyclooxygenase-2 upregulation by epithelial proteinase-activated receptor-2 activation during early lip carcinogenesis
-
-
?
prothrombin + H2O
thrombin + ?
show the reaction diagram
-
-
-
-
prothrombin + H2O
thrombin + ?
show the reaction diagram
-
-
-
-
-
S2366 + H2O
?
show the reaction diagram
Q7YS62
-
-
-
?
t-butyloxycarbonyl-Gln-Ala-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 100%
-
?
t-butyloxycarbonyl-Gln-Arg-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 26.0%
-
?
t-butyloxycarbonyl-Gln-Gly-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 63.3%
-
?
t-butyloxycarbonyl-Glu(OBzl)-Ala-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 67.3%
-
?
t-butyloxycarbonyl-Glu(OBzl)-Gly-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 26.3%
-
?
t-butyloxycarbonyl-Glu-Lys-Lys-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 1.6%
-
?
t-butyloxycarbonyl-Gly-Lys-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 10.9%
-
?
t-butyloxycarbonyl-Ile-Glu-Gly-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 3.5%
-
?
t-butyloxycarbonyl-Leu-Arg-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 5.9%
-
?
t-butyloxycarbonyl-Leu-Gly-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 30.0%
-
?
t-butyloxycarbonyl-Leu-Lys-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 14.4%
-
?
t-butyloxycarbonyl-Phe-Ser-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
-
-
?
t-butyloxycarbonyl-Phe-Ser-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 36.3%
-
?
t-butyloxycarbonyl-Val-Pro-Arg-4-methyl-coumarin 7-amide + H2O
?
show the reaction diagram
-
synthetic substrate, relative activity 6.1%
-
?
tert-butyloxycarbonyl-Gly-Lys-Arg 4-methylcoumarin 7-amide + H2O
tert-butyloxycarbonyl-Gly-Lys-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
TGFbeta + H2O
activated TGFbeta + ?
show the reaction diagram
-
activation, tryptase activates TGFbeta, a key remodelling factor in asthma, in human airway smooth muscle cells via direct proteolysis in a PAR2-independent manner, TGFbeta is produced as a latent complex and the main limiting step in TGFb bioavailability is its activation, overview
-
-
?
Tos-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
Tos-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Tosyl-Arg methyl ester + H2O
?
show the reaction diagram
-
-
-
-
-
Tosyl-Gly-L-Pro-Arg 4-nitroanilide + H2O
Tosyl-Gly-L-Pro-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
tosyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin + H2O
tosyl-Gly-L-Pro-L-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
tosyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
Tosyl-Gly-Pro-Lys 4-nitroanilide + H2O
Tosyl-Gly-Pro-Lys + 4-nitroaniline
show the reaction diagram
-
-
-
-
-
tosyl-Gly-Pro-Lys-4-nitroanilide + H2O
tosyl-Gly-Pro-Lys + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
tosyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
tosyl-glycine-L-proline-L-arginine-4-nitroanilide + H2O
tosyl-glycine-L-proline-L-arginine + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
tosyl-GPK-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
tosyl-GPR-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
Vasoactive intestinal peptide + H2O
?
show the reaction diagram
-
-
-
-
-
Z-D-Arg-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
[Arg8]vasopressin + H2O
?
show the reaction diagram
-
-
-
-
-
MeOCO-Nle-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
-
pituitary enzyme has a preference for cleaving COOH-terminal to arginine or lysine residues which are preceded by a proline residue 4 or 6 residues NH2-terminal to the site of cleavage
-
-
-
additional information
?
-
-
kininogenase activity
-
-
-
additional information
?
-
-
the enzyme inactivates fibrinogen and high-molecular weight kininogen and converts C3 to C3a
-
-
-
additional information
?
-
-
specificity overview: peptide 4-nitroanilides
-
-
-
additional information
?
-
-
not: casein, hemoglobin, azocoll
-
-
-
additional information
?
-
-
no activation of the precursor of matrix metalloproteinase 2
-
-
-
additional information
?
-
-
skin and lung enzymes have both extended substrate-binding sites and proline residues at P3 substantially decrease kcat/Km, both enzymes prefer the tripeptide 4-nitroanilides with a P2 Gly residue over Phe, both favour the substrate benzyloxycarbonyl-Lys-Gly-Arg 4-nitroanilide over similar substrates containing six other representive amino acid residues at P3
-
-
-
additional information
?
-
-
4 closely related isoenzymes, tryptase alpha, I tryptase, tryptase II/beta and III tryptase, preferentially cleaves peptide substrates carboxy-terminal to arginine and lysine residues, hydrolyses bronchodilatatory neuropeptides, vasoactive intestinal peptide and peptide histidine methionine in vitro, cleaves fibrinogen and fibronectin inactivating, and activating the zymogens of stromelysin-1 and urokinase-type plasminogen activator
-
?
additional information
?
-
-
activity only toward substrates with Arg at the P1 position, only 0.3% and 0.1% activity with t-butyloxycarbonyl-Val-Leu-Lys-4-methylcoumarin 7-amide and Arg-4-methylcoumarin 7-amide, Suc-Ala-Pro-Ala-4-methylcoumarin 7-amide and Suc-Leu-Leu-Val-Leu-4-methylcoumarin 7-amide are no substrates
-
?
additional information
?
-
-
Ile-Phe-Lys-p-nitroanilide, N-acetyl-Ile-Glu-Ala-Arg-p-nitroanilide, N-benzoyl-Arg-p-nitroanilide, N-benzoyl-Ile-Glu-Gly-Arg-p-nitroanilide, N-benzoyl-Phe-Val-Arg-p-nitroanilide, or N-benzoyl-Pro-Phe-Arg-p-nitroanilide are no substrates
-
?
additional information
?
-
-
little or no reaction with Suc-Ala-Ala-Pro-Phe-p-nitroanilide and MeO-Suc-Arg-Pro-Tyr-p-nitroanilide
-
?
additional information
?
-
-
tryptases betaI and betaII have a strict preference for cleavage after the basic amino acids, lysine and arginine, with only a slight preference for lysine over arginine, prefernce for proline at P4, preference for arginine or lysine at P3 and P2, these enzymes are not controlled by blood plasma proteinase inhibitors and only cleave a few physiological substrates in vitro
-
?
additional information
?
-
-
unlike beta-tryptases, alpha-tryptases apparently are proteolytically inactive
-
?
additional information
?
-
-
tryptase may have kallikrein-like activity under physiological conditions, tryptase could be of importance in the generation of kinnins subsequent to mast cell activation
-
-
-
additional information
?
-
-
enzyme plays a crucial role in the process of degranulation
-
-
-
additional information
?
-
-
potential biological activities of human enzyme: 1. fibrinogenolysis, prevents clotting at local sites of mast cell activation
-
-
-
additional information
?
-
-
the preference of the skin tryptase for substrates with 2 terminal basic residues indicates that this enzyme could process prohormones and proproteins which contain this structural feature at the cleavage site
-
-
-
additional information
?
-
-
2. augmentation of histamine-mediated contractility of airway smooth, increases airway hyperreactivity to histamine and allergens, 3. degradation of vasoactive intestinal peptide, decreases endogenous bronchodilatory activity in lung 4. activation of prostromelysin, facilitates activation of procollagenase and tissue remodeling, 5. degradation of fibronectin, tissue remodeling, 6. stimulation of fibroblast proliferation, enhances fibrogenesis or wound repair
-
-
-
additional information
?
-
-
biological functions and true roles of tryptase has not yet been demonstrated
-
?
additional information
?
-
-
currently unknown whether tryptases perform redundant or unique functions in vivo
-
?
additional information
?
-
-
post-translational proteolytic cleavage of the precursors of the fusion glycoproteins of enveloped RNA viruses is indispensable for their fusion activity and infectivity, enzyme triggers infection by pneumotropic Sendai and influenza A viruses by processing
-
?
additional information
?
-
-
tryptase activates PKB in inflammatory reaction in ECV304 cells, tryptase can activate phosphoinositol-3-kinase/protein kinase B pathway and enhance IL-8 expression
-
-
-
additional information
?
-
-
beta-tryptase is involved in the pathogenesis of airway inflammation, the enzyme accounts for more than 25% or total protein in human mast cells, activated cells release the enzyme along with histamine and heparin proteoflycans, overview
-
-
-
additional information
?
-
-
the enzyme is an inflammation mediator
-
-
-
additional information
?
-
-
the enzyme is an inflammation mediator, mMCP-6 is a major storage component of connective tissue-type mast cells, and is not normally released into the environment
-
-
-
additional information
?
-
-
the enzyme is involved in allergic inflammation, mechanism, overview
-
-
-
additional information
?
-
-
the lack of eosinophils in asthmatic airway smooth muscle bundles in contrast to the large number of mast cells is a key feature of asthma and is caused by beta-tryptase abrogating the eosinophil chemotactic activities of ASM cell-derived eosinophil chemoattractants such as eotaxin and RANTES, overview
-
-
-
additional information
?
-
-
beta-tryptase is a tetramer that has enzymatic activity, but requires heparin binding to maintain functional and structural stability, alpha-tryptase has little, if any, enzymatic activity but is a stable tetramer in the absence of heparin, both forms are in a two-state equilibrium, which is influenced by the residues in the vicinity of the active site and by inhibitor/substrate binding, substrate binding structure, overview, Asp216 and Lys192 are the main determinants of tryptase activity
-
-
-
additional information
?
-
Q7YS62
equine tryptase has alanine at residue 216, rather than glycine, which confers increased arginine substrate specificity in vitro and may restrict fibrinogenolysis in vivo
-
-
-
additional information
?
-
-
the enzyme is a serine protease that is a major and selective component of the secretory granules of all human mast cells, active monomers of human beta-tryptase have expanded substrate specificities, overview
-
-
-
additional information
?
-
-
the unique structure of the proteinase comprises four almost identical monomer subunits arranged in a square flat ring with its substrate pockets faced inside, forming a tetramer with a central pore that can be penetrated by a short peptide, the optimal length of the tryptase substrate is a pentasaccharide, substrate specificity and cleavage pattern, screening of a peptide library, overview
-
-
-
additional information
?
-
-
beta-tryptase enhances release of vascular endothelial growth factor from human osteoarthritic chondrocytes
-
-
-
additional information
?
-
-
mast cell secretion of the tryptase MCP-6 contributes to eosinophil recruitment to the site of Trichinella spiralis larval infection
-
-
-
additional information
?
-
-
mast cell-derived tryptase-heparin complexes play important roles in mouse bovine serum albumin/interleukin-1beta-induced arthritis
-
-
-
additional information
?
-
-
ferritin is not a substrate for tryptase
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
complement component 3 + H2O
?
show the reaction diagram
-
digestion
-
-
?
Fibrinogen + H2O
?
show the reaction diagram
-
digestion
-
-
?
fibrinogen + H2O
fibrin + ?
show the reaction diagram
Q7YS62
-
-
-
?
pro-matrix metalloprotease-3 + H2O
?
show the reaction diagram
-
digestion
-
-
?
pro-matrix metalloproteinase-2 + H2O
matrix metalloproteinase-2 + ?
show the reaction diagram
-
-
-
-
?
pro-nerve growth factor + H2O
mature nerve growth factor and smaller fragments
show the reaction diagram
-
-
analyzed by MS/MS
-
?
Pro-urokinase + H2O
?
show the reaction diagram
-
digestion
-
-
?
protease-activated receptor-2 + H2O
?
show the reaction diagram
-
digestion
-
-
?
proteinase-activated receptor-2 + H2O
?
show the reaction diagram
-
tryptase may contribute to cyclooxygenase-2 upregulation by epithelial proteinase-activated receptor-2 activation during early lip carcinogenesis
-
-
?
TGFbeta + H2O
activated TGFbeta + ?
show the reaction diagram
-
tryptase activates TGFbeta, a key remodelling factor in asthma, in human airway smooth muscle cells via direct proteolysis in a PAR2-independent manner, TGFbeta is produced as a latent complex and the main limiting step in TGFb bioavailability is its activation, overview
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
digestion
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
-
tryptase may have kallikrein-like activity under physiological conditions, tryptase could be of importance in the generation of kinnins subsequent to mast cell activation
-
-
-
additional information
?
-
-
enzyme plays a crucial role in the process of degranulation
-
-
-
additional information
?
-
-
potential biological activities of human enzyme: 1. fibrinogenolysis, prevents clotting at local sites of mast cell activation
-
-
-
additional information
?
-
-
the preference of the skin tryptase for substrates with 2 terminal basic residues indicates that this enzyme could process prohormones and proproteins which contain this structural feature at the cleavage site
-
-
-
additional information
?
-
-
2. augmentation of histamine-mediated contractility of airway smooth, increases airway hyperreactivity to histamine and allergens, 3. degradation of vasoactive intestinal peptide, decreases endogenous bronchodilatory activity in lung 4. activation of prostromelysin, facilitates activation of procollagenase and tissue remodeling, 5. degradation of fibronectin, tissue remodeling, 6. stimulation of fibroblast proliferation, enhances fibrogenesis or wound repair
-
-
-
additional information
?
-
-
biological functions and true roles of tryptase has not yet been demonstrated
-
?
additional information
?
-
-
currently unknown whether tryptases perform redundant or unique functions in vivo
-
?
additional information
?
-
-
post-translational proteolytic cleavage of the precursors of the fusion glycoproteins of enveloped RNA viruses is indispensable for their fusion activity and infectivity, enzyme triggers infection by pneumotropic Sendai and influenza A viruses by processing
-
?
additional information
?
-
-
tryptase activates PKB in inflammatory reaction in ECV304 cells, tryptase can activate phosphoinositol-3-kinase/protein kinase B pathway and enhance IL-8 expression
-
-
-
additional information
?
-
-
beta-tryptase is involved in the pathogenesis of airway inflammation, the enzyme accounts for more than 25% or total protein in human mast cells, activated cells release the enzyme along with histamine and heparin proteoflycans, overview
-
-
-
additional information
?
-
-
the enzyme is an inflammation mediator
-
-
-
additional information
?
-
-
the enzyme is an inflammation mediator, mMCP-6 is a major storage component of connective tissue-type mast cells, and is not normally released into the environment
-
-
-
additional information
?
-
-
the enzyme is involved in allergic inflammation, mechanism, overview
-
-
-
additional information
?
-
-
the lack of eosinophils in asthmatic airway smooth muscle bundles in contrast to the large number of mast cells is a key feature of asthma and is caused by beta-tryptase abrogating the eosinophil chemotactic activities of ASM cell-derived eosinophil chemoattractants such as eotaxin and RANTES, overview
-
-
-
additional information
?
-
-
beta-tryptase enhances release of vascular endothelial growth factor from human osteoarthritic chondrocytes
-
-
-
additional information
?
-
-
mast cell secretion of the tryptase MCP-6 contributes to eosinophil recruitment to the site of Trichinella spiralis larval infection
-
-
-
additional information
?
-
-
mast cell-derived tryptase-heparin complexes play important roles in mouse bovine serum albumin/interleukin-1beta-induced arthritis
-
-
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
CaCl2
-
tryptase free from trypstatin is activated by 10 mM CaCl2, but tryptase associated with trypstatin is not
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2S)-1-acetyl-N-[4-[(aminoiminomethyl)amino]-1-(2-benzothiazolylcarbonyl)butyl]-2,5-azetidinearboxamide
-
-
-
(2S)-1-acetyl-N-[4-[(aminoiminomethyl)amino]-1-(2-benzothiazolylcarbonyl)butyl]-2,5-dihydro-1H-pyrrole-2-carboxamide
-
-
(2S)-1-acetyl-N-[4-[(aminoiminomethyl)amino]-1-(2-benzothiazolylcarbonyl)butyl]-2-pyrrolidinecarboxamide
-
-
(2S)-1-acetyl-N-[4-[(aminoiminomethyl)amino]-1-(2-benzothiazolylcarbonyl)butyl]-4-methylpentanamide
-
-
-
(Arg-Trp-Lys-Gly)4(Lys)2Lys-NH2
-
noncompetitive
(Lys-Lys-Phe-Gly)4(Lys)2Lys-NH2
-
noncompetitive
1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl-methyl 4-[[(phenylmethoxy)carbonyl]amino]-benzoate
-
-
1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl-methyl 5-[[(phenylmethoxy)carbonyl]amino]-pentanoate
-
-
1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl-methyl N-[(phenylmethoxy)carbonyl]-beta-alanate
-
-
1,2,5-thiadiazolidin-3-one 1,1-dioxide
-
1,2,5-zhiadiazolidin-3-one 1,1-dioxide-based heterocyclic sulfides are potent inhibitors
1,2-benzisothiazol-3-one 1,1-dioxide
-
-
1-acetyl-N-[(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]prolinamide
-
-
1-methylethyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
2-methoxyethyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
3-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-1,1-diethylurea
-
-
3-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-1,1-dimethylurea
-
-
4',6-Diamidino-2-phenylindole
-
-
4'-[[5-(phenylethynyl)furan-2-yl]carbonyl]spiro[1-benzofuran-3,1'-cyclohexane]-5-carboxamide
-
-
4'-[[5-(phenylethynyl)furan-2-yl]carbonyl]spiro[1-benzofuran-3,1'-cyclohexane]-5-carboximidamide
-
-
4-Amidinophenylpyruvic acid
-
-
4-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]butanamide
-
-
4-aminobenzamidine
-
-
4-Methylumbelliferyl 4-guanidinobenzoate
-
-
4-Nitrophenyl 4-guanidinobenzoate
-
-
5-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]pentanamide
-
-
6-amidino-2-naphthyl p-guanidinobenzoate dimethane sulfonate
-
nafamostat mesilate
6-amino-N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
-
6-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
-
7-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]heptanamide
-
-
acetyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
acetyl-PRNK-chloromethylketone
-
-
Alpha1-antitrypsin
-
-
-
Alpha1-antitrypsin
-
human and dog enzyme insensitive
-
Alpha1-antitrypsin
-
rat peritoneal mast cell enzyme, no inhibition of skin enzyme
-
Alpha1-antitrypsin
-
not
-
antipain
-
-
antithrombin III
-
-
-
APC-1167
-
-
-
APC-366
-
low molecular weight active site-directed competitive tryptase inhibitor
APC366
-
N-(1-hydroxy-2-naphthoyl)-L-arginyl-L-prolinamide, selective inhibitor of mast cell tryptase
APC366
-
-
Aprotinin
-
-
Aprotinin
-
-
Aprotinin
-
not
Aprotinin
-
-
Aprotinin
-
weak inhibitor
Arg-Trp-Lys-Gly-NH2
-
noncompetitive
BABIM
-
-
benzamidine
-
-
benzamidine
-
and derivatives
benzamidine
-
not
benzamidine
-
-
benzamidine
-
-
benzyl 4-[(3-[N2-[(benzyloxy)carbonyl]-L-lysyl]-1,2,4-oxadiazol-5-yl)methyl]piperazine-1-carboxylate
-
-
benzyl [(1S)-2-(1,3-benzothiazol-2-yl)-1-(1H-indol-2-ylmethyl)-2-oxoethyl]carbamate
-
-
benzyl [(1S)-2-(1,3-benzothiazol-2-yl)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)ethyl]carbamate
-
-
benzyl [(1S)-5-amino-1-(1,3-benzothiazol-2-ylcarbonyl)pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-([5-[4-(benzylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-([5-[4-(benzyloxy)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-([5-[4-([2-[3-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-([5-[4-([2-[4-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[4-[(2-thiophen-2-ylethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[4-[(3,4-dimethylbenzyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[4-[(3-methylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[4-[(3-phenylpropyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[4-[(4-phenylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-1-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-2-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[[5-(4-methoxybenzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[[5-(4-[[(2E)-3-phenylprop-2-en-1-yl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,4-dichlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate10n
-
-
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,5-difluorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(4-fluorophenoxy)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
benzyl [(1S)-5-amino-1-[[5-(4-[[4-(2-fluorobenzyl)piperazin-1-yl]carbonyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
benzyl [(1S,3E)-5-amino-1-(1,3-benzothiazol-2-ylcarbonyl)pent-3-en-1-yl]carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(2,4-dichlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(3,4-dichlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(3,4-dimethoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(3-chlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(3-methoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(4-chlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(4-fluorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-(4-[(4-methoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((1S)-5-amino-1-[(5-benzyl-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl((benzyl ((1S)-5-amino-1-[(5-(4-[(3,4-dimethoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate1S)-5-amino-1-[(5-(4-[(3-methoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[3-(2-phenylethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[3-(3-phenylpropoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[4-(2-phenylethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[4-(3-phenylpropoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[4-(benzyloxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[4-(cyclohexylmethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[4-(naphthalen-1-ylmethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
benzyl[(1S)-5-amino-1-((5-[4-(naphthalen-2-ylmethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
BMS-262084
-
-
Bovine pancreatic trypsin inhibitor
-
may play a physiological role in regulation of tryptase proteolytic activity
-
Bovine pancreatic trypsin inhibitor
-
pH-dependent
-
Bovine pancreatic trypsin inhibitor
-
the functional unit of bovine tryptase is formed of at least 4 binding sites for this inhibitor
-
Bovine pancreatic trypsin inhibitor
-
-
-
BPTI
-
irreversible complex formation between protease and serpin
-
BPTI
-
-
-
CaCl2
-
-
Calcium
-
5 mM is needed to cause an irreversible 50% loss of activity after 60 min at room temperature
ck-MCoEeTI
-
-
-
CRA-2059
-
synthetic inhibitor
CRA-2059
-
-
cyclotheonamide E4
-
-
c[-Pro-beta3hArg(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHAc)-CO-]
-
-
c[-Pro-beta3hArg(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHCO-(CH2)5-NH2)-CO-]
-
-
c[-Pro-beta3hPhe(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHCO-(CH2)5-NH2)-CO-]
-
-
c[-Pro-beta3Lys(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHAc)-CO-]
-
-
D-Tyr-Glu-Phe-Lys-Arg-CH2Cl
-
-
Dansyl-L-glutamyl-glycyl-L-arginine chloromethyl ketone
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
DTNB
-
-
ethyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
ethyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
ethyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
ethyl[(1S)-5-amino-1-((5-[4-(2-phenylethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
ferritin
-
ferritin can retard the cleavage of both native oxidized high-molecular-weight kininogen by tryptase, initial rates of cleavage are reduced 45-75% in the presence of ferritin
-
FUT175
-
a selective tryptase inhibitor
gabexate mesilate
-
-
histamine
-
-
JNJ-27390467
-
-
LDTI
-
non-competitive inhibitor, derived from Hirudo medicinalis
-
LDTI
-
only naturally occuring inhibitor, leech-derived tryptase inhibitor
-
Leupeptin
-
-
Leupeptin
-
-
Leupeptin
-
binding structure with alpha- and beta-tryptase, overview
Lys-Lys-Phe-Gly-NH2
-
noncompetitive
M58539
-
i.e. N-[3-[4-(aminomethyl)phenyl]propyl]-N'-[(1-chloronaphthalen-2-yl)sulfanyl]ethane-1,2-diamine, a highly selective inhibitor
MCoEeTI
-
-
-
MCoEeTI[K10R]
-
-
-
MCoTI-I
-
-
-
MCoTI-II
-
-
-
MCoTI-II-DELTA[DG]
-
-
-
MCoTI-II-DELTA[GSDGV]
-
-
-
MCoTI-II-DELTA[SDGGV]
-
-
-
MCoTI-II-DELTA[SDGG]
-
-
-
MCoTI-II-DELTA[SDGG][K10R]
-
-
-
MCoTI-II[K10A]
-
-
-
MCoTI-II[K10F]
-
-
-
MCoTI-II[K10Q]
-
-
-
MCoTI-II[K10R]
-
-
-
MCoTI-II[K10V]
-
-
-
MCoTI-II[K10V]-[I11P]
-
-
-
MCoTI-II[PKI]-[AVP]
-
-
-
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[(2-hydroxyethyl)(methyl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
methyl [(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]carbamate
-
-
methyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
mucus protease inhibitor
-
-
-
N-tosyl-L-Lys chloromethyl ketone
-
-
N-tosyl-L-Lys chloromethyl ketone
-
-
N-tosyl-L-Lys chloromethyl ketone
-
-
N-tosyl-L-Lys chloromethyl ketone
-
-
N-tosyl-L-Phe chloromethyl ketone
-
-
N-tosyl-L-Phe chloromethyl ketone
-
weak
N-[(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-piperidin-4-ylpropyl]-3,4-difluorobenzamide
-
-
N-[(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]-3,4-difluorobenzamide
-
-
N-[(1S)-3-azetidin-3-yl-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)propyl]-3,4-difluorobenzamide
-
-
N-[(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]-3,4-difluorobenzamide
-
-
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-1,3-benzodioxole-5-carboxamide
-
-
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,4-difluorobenzamide
-
-
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,5-difluorobenzamide
-
-
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3-fluorobenzamide
-
-
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-chlorobenzamide
-
-
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-fluorobenzamide
-
-
N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
-
N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
-
N-[2-(3-chlorophenyl)ethyl]-4-([3-[N2-(2,2-dimethylpropanoyl)-L-lysyl]-1,2,4-oxadiazol-5-yl]methyl)benzamide
-
-
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(1,2,3,4-tetrahydroisoquinolin-7-ylsulfanyl)ethane-1,2-diamine
-
-
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(1-benzothiophen-2-ylsulfanyl)ethane-1,2-diamine
-
-
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(1-benzothiophen-5-ylsulfanyl)ethane-1,2-diamine
-
-
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(2,3-dihydro-1H-inden-5-ylsulfanyl)ethane-1,2-diamine
-
-
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(naphthalen-2-ylsulfanyl)ethane-1,2-diamine
-
-
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(phenylsulfanyl)ethane-1,2-diamine
-
-
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-[(2-methyl-1,3-benzothiazol-6-yl)sulfanyl]ethane-1,2-diamine
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,2,2-trifluoroacetamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,2-dimethylpropanamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,4-difluorobenzamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,5-dimethylfuran-3-carboxamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2-fluorobenzamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2-methoxyacetamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2-methylpropanamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-3,4-difluorobenzamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-3-fluorobenzamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-4-chlorobenzamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-4-fluorobenzamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]cyclopentanecarboxamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]cyclopropanecarboxamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]furan-2-carboxamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]hexanamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]morpholine-4-carboxamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]piperidine-1-carboxamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]pyrrolidine-1-carboxamide
-
-
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]tetrahydrofuran-3-carboxamide
-
-
NaCl
-
reversible at 1 M
NaCl
-
-
Nafamostat
-
complete inhibition at 0.1 mM
nafamostat mesilate
-
-
neutrophil myeloperoxidase
-
important component of the neutrophil response to microbial infection, high concentrations of heparin can prevent the inhibition of tryptase by MPO
-
p-Aminophenylmethanesulfonyl fluoride
-
lung enzyme is inhibited over 3times faster than the skin enzyme
p-chloromercuribenzoate
-
-
Pentamidine
-
nonselective inhibitor
Peptide chloromethyl ketone inhibitors
-
-
-
polybrene
-
heparin antagonist, potent inhibitor, noncompetitive inhibition
polybrene
-
heparin antagonist, potent inhibitor, noncompetitive inhibition, recombinant tryptase
prop-2-en-1-yl [(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]carbamate
-
-
protamine
-
heparin antagonist, potent inhibitor, competitive inhibition
protamine
-
heparin antagonist, potent inhibitor, competitive inhibition, recombinant tryptase
rLDTI
-
recombinant leech-derived tryptase inhibitor
-
RWJ-56423
-
-
RWJ-58643
-
-
SBTII
-
-
Soybean trypsin inhibitor
-
-
-
Soybean trypsin inhibitor
-
inhibition of rat peritoneal mast cell enzyme, no inhibition of skin enzyme
-
Soybean trypsin inhibitor
-
not
-
Soybean trypsin inhibitor
-
not
-
Sulfonyl fluoride inhibitors
-
-
trans-4-(Guanidinomethyl)cyclohexanecarboxylic acid esters
-
most effective: trans-4-(guanidinomethyl)cyclohexanecarboxylic acid butylphenyl ester
Trypstatin
-
inhibition above pH 7.5
-
Trypstatin
-
purification
-
Tryptase inhibitor
-
derived from the medical leech Hirudo medicinalis
-
ZnSO4
-
-
[1'-(acetyloxy)-5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
-
[5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
-
[5'-(aminomethyl)-1'-[(methylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
-
[5'-(aminomethyl)-1'-[(phenylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl](5-benzylfuran-2-yl)methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(2-phenylethyl)furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylsulfanyl)furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-chlorophenyl)ethynyl]furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-fluorophenyl)ethynyl]furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methoxyphenyl)ethynyl]furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methylphenyl)ethynyl]furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-hydroxyphenyl)ethynyl]furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-methylphenyl)ethynyl]furan-2-yl]methanone
-
-
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-tert-butylphenyl)ethynyl]furan-2-yl]methanone
-
-
[5-[(1E)-1-aminoprop-1-en-1-yl]spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
-
-
[6'-(aminomethyl)-2',3'-dihydrospiro[cyclohexane-1,1'-inden]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
-
MOL 6131
-
developed against mast cell beta-tryptase and studied in ovalbumin-induced allergic airway inflammation
additional information
-
alpha2-macroglobulin; not: alpha1-proteinase inhibitor
-
additional information
-
not affected by the protein inhibitors of serine proteinases normally present in human extracellular fluids
-
additional information
-
antileukoprotease; antithrombin III; hirudin; low-molecular weight elastase inhibitor from human lung; no specific physiologic inhibitor has yet been found for the protease
-
additional information
-
not: alpha1-proteinase inhibitor; plasma
-
additional information
-
lima bean trypsin inhibitor; ovomucoid
-
additional information
-
lima bean trypsin inhibitor; ovomucoid inhibitor; plasma (human)
-
additional information
-
chymostatin, E64 and pestatin have no effect
-
additional information
-
unique tryptase inasmuch as it has no endogenous inhibitors
-
additional information
-
no inhibition of native or recombinant enzyme by soybean trypsin inhibitor SBTI
-
additional information
-
library screening and inhibitor design and synthesis, inhibition mechanism, overview
-
additional information
-
design of potent and selective enzyme inhibitors based on alpha-keto-[1,2,4]-oxadiazoles, overview
-
additional information
-
synthesis and inhibitory potency of spirocyclic piperidine amide derivatives as enzyme inhibitors, overview
-
additional information
-
tryptase-small-interfering RNA vector inhibits tryptase expression in P815 cells, reduced tryptase expression significantly inhibits the synthesis and release of interleukin-6 and tissue necrosis factor-alpha in vascular endothelial cells
-
additional information
-
CXCL4 does not act as a direct beta-tryptase inhibitor, but destabilizes active tetrameric enzyme by antagonizing the heparin component required for the integrity of the tetramer
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
heparin
-
is required for stabilization of the enzyme tetramer as a prerequisite for catalytic activity, the enzyme activity is 70fold increased, pH-dependent complex formation and complex structure, overview
heparin
-
activates
additional information
-
tryptase levels do not increase in patients undergoing elective defibrillation or electro convulsive therapy with the administration of suxamethonium
-
additional information
-
acute exposure of human skin to ultraviolet or infrared radiation or heat stimuli increases mast cell numbers and tryptase expression in human skin in vivo
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.05
Ac-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.062
Ac-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.1105
Ac-PANK-AAC
-
pH 7.5, 30C, betaII tryptase
0.1333
Ac-PANK-AAC
-
pH 7.5, 30C, betaI tryptase
0.0089
Ac-PRNK-AAC
-
pH 7.5, 30C, betaII tryptase
0.0145
Ac-PRNK-AAC
-
pH 7.5, 30C, betaI tryptase
0.0165
Ac-PRNR-AAC
-
pH 7.5, 30C, betaII tryptase
0.0186
Ac-PRNR-AAC
-
pH 7.5, 30C, betaI tryptase
0.071
Ac-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.0147
Ac-PRTK-AAC
-
pH 7.5, 30C, betaII tryptase
0.0234
Ac-PRTK-AAC
-
pH 7.5, 30C, betaI tryptase
0.04
Ala-Ala-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.053
Ala-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.1
Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.0002
Benzyloxycarbonyl-Ala-Arg-Arg 4-methylcoumarin 7-amide
-
-
0.0231
benzyloxycarbonyl-Arg 4-methylcoumarin 7-amide
-
-
0.0409
Benzyloxycarbonyl-L-Ala-L-Arg-L-Arg 4-methylcoumarin 7-amide
-
-
0.323
benzyloxycarbonyl-L-Ala-L-Leu-L-Lys 4-methylcoumarin 7-amide
-
-
0.0138
Benzyloxycarbonyl-L-Ala-L-Lys-L-Arg 4-methylcoumarin 7-amide
-
-
0.0148
Benzyloxycarbonyl-L-Ala-L-Lys-L-Lys 4-methylcoumarin 7-amide
-
-
0.0023
bovine prothrombin
-
-
-
0.3
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
1.19
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
2.36
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
4.8 - 5
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
0.062
D-Ile-Pro-Arg-4-nitroanilide
-
pH 8.0, 25C, active enzyme tetramer, in presence of heparin and Na+
0.081
D-Ile-Pro-Arg-4-nitroanilide
-
pH 6.8, 25C, active enzyme tetramer, in presence of heparin and Na+
0.4
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 60 ng polybrene
0.43
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 80 ng polybrene
0.44
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 100 ng polybrene
0.46
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C
1.7
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 100 ng protamine
6.7
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 800 ng protamine
7.4
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 400 ng protamine
8.2
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 200 ng protamine
0.7
D-Phe-Pip-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
0.78
D-Phe-Pip-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1 and S2
0.79
D-Phe-Pip-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
1.64
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
1.75
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
2.59
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
13.5
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
1.12
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
1.41
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
3.11
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
3.49
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
5.03
Glu-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
10.5
Glu-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
0.37
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
0.42
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoforms S1 and S2
0.64
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
0.111
Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.58
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
0.83
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
1.04
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
0.922
N-(p-tosyl)-Gly-Pro-Arg-4-nitroanilide
Q7YS62
pH 8.0, 22C
2.849
N-(p-tosyl)-Gly-Pro-Lys-p-nitroanilide
Q7YS62
pH 8.0, 22C
0.049
N-p-tosyl-Gly-Pro-Arg-p-nitroanilide
-
pH 7.4, 37C, tryptase beta/II
0.12
N-p-tosyl-Gly-Pro-Arg-p-nitroanilide
-
pH 7.4, 37C, D215G mutant
0.19
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 1200 ng polybrene
0.2
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 600 ng polybrene
0.21
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 800 ng or 1000 ng polybrene
0.27
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C
0.41
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 0.001 mg protamine
0.53
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 0.0015 mg protamine
0.64
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 0.002 mg protamine
3.5
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 8.2, 22C, recombinant tryptase
4.2
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 8.2, 22C, HMC-1 tryptase
0.044
Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.043
t-butyloxycarbonyl-Phe-Ser-Arg-4-methyl-coumarin 7-amide
-
pH 8.0, 30C
0.0046
Tert-Butyloxycarbonyl-Gly-Lys-Arg 4-methylcoumarin 7-amide
-
-
0.029
tert-butyloxycarbonyl-Phe-Ser-Arg 4-methylcoumarin 7-amide
-
-
0.031
tert-butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide
-
-
0.35
tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 7.6, 20C, isoform L1
0.44
tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 7.6, 20C, isoforms S1 and S2
0.49
tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 7.6, 20C, isoform L2
0.04
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
0.15
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
0.23
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
0.36
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
1.16
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
additional information
additional information
-
overview: kinetic constant for the hydrolysis of synthetic thioester substrates and 4-nitroanilide substrates by the lung and by the skin enzyme
-
additional information
additional information
-
effect of NaCl on Km
-
additional information
additional information
-
overview: Km values of peptide 4-nitroanilide substrates
-
additional information
additional information
-
-
-
additional information
additional information
-
kinetics and binding constants
-
additional information
additional information
Q7YS62
kinetics
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
141
Ac-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
367
Ac-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
1.1
Ac-PANK-AAC
-
pH 7.5, 30C, betaI tryptase
3.5
Ac-PANK-AAC
-
pH 7.5, 30C, betaII tryptase
0.97
Ac-PRNK-AAC
-
pH 7.5, 30C, betaII tryptase
0.99
Ac-PRNK-AAC
-
pH 7.5, 30C, betaI tryptase
3.8
Ac-PRNR-AAC
-
pH 7.5, 30C, betaI tryptase
21.75
Ac-PRNR-AAC
-
pH 7.5, 30C, betaII tryptase
21.8
Ac-PRNR-AAC
-
pH 7.5, 30C, betaII tryptase
378
Ac-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.99
Ac-PRTK-AAC
-
pH 7.5, 30C, betaI tryptase
1.1
Ac-PRTK-AAC
-
pH 7.5, 30C, betaII tryptase
187
Ala-Ala-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
233
Ala-Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
159
Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
0.8
Benzyloxycarbonyl-Ala-Arg-Arg 4-methylcoumarin 7-amide
-
-
0.05
benzyloxycarbonyl-Arg 4-methylcoumarin 7-amide
-
-
5.35
benzyloxycarbonyl-Arg 4-nitroanilide
-
skin enzyme
5.52
benzyloxycarbonyl-Arg 4-nitroanilide
-
lung enzyme
104
Benzyloxycarbonyl-Gly-Arg 4-trifluoromethylcoumarin 7-amide
-
skin enzyme
107
Benzyloxycarbonyl-Gly-Arg 4-trifluoromethylcoumarin 7-amide
-
lung enzyme
551
Benzyloxycarbonyl-Gly-Pro-Arg 4-nitroanilide
-
skin enzyme
553
Benzyloxycarbonyl-Gly-Pro-Arg 4-nitroanilide
-
lung enzyme
2040
Benzyloxycarbonyl-L-Ala-L-Arg-L-Arg 4-methylcoumarin 7-amide
-
-
1870
benzyloxycarbonyl-L-Ala-L-Leu-L-Lys 4-methylcoumarin 7-amide
-
-
3290
Benzyloxycarbonyl-L-Ala-L-Lys-L-Arg 4-methylcoumarin 7-amide
-
-
1520
Benzyloxycarbonyl-L-Ala-L-Lys-L-Lys 4-methylcoumarin 7-amide
-
-
45.7
Benzyloxycarbonyl-Lys-Arg 4-trifluoromethylcoumarin 7-amide
-
skin and lung enzyme
46.3
bovine prothrombin
-
-
-
0.03 - 0.55
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
1.66
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
2.51
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
2.94
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
3 - 6
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
6.51
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
8.9
Bz-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
97
D-Ile-Pro-Arg-4-nitroanilide
-
pH 6.8, 25C, active enzyme tetramer, in presence of heparin and Na+
170
D-Ile-Pro-Arg-4-nitroanilide
-
pH 8.0, 25C, active enzyme tetramer, in presence of heparin and Na+
3 - 6
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 200 ng protamine
5
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 150 ng polybrene
8
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 100 ng polybrene
9.9
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 80 ng polybrene
14
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C
16
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 100 ng protamine
17
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 60 ng polybrene
26
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 800 ng protamine
40
D-Ile-Pro-Arg-p-nitroanilide
-
pH 6.0, 25C, 400 ng protamine
24.1
D-Phe-Pip-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
27.1
D-Phe-Pip-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
51
D-Phe-Pip-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
59.5
D-Phe-Pip-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
2.8
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
5
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
5.2
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
5.3
D-Pro-Phe-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
0.833
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
7.1
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
16.3
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
21.1
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
31
D-Val-Leu-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
9
Glu-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
60.6
Glu-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
183
Glu-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
1.5
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
1.7
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
2.6
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
56.4
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
56.9
Glu-Pro-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
199
Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
15.2
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
22.9
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
30.5
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
2628
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
23.5
N-(p-tosyl)-Gly-Pro-Arg-4-nitroanilide
Q7YS62
pH 8.0, 22C
12
N-(p-tosyl)-Gly-Pro-Lys-p-nitroanilide
Q7YS62
pH 8.0, 22C
1.9
N-p-tosyl-Gly-Pro-Arg-p-nitroanilide
-
pH 7.4, 37C, D215G mutant
21
N-p-tosyl-Gly-Pro-Arg-p-nitroanilide
-
pH 7.4, 37C, tryptase beta/II
0.74
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 1200 ng polybrene
1.5
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 1000 ng polybrene
2.6
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 800 ng polybrene
3.6
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 600 ng polybrene
3.9
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 0.002 mg protamine
4.3
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C
5.1
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 0.0015 mg protamine
5.8
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 0.001 mg protamine
6.08
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 6.0, 25C, 1200 ng polybrene
490
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 8.2, 22C, recombinant tryptase
540
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 8.2, 22C, HMC-1 tryptase
435
Pro-Ile-Arg-Asn-Lys-5-amino-2-nitrobenzoylamide
-
-
7
t-butyloxycarbonyl-Phe-Ser-Arg-4-methyl-coumarin 7-amide
-
pH 8.0, 30C
0.5
Tert-Butyloxycarbonyl-Gly-Lys-Arg 4-methylcoumarin 7-amide
-
-
1.4
tert-butyloxycarbonyl-L-Val-L-Pro-L-Arg-4-methylcoumarin 7-amide
-
-
2.2
tert-butyloxycarbonyl-Phe-Ser-Arg 4-methylcoumarin 7-amide
-
-
27.9
tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 7.6, 20C, isoform L2
40
tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 7.6, 20C, isoform L1
45.9
tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 7.6, 20C, isoform S2
75.5
tosyl-Gly-Pro-Lys-p-nitroanilide
-
pH 7.6, 20C, isoform S1
1.9
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L1
3
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform L2
5.4
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S2
10.3
Z-D-Arg-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
2630
MeOCO-Nle-Gly-Arg-p-nitroanilide
-
pH 7.6, 20C, isoform S1
additional information
additional information
-
overview: kinetic constant for the hydrolysis of synthetic thioester substrates and 4-nitroanilide substrates by the lung and by the skin enzyme
-
additional information
additional information
-
effect of NaCl on turnover number
-
additional information
additional information
-
of peptide 4-nitroanilide substrates
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00017
(Arg-Trp-Lys-Gly)4(Lys)2Lys-NH2
-
22C, pH not specified in the publication
0.000323
(Lys-Lys-Phe-Gly)4(Lys)2Lys-NH2
-
22C, pH not specified in the publication
0.00063
(Lys-Lys-Phe-Gly)4(Lys)2Lys-NH2
-
22C, pH not specified in the publication
0.000006
1-acetyl-N-[(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]prolinamide
-
-
0.000005
1-methylethyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000005
2-methoxyethyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000018
3-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-1,1-diethylurea
-
-
0.0000096
3-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-1,1-dimethylurea
-
-
0.001
4-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]butanamide
-
-
0.05697
4-aminobenzamidine
-
22C, pH not specified in the publication
0.000012
5-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]pentanamide
-
-
0.0000000953
6-amidino-2-naphthyl p-guanidinobenzoate dimethane sulfonate
-
pH 7.8, 37C
0.000007
6-amino-N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
-
0.000016
6-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
-
0.000023
7-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]heptanamide
-
-
0.000003
acetyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
0.0092
APC-1167
-
pH 8.2, 22C, recombinant tryptase
-
0.0097
APC-1167
-
pH 8.2, 22C
-
0.00053
APC-366
-
pH 6.0, 25C, 4 h incubation
0.0017
APC-366
-
pH 8.2, 22C, recombinant tryptase
0.0028
APC-366
-
pH 8.2, 22C
0.25
APC-366
-
pH 6.0, 25C, 40 min incubation
0.25
Aprotinin
-
pH 8.2, 22C
0.369
Aprotinin
-
pH 8.2, 22C, recombinant tryptase
0.3058
Arg-Trp-Lys-Gly-NH2
-
22C, pH not specified in the publication
0.0025
BABIM
-
pH 8.2, 22C, recombinant tryptase
0.0046
BABIM
-
pH 8.2, 22C
0.00047
benzyl 4-[(3-[N2-[(benzyloxy)carbonyl]-L-lysyl]-1,2,4-oxadiazol-5-yl)methyl]piperazine-1-carboxylate
-
-
0.012
benzyl [(1S)-2-(1,3-benzothiazol-2-yl)-1-(1H-indol-2-ylmethyl)-2-oxoethyl]carbamate
-
-
0.045
benzyl [(1S)-2-(1,3-benzothiazol-2-yl)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)ethyl]carbamate
-
-
0.0073
benzyl [(1S)-5-amino-1-(1,3-benzothiazol-2-ylcarbonyl)pentyl]carbamate
-
-
0.0000037
benzyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
0.000037
benzyl [(1S)-5-amino-1-([5-[4-(benzylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
0.000012
benzyl [(1S)-5-amino-1-([5-[4-(benzyloxy)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
0.0000082
benzyl [(1S)-5-amino-1-([5-[4-([2-[3-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
0.00022
benzyl [(1S)-5-amino-1-([5-[4-([2-[4-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
0.0000024
benzyl [(1S)-5-amino-1-[(5-[4-[(2-thiophen-2-ylethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000039
benzyl [(1S)-5-amino-1-[(5-[4-[(3,4-dimethylbenzyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.0000099
benzyl [(1S)-5-amino-1-[(5-[4-[(3-methylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000003
benzyl [(1S)-5-amino-1-[(5-[4-[(3-phenylpropyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.0000032
benzyl [(1S)-5-amino-1-[(5-[4-[(3-phenylpropyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.00006
benzyl [(1S)-5-amino-1-[(5-[4-[(4-phenylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000013
benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-1-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000011
benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-2-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.00023
benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000011
benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.000034
benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.0000058
benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.00077
benzyl [(1S)-5-amino-1-[[5-(4-methoxybenzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.0000036
benzyl [(1S)-5-amino-1-[[5-(4-[[(2E)-3-phenylprop-2-en-1-yl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.000016
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,4-dichlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.0000035
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,5-difluorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.0000018
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.0000029
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(4-fluorophenoxy)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.00014
benzyl [(1S)-5-amino-1-[[5-(4-[[4-(2-fluorobenzyl)piperazin-1-yl]carbonyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.025
benzyl [(1S,3E)-5-amino-1-(1,3-benzothiazol-2-ylcarbonyl)pent-3-en-1-yl]carbamate
-
-
0.000096
benzyl((1S)-5-amino-1-[(5-(4-[(2,4-dichlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.00001
benzyl((1S)-5-amino-1-[(5-(4-[(3,4-dichlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.000024
benzyl((1S)-5-amino-1-[(5-(4-[(3,4-dimethoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.000013
benzyl((1S)-5-amino-1-[(5-(4-[(3-chlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.000041
benzyl((1S)-5-amino-1-[(5-(4-[(3-methoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.000014
benzyl((1S)-5-amino-1-[(5-(4-[(4-chlorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.000016
benzyl((1S)-5-amino-1-[(5-(4-[(4-fluorobenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.000019
benzyl((1S)-5-amino-1-[(5-(4-[(4-methoxybenzyl)oxy]benzyl)-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.0027
benzyl((1S)-5-amino-1-[(5-benzyl-1,2,4-oxadiazol-3-yl)carbonyl]pentyl)carbamate
-
-
0.00036
benzyl[(1S)-5-amino-1-((5-[3-(2-phenylethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.00012
benzyl[(1S)-5-amino-1-((5-[3-(3-phenylpropoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.000012
benzyl[(1S)-5-amino-1-((5-[4-(2-phenylethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.000025
benzyl[(1S)-5-amino-1-((5-[4-(3-phenylpropoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.00018
benzyl[(1S)-5-amino-1-((5-[4-(benzyloxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.0011
benzyl[(1S)-5-amino-1-((5-[4-(cyclohexylmethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.000078
benzyl[(1S)-5-amino-1-((5-[4-(naphthalen-1-ylmethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.000027
benzyl[(1S)-5-amino-1-((5-[4-(naphthalen-2-ylmethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.00011
ck-MCoEeTI
-
-
-
0.00000062
CRA-2059
-
pH 8.0, 25C, tryptase-beta
0.04
c[-Pro-beta3hArg(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHAc)-CO-]
-
pH not specified in the publication, temperature not specified in the publication
0.000007
c[-Pro-beta3hArg(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHCO-(CH2)5-NH2)-CO-]
-
pH not specified in the publication, temperature not specified in the publication
0.000025
c[-Pro-beta3hPhe(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHCO-(CH2)5-NH2)-CO-]
-
pH not specified in the publication, temperature not specified in the publication
0.38
c[-Pro-beta3Lys(3-H2N-CH2)-D-allo-Ile-vTyr-NH-CH2-CH(NHAc)-CO-]
-
pH not specified in the publication, temperature not specified in the publication
0.0000028
ethyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
-
0.0000019
ethyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
-
0.0000047
ethyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.0000054
ethyl[(1S)-5-amino-1-((5-[4-(2-phenylethoxy)benzyl]-1,2,4-oxadiazol-3-yl)carbonyl)pentyl]carbamate
-
-
0.0000951
gabexate mesilate
-
pH 7.8, 37C
0.4717
Lys-Lys-Phe-Gly-NH2
-
22C, pH not specified in the publication
0.000005
M58539
-
-
0.000033
MCoEeTI
-
-
-
0.000028
MCoEeTI[K10R]
-
-
-
0.0016
MCoTI-I
-
-
-
0.0006
MCoTI-II, MCoTI-II-DELTA[DG]
-
-
-
0.002
MCoTI-II-DELTA[GSDGV]
-
Ki above 0.002 mM
-
0.003
MCoTI-II-DELTA[SDGGV]
-
Ki above 0.003 mM
-
0.000009
MCoTI-II-DELTA[SDGG]
-
-
-
0.00001
MCoTI-II-DELTA[SDGG][K10R]
-
-
-
0.05
MCoTI-II[K10A], MCoTI-II[K10F], MCoTI-II[K10Q]
-
IC50 above 0.05 mM
-
0.085
MCoTI-II[K10R]
-
-
-
0.05
MCoTI-II[K10V], MCoTI-II[K10V]-[I11P], MCoTI-II[PKI]-[AVP]
-
IC50 above 0.05 mM
-
0.000011
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[(2-hydroxyethyl)(methyl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.00013
methyl [(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]carbamate
-
-
0.000017
methyl [5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
-
0.00045
N-[(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-piperidin-4-ylpropyl]-3,4-difluorobenzamide
-
-
0.000021
N-[(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]-3,4-difluorobenzamide
-
-
0.00059
N-[(1S)-3-azetidin-3-yl-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)propyl]-3,4-difluorobenzamide
-
-
0.000004
N-[(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]-3,4-difluorobenzamide
-
-
0.0000021
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-1,3-benzodioxole-5-carboxamide
-
-
0.0000017
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,4-difluorobenzamide
-
-
0.0000015
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,5-difluorobenzamide
-
-
0.0000017
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3-fluorobenzamide
-
-
0.0000019
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-chlorobenzamide
-
-
0.0000018
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-fluorobenzamide
-
-
0.04
N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
-
0.38
N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
-
0.000002
N-[2-(3-chlorophenyl)ethyl]-4-([3-[N2-(2,2-dimethylpropanoyl)-L-lysyl]-1,2,4-oxadiazol-5-yl]methyl)benzamide
-
-
0.00019
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(1,2,3,4-tetrahydroisoquinolin-7-ylsulfanyl)ethane-1,2-diamine
-
-
0.00013
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(1-benzothiophen-2-ylsulfanyl)ethane-1,2-diamine
-
-
0.00021
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(1-benzothiophen-5-ylsulfanyl)ethane-1,2-diamine
-
-
0.0002
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(2,3-dihydro-1H-inden-5-ylsulfanyl)ethane-1,2-diamine
-
-
0.000073
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(naphthalen-2-ylsulfanyl)ethane-1,2-diamine
-
-
0.00076
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-(phenylsulfanyl)ethane-1,2-diamine
-
-
0.00027
N-[3-[4-(aminomethyl)phenyl]propyl]-N'-[(2-methyl-1,3-benzothiazol-6-yl)sulfanyl]ethane-1,2-diamine
-
-
0.0000029
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,2,2-trifluoroacetamide
-
-
0.0000038
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,2-dimethylpropanamide
-
-
0.0000033
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,4-difluorobenzamide
-
-
0.000046
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2,5-dimethylfuran-3-carboxamide
-
-
0.0000062
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2-fluorobenzamide
-
-
0.0000037
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2-methoxyacetamide
-
-
0.0000068
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-2-methylpropanamide
-
-
0.0000076
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-3,4-difluorobenzamide
-
-
0.0000058
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-3-fluorobenzamide
-
-
0.0000066
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-4-chlorobenzamide
-
-
0.0000025
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]-4-fluorobenzamide
-
-
0.0000065
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]cyclopentanecarboxamide
-
-
0.0000046
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]cyclopropanecarboxamide
-
-
0.0000023
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]furan-2-carboxamide
-
-
0.0000098
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]hexanamide
-
-
0.0000057
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]morpholine-4-carboxamide
-
-
0.0000092
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]piperidine-1-carboxamide
-
-
0.000032
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]pyrrolidine-1-carboxamide
-
-
0.000022
N-[5-amino-1-[(5-[4-[2-(3,4-dichlorophenyl)ethoxy]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]tetrahydrofuran-3-carboxamide
-
-
0.0023
Pentamidine
-
pH 8.2, 22C, recombinant tryptase
0.0028
Pentamidine
-
pH 8.2, 22C
0.000025
prop-2-en-1-yl [(1S)-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)-3-pyrrolidin-3-ylpropyl]carbamate
-
-
0.0000012
rLDT1
-
pH 7.6, 25C
-
0.000001
RWJ-56423
-
pH 7.4, 37C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00078
4'-[[5-(phenylethynyl)furan-2-yl]carbonyl]spiro[1-benzofuran-3,1'-cyclohexane]-5-carboximidamide
-
pH 7.4, 37C
0.0000051
cyclotheonamide E4
-
-
0.0000036
JNJ-27390467
-
pH 7.4, 37C
0.000015
[1'-(acetyloxy)-5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.000023
[5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.0000018
[5'-(aminomethyl)-1'-[(methylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.0000057
[5'-(aminomethyl)-1'-[(phenylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.000028
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl](5-benzylfuran-2-yl)methanone
-
pH 7.4, 37C
0.000082
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(2-phenylethyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.0000045
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.00009
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylsulfanyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.0000052
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-chlorophenyl)ethynyl]furan-2-yl]methanone
-
pH 7.4, 37C
0.0000043
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-fluorophenyl)ethynyl]furan-2-yl]methanone
-
pH 7.4, 37C
0.000013
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methoxyphenyl)ethynyl]furan-2-yl]methanone
-
pH 7.4, 37C
0.0000012
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methylphenyl)ethynyl]furan-2-yl]methanone
-
pH 7.4, 37C
0.0032
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-hydroxyphenyl)ethynyl]furan-2-yl]methanone
-
pH 7.4, 37C
0.0000083
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-methylphenyl)ethynyl]furan-2-yl]methanone
-
pH 7.4, 37C
0.0007
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-tert-butylphenyl)ethynyl]furan-2-yl]methanone
-
pH 7.4, 37C
0.000059
[5-[(1E)-1-aminoprop-1-en-1-yl]spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
-
pH 7.4, 37C
0.0000031
[6'-(aminomethyl)-2',3'-dihydrospiro[cyclohexane-1,1'-inden]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
pH 7.4, 37C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.000000055
-
substrate tosyl-Gly-Pro-Lys-4-nitroanilide, pH not specified in the publication, temperature not specified in the publication
1000
-
purified commercial preparation from lung
3930
-
-
additional information
-
-
additional information
-
-
additional information
-
-
additional information
-
specific activity for hydrolysis of model substrates by HAST and rHTs, micromol of nitroanilide min-1/nmol subunit
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
6 - 8.5
-
in complex with heparin
6
-
assay at
7.4
-
assay at
7.5 - 8
-
-
7.5 - 8
-
-
7.5 - 8
Q7YS62
assay at
7.5
-
tryptase associated with trypstatin
8.5
-
tryptase free of trypstatin
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5.5 - 10
-
-
6 - 8.5
-
no activity below pH 6 or above pH 8.5
6 - 9
-
-
6
-
no activity below
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
22
Q7YS62
assay at room temperature
25
-
assay at
25
-
assay at
37
-
assay at
pI VALUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5.1
-
isoelectric focusing
5.7
-
lung mast cell lysate and lung tryptase, isoelectric focusing
5.8
-
skin mast cell lysate, isoelectric focusing
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
basophils preferentially express mast cell protease 11 among the mast cell tryptase family, basophils rather than mast cells are the major source of mast cell protease-11
Manually annotated by BRENDA team
-
significantly more tryptase in peritumoral tissue than in normal breast tissue
Manually annotated by BRENDA team
-
connective tissues of adult mice, MCP-7
Manually annotated by BRENDA team
-
isozyme gammaI-tryptase and gammaII-tryptase
Manually annotated by BRENDA team
-
commercial preparation
Manually annotated by BRENDA team
-
purified commercial preparation
Manually annotated by BRENDA team
-
present in pituitary connective tissue
Manually annotated by BRENDA team
-
from liver capsule
Manually annotated by BRENDA team
-
propagated in nude mice
Manually annotated by BRENDA team
-
cell line HMC-1 obtained from a patient with mast cell leukemia
Manually annotated by BRENDA team
-
mast cell tryptase activates peripheral blood eosinophils to release granule-associated enzymes
Manually annotated by BRENDA team
-
airway mast cells and mast cell-like cell line, HMC-1, delta-tryptase is primarily expressed by mast cells, in tissues such as colon, lung and heart as well as in HMC-1 cells
Manually annotated by BRENDA team
-
mMCP-6 is exclusively expressed in connective tissuetype mast cells, mMCP-7 occurs in early stage cultures of bone marrow-derived mast cells, MCP-11 expression is highest at early stages of mast cell development
Manually annotated by BRENDA team
-
pulmonary mast cell
Manually annotated by BRENDA team
-
skin mast cell
Manually annotated by BRENDA team
-
tryptase predominates in mast cells of mucosal tissue
Manually annotated by BRENDA team
-
mast cell protease-11 is highly expressed by primary basophils and to a much lesser extent, by some mast cells
Manually annotated by BRENDA team
-
connective tissues of adult mice, MCP-7
Manually annotated by BRENDA team
-
tryptase is not cleared by the kidneys into the urine
Manually annotated by BRENDA team
additional information
-
mMCP-6, mMCP-7 can be detected in plasma as early as 20 min after mast cell degranulation
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
of degranulated mast cells
Manually annotated by BRENDA team
-
alpha-tryptase is present at low levels in the circulation, even in the absence of mast cell degranulation
-
Manually annotated by BRENDA team
-
extracellular matrix that surrounds the degranulated mast cell, MCP-6
-
Manually annotated by BRENDA team
-
secreted from activated mast cells
-
Manually annotated by BRENDA team
-
anchored, gamma-tryptase, i.e. transmembrane tryptase
Manually annotated by BRENDA team
-
tryptase and cathepsin-G are colocalized in skin mast cell secretory granules
Manually annotated by BRENDA team
-
alpha-, beta-, and delta-tryptase
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
16000 - 120000
-
gel filtration
651154
29000 - 40000
-
immunoreaction
651154
30000 - 37000
-
Western blotting with monoclonal antibody AA5
651154
100000
-
enzyme-antithrombin III complex, gel filtration
683545
110000
-
human, gel filtration in presence of 0.3 M NaCl
29377
120000
-
human, gel filtration
29373
120000
-
rat, gel filtration
29389
120000
-
gel filtration
651070
120000
-
alpha1-tryptase, X-ray exposure
652893
132000
-
human, gel filtration
29384
132000
-
dog, gel filtration
29391
134000
-
human
29378
135000 - 144000
-
human
29379
140000
-
dog, gel filtration
29382
144000
-
dog
29378
145000 - 160000
-
rat mast cell enzyme
29378
145000
-
rat, gel filtration
29395
150000
-
human mast cell line HMC-1, molecular sieve HPLC
29408
150000
-
rHT, gel filtration
650140
200000
-
gel filtration
650078
360000
-
bovine
29378
360000
-
bovine; gel filtration
29393
360000
-
-
650440
additional information
-
MW of the complex of tryptase and trypstatin: 144000, rat, gel filtration, MW of trypstatin is 7600 on gel filtration
29374
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 39000 + x * 40000, SDS-PAGE of DFP-labelled enzyme
?
-
x * 30000-34000, rat
?
-
x * 31000 + x * 32000, dog, SDS-PAGE of denatured enzyme
?
-
x * 32000 + x * 35000, human cell line HMC-1, SDS-PAGE
?
-
x * 29000 + x * 33000, human, SDS-PAGE
homotetramer
-
-
homotetramer
-
2 * 000, SDS-PAGE
oligomer
-
10 * 35000-38000
oligomer
-
9-12 * 31000-38000, SDS-PAGE
tetramer
-
4 * 32400-36300, human, SDS-PAGE, various enzyme forms
tetramer
-
x * 34000 + x * 38000, human, SDS-PAGE
tetramer
-
4 * 30000-40000, rat, mast cell enzyme
tetramer
-
2 * 34000 + 2 * 33000, human, SDS-PAGE of DFP-inhibited enzyme
tetramer
-
x * 31000 + x * 33000, human, SDS-PAGE, the enzyme is apparently a noncovalently linked tetramer with two sets of dissimilar, although antigenically related polypeptides
tetramer
-
4 * 31000-34000, human
tetramer
-
4 * 30000-35000, dog
tetramer
-
4 * 35000, dog, SDS-PAGE
tetramer
-
4 * 32000, SDS-PAGE
tetramer
-
4 * 30000, rHTalpha, mutant D216G, SDS-PAGE, recombinant rHTbeta
tetramer
-
alpha1-tryptase
tetramer
-
beta/II tryptase
tetramer
-
a homotetramer of four catalytically active subunits, unless stabilized by heparin or high salt, the active tetramer converts to an inactive state consisting of an inactive-destabilized tetramer that reversibly dissociates to inactive monomers upon dilution, overview
tetramer
-
a homotetramer with the active sites facing into the central cavity of the four monomers, the monomers are active, when stabilized by heparin-proteoglycan, and have expanded substrate specificities, overview
tetramer
-
alpha- and beta-tryptase, active form
tetramer
-
beta-tryptase is a tetramer that has enzymatic activity, but requires heparin binding to maintain functional and structural stability, alpha-tryptase has little, if any, enzymatic activity, probably due to a cryptic active site, but is a stable tetramer in the absence of heparin, both forms are in a two-state equilibrium, which is influenced by the residues in the vicinity of the active site and by inhibitor/substrate binding, overview
tetramer
-
structure of enzyme forms, overview
monomer
-
a homotetramer with the active sites facing into the central cavity of the four monomers, the monomers are active, when stabilized by heparin-proteoglycan, and have expanded substrate specificities, overview
additional information
-
activity of different enzyme conformations, overview
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
-
-
glycoprotein
-
carbohydrate is present on each subunit
glycoprotein
-
some of the MW heterogeneity of the multiple forms results from N-linked glycosylation
glycoprotein
-
-
glycoprotein
-
carbohydrate is present on each subunit
glycoprotein
-
treatment of the enzyme with N-glycosidase decreases the subunit MW by 4000, putative glycosylation site at residue 21
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
2.2 A crystal structure of mature alpha1-tryptase, crytallized by vapor diffusion method, space group P2(1)2(1)2(1), with unit cell dimensions of a = 91.44 A, b = 110.69 A, c = 130.09 A
-
3-A crystal structure of beta/II-tryptase
-
3A crystal structure in a complex with 4-amidinophenyl pyruvic acid, large crystals of the tetragonal space group P4(1) with cell axes a = b = 82.93 A
-
beta-tryptase by the hanging drop vapour diffusion, 2 mg/ml protein in 10 mM MES, pH 6.1, and 2 M NaCl mixed with 0.1 M NaOAc, pH 4.6, 0.2 M ammonium sulfate, and 30% PEG 1500, 2-5 days at room temperature, X-ray diffraction structure determination and analysis at 1.6-2.5 A resolution, molecular modeling
-
co-crystallization of free and of leupeptin-complexed alphaI-tryptase mutants, 12 mg/ml protein in 10 mM Mops, pH 6.8, 0.7 M NaCl and 0.2 mM leupeptin at room temperature, sitting drop vapor diffusion method, equilibration against reservoir buffer containing 28% PEG 1500, 2 weeks, X-ray diffraction structure determination and anaylsis at 1.6 A resolution, molecular replacement
-
structure of the rat enzyme at 1.9 A resolution
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
3.5 - 7.5
-
25C, 2 h, relatively stable in this range, rapid loss of activity below and above
29395
additional information
-
inactivation of active monomers at neutral pH without stabilization by heparin-proteoglycans
683545
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
25
-
pH 7.5, 30 min, stable up to
29395
25
-
HST, half-life 24 min, rHtbeta 8.5 min, rHTbeta-E149T 7.5 min, rHTalpha-K192Q-D216G 35 min
650140
30
-
pH 7.5, 30 min, 50% loss of activity
29395
30
-
HST, half-life 4.3 min, rHtbeta 1.7 min, rHTbeta-E149T 2.3 min, rHTalpha-D216G 385 min, rHTalpha-K192Q-D216G 14 min
650140
35
-
pH 7.5, 30 min, complete loss of activity at 35C or above
29395
37
-
HST, half-life 1 min, rHtbeta 0.5 min, rHTbeta-E149T 1.0 min, rHTalpha-D216G 85 min, rHTalpha-K192Q-D216G 1.8 min
650140
additional information
-
presence of 1 M NaCl improves thermal stability, heparin does not stabilize the enzyme against thermal denaturation
29395
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
heparin stabilizes
-
heparin stabilizes human and dog enzyme
-
addition of protein to the tryptase-heparin mixture is needed to keep the enzyme stable
-
calcium destabilizes
-
chondroitin monosulfate stabilizes, prolongs t1/2 at 37C 20fold
-
chondroitin sulfate E stabilizes, prolongs t1/2 at 37C 69fold
-
heparan sufate stabilizes, prolongs t1/2 at 37C 20fold
-
heparin glycosaminoglycan fragments of MW greater than 5700 stabilizes
-
heparin glycosaminoglycan partially stabilizes the tryptase
-
heparin glycosaminoglycan stabilizes, maximal stabilization at a weight ratio to tryptase equal to or greater than unity
-
heparin stabilizes
-
heparin stabilizes human and dog enzyme
-
heparin stabilizes the active tetramer
-
heparin-proteoglycan stabilizes the active enzyme monomers
-
In low-salt buffer the enzyme is labile, at least 1.4 M KCl is needed to keep the enzyme stable if incubated at 37C for 30 min
-
increasing the NaCl concentration from 0.01 M to 1.0 M increases stability of free tryptase, in the presence of stabilizing polysaccharides it decreases the stability of tryptase until dissociation of tryptase from each polysaccharide occurs, thereafter tryptase stability increases as does that of free tryptase
-
kinetic characterization of spontaneous inactivation
-
mature alpha1-tryptase does not require heparin-binding for stability
-
poly-D-glutamic acid stabilizes, prolongs t1/2 at 37C 55fold: Dextran sulfate and heparin provide complete stabilization of tryptase activity for 120 min at 37C
-
stabilized by heparin proteoglycans
-
stable to repeated freeze-thaw cycles
-
heparin stabilizes the enzyme, retains about 50% activity in a low-salt solution after 2 h incubation at 25C
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20C, high salt concentration, 50% glycerol, stable for some months
-
4C, pH 6.1, high salt concentration, stable for about 2 or 3 weeks
-
25C, stable for at least 8 days
-
4C, stable for at least 6 months in buffer containing NaCl, rapid loss of activity without addition of NaCl
-
NaCl, 1 M, necessary for long term storage
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
commercial preparation
-
expression and purification of recombinant human enzyme in a baculovirus system; multiple electrophoretic forms
-
HST and rHT
-
immunoaffinity purification with mouse monoclonal antibody, B2, G4, B2 and C11
-
low MW and high MW isoforms, may represent different gene products or they may result from post-translational modification
-
lung beta-tryptase, commercial preparation
-
multiple forms
-
native enzyme by gel filtration
-
recombinant alpha1-tryptase
-
recombinant alphaI-tryptase mutants from insect cells
-
recombinant enzyme
-
recombinant tryptases alpha and beta/II
-
recombinant tryptases betaI and betaII
-
immunoprecipitation (anti-FLAG M2 agarose), enterokinase cleavage
-
recombinant enzyme
-
multiple isoelectric forms
-
skin-derived enzyme is not associated with trypstatin; with an associated protein (trypstatin) that inhibits the protease activity above pH 7.5 (enzyme from peritoneal mast cells)
-
with an associated protein (trypstatin) that inhibits the protease activity above pH 7.5 (enzyme from peritoneal mast cells)
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
gene mtc1, DNA and amino acid sequence determination and analysis, equine tryptase has alanine at residue 216, rather than glycine, which confers increased arginine substrate specificity in vitro and may restrict fibrinogenolysis in vivo
Q7YS62
cDNA cloned and expressed in the methylotrophic yeast Pichia pastoris as protryptase
-
commercial preparation
-
expressed in Pichia pastoris
-
expressed in Pichia pastoris yeast system pPICZa
-
expression of alphaI-tryptase mutants in insect cells
-
expression of gamma-tryptase as either a soluble, single-chian enzyme with a C-terminal His tag or as a soluble pseudozymogen activated by enterokinase cleavage to form a two-chain protein with an N-terminal His tag. Both recombinant proteins are expressed at high levels in Pichia pastoris
-
expression pattern and sequence comparisons of isozymes, overview
-
genetic localization
-
human mast cell tryptases are the products of a multigene family
-
lung beta-tryptase, commercial preparation
-
skin beta-tryptase, commercial preparation
-
tryptases alpha and beta/II cDNA cloned and expressed in baculovirus-infected high five TM insect cells
-
tryptases betaI and betaII heterolougously expressed in the yeast Pichia pastoris
-
expression pattern and sequence comparisons of isozymes, overview
-
genetic localization
-
recombinant tryptase expressed in human 293 cells
-
version with Flag peptide and enterokinase-cleavage site expressed in Sf9 insect cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
Hymenoptera venom immunotherapy is associated with a small, but continuous decrease of baseline serum mast cell tryptase concentration over time
-
mast cell tryptase level is significantly lower in pregnant women with preeclampsia and healthy pregnant women than in healthy non-pregnant women
-
microphthalmia-associated transcription factor plays a role in regulating the transcription of tryptase gene in human mast cells
-
elevated postmortem mast cell tryptase level indicate anaphylaxis
-
elevated tryptase levels are found to cluster in patients with myeloid neoplasms, including chronic myeloid leukaemia, chronic myelomonocytic leukaemia, myelodysplastic syndromes, acute myeloid leukaemia, and mastocytosis
-
increased tryptase is associated with higher tumor grade and more lymph node metastasis in breast cancer tissue
-
morphometric analysis shows a significantly higher positivity for tryptase in the cords of liveborn fetuses than in those of stillborn fetuses
-
significantly higher concentrations of tryptase are found in peripheral blood of sarcoidosis patients than controls, patients with progressive disease show the highest tryptase concentrations in serum
-
the transcriptional activity of tryptase gene is specifically higher in HMC-1 cells compared to the tryptase-negative cells
-
tryptase levels are higher in individuals that are non-atopic, overweight, or have metabolic syndrome compared to individuals that are atopic, normal weight, or do not have the metabolic syndrome, however, these associations are attenuated after adjusting for age
-
mast cells from IL1RL1-null mice exhibit a marked reduction in MCP-6 expression
-
mast cells lacking IL1RL1 exhibit defective fibroblast-driven tryptase accumulation
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
D215G
-
site-directed mutagenesis, derivative of tryptase alpha and beta/II
D216G
-
active site variant of rHTalpha
D216G
-
site-directed mutagenesis, alphaI-tryptase mutant, crystal structure determination and analysis, the sole mutation of Asp216 to Gly produces a protease with catalytic and instability properties intermediate between those of alpha and beta-tryptases
E149T
-
active site variant of rHTbeta
G215D
-
the mutation distorts the substrate binding site and limits peptidase activity
K192Q
-
active site variant of rHTalpha
K192Q
-
site-directed mutagenesis, alphaI-tryptase mutant, crystal structure determination and analysis, the single mutation of Lys192 to Gln had no effect on activity or enzyme stability
K192Q/D216G
-
active site variant of rHTalpha
R3Q
-
site-directed mutagenesis, derivative of tryptase beta/II
S200A
-
part of catalytic triad, inactive
K192Q/D216G
-
site-directed mutagenesis, alphaI-tryptase mutant, crystal structure determination and analysis
additional information
-
dysfunctional tryptase alleles are always coinherited with functional alleles
Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
reconstitution of active tetramer from inactive monomers, overview
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
-
beta-tryptases are the major focus of drug development for therapeutic inhibition
medicine
-
development of tryptase inhibitors for the treatment of asthma
medicine
-
heparin antagonists potentially may be used in treatment of mast cell-mediated diseases, potent and selective inhibitor of tryptase will be an essential tool to determine the role of tryptase in inflammation and other processes, tryptase plays a role in asthma and other allergic and inflammatory skin diseases like psoriasis and atopic dermatitis
medicine
-
important in bacterial infections of the lung
medicine
-
potent and selective inhibitor of tryptase will be an essential tool to determine the role of tryptase in inflammation and other processes, tryptase plays a role in asthma and other allergic and inflammatory skin diseases like psoriasis and atopic dermatitis
medicine
-
tryptase is a potent activator of pro-uPA, the zymogen form of a protease asociated with tumor metastasis and invasion, viable drug target to create therapeutically useful inhibitors
medicine
-
serum mast cell tryptase level is significantly increased in untreated patients with mastocytosis
medicine
-
the concomitant presence of systemic reactions (especially anaphylaxis) after Hymenoptera stings and increased serum baseline tryptase levels strongly suggests that a bone marrow examination is indicated for the diagnosis of clonal mast cell disease
medicine
-
the number of both tryptase- and cathepsin-G-positive mast cells is significantly higher in cutaneous mastocytosis as compared to normal skin
medicine
-
the serum basal tryptase level can be the indirect link between systemic mastocytosis and Hymenoptera venom allergy
medicine
-
there is no correlation of serum tryptase level with either the severity of psoriasis or the severity of atopic dermatitis, serum total tryptase does not prove to be a useful tool in assessing severity of psoriasis or atopic dermatitis
medicine
-
mast cell tryptase can be an indicator of type I hypersensitivity reaction and thus may serve as a surrogate marker of anaphylaxis
medicine
-
tryptase is a diagnostic marker of myeloid neoplasms and a useful test in clinical haematology
medicine
-
tryptase may represent a marker of sarcoidosis severity
medicine
-
tryptase serum concentrations can discriminate between the allergic and histamine fish poisoning syndromes
medicine
-
tryptase is involved in the itch of chronic dermatitis
medicine
-
viruses utilizes the enzyme to trigger their infectivity and multiplication in lungs, an inhibitor may regulate the enzyme activity and viral infections in vivo