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Information on EC 3.4.21.34 - plasma kallikrein and Organism(s) Rattus norvegicus and UniProt Accession P14272

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EC Tree
     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.34 plasma kallikrein
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This record set is specific for:
Rattus norvegicus
UNIPROT: P14272 not found.
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Word Map
The taxonomic range for the selected organisms is: Rattus norvegicus
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota
Reaction Schemes
selective cleavage of some Arg-/- and Lys-/- bonds, including Lys-/-Arg and Arg-/-Ser in (human) kininogen to release bradykinin
Synonyms
kallikrein, prekallikrein, plasma kallikrein, urinary kallikrein, kininogenase, plasma prekallikrein, plasma pk, pancreatic kallikrein, klk13, klkb1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
bradykininogenase
-
-
-
-
callicrein
-
-
-
-
depot-Padutin
-
-
-
-
dilminal D
-
-
-
-
Fletcher factor
-
-
-
-
glumorin
-
-
-
-
kallidinogenase
-
-
-
-
kallikrein
-
-
-
-
kallikrein I
-
-
-
-
kallikrein II
-
-
-
-
kininogenase
-
-
-
-
kininogenin
-
-
-
-
onokrein P
-
-
-
-
padreatin
-
-
-
-
padutin
-
-
-
-
pancreatic kallikrein
-
-
-
-
Plasma prekallikrein
-
-
-
-
serum kallikrein
-
-
-
-
urinary kallikrein
-
-
-
-
urokallikrein
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
410538-33-9
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
factor XII + H2O
?
show the reaction diagram
activation of the factor XII, bound to negatively charged surfaces
-
?, ir
kininogen + H2O
bradykinin + fragments of kininogen
show the reaction diagram
high-molecular weight kininogen
-
?, ir
Prorenin + H2O
Renin + ?
show the reaction diagram
kininogen + H2O
bradykinin + ?
show the reaction diagram
kininogen + H2O
bradykinin + fragments of kininogen
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Ala-Lys-Arg-4-methylcoumarin 7-amide
N-benzyloxycarbonyl-Ala-Lys-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-GEFIKKSSFQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIK + KSSFQ-N-(2,4-dinitrophenyl)-ethylene diamine
show the reaction diagram
-
synthetic fluorogenic substrate
67% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-GEFIKKSSFQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIKK + SSFQ-N-(2,4-dinitrophenyl)-ethylene diamine
show the reaction diagram
-
synthetic fluorogenic substrate
33% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-GEFIKKSSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIK + KSSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine
show the reaction diagram
-
synthetic fluorogenic substrate
62% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-GEFIKKSSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIKK + SSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine
show the reaction diagram
-
synthetic fluorogenic substrate
38% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-IKKSSF-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-IKK + SSF-N-(2,4-dinitrophenyl)-ethylene diamine
show the reaction diagram
-
synthetic fluorogenic substrate
identification by mass spectroscopy
?
Prorenin + H2O
Renin + ?
show the reaction diagram
-
rat prorenin, very low activity
-
ir
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
factor XII + H2O
?
show the reaction diagram
activation of the factor XII, bound to negatively charged surfaces
-
ir
kininogen + H2O
bradykinin + fragments of kininogen
show the reaction diagram
high-molecular weight kininogen
-
ir
Prorenin + H2O
Renin + ?
show the reaction diagram
activation of prorenin, involved in the renin-angiotensin system
-
ir
kininogen + H2O
bradykinin + ?
show the reaction diagram
-
-
-
-
?
kininogen + H2O
bradykinin + fragments of kininogen
show the reaction diagram
-
-
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-benzyl-1H-pyrazole-4-carboxylic acid 4-carbamimidoyl-benzylamide
-
ASP-440, small molecule inhibitor of plasma kallikrein
2-[3'-acetyl-5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2'-fluoro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-carbamoyl-6-hydroxybiphenyl-3-yl]butanedioic acid
-
inhibitor with the best potency and selectivity profile for plasma kallikrein versus related serine proteases. This compound is highly stable in vivo and could be further developed for the treatment and inflammatory or coagulation disorders. Pharmacokinetic data
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-cyano-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-4'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methoxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methylbiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methoxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methylbiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methoxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methylbiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
antipain
-
-
bicyclic peptide Ac-CiS1F2[Aze]3Y4[HArg]5Cii[Ala(PsiCH2-NH)]6H7Q8D9L10Ciii
-
-
-
bicyclic peptide Ac-CiS1W2P3A4R5CiiL6H7Q8D9L10Ciii
-
-
-
C1-inhibitor
-
-
-
diisopropylfluorophosphate
-
-
human IgG1 monoclonal antibody DX-2930
-
potently and specifically inhibits plasma kallikrein
-
leupeptin
-
-
Soybean trypsin inhibitor
-
-
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
factor XIIa
activation by cleavage into light- and heavy-chain, that are linked by one or more disulfide bridges after cleavage
-
factor XIIa
-
-
-
additional information
binding to negatively charged surfaces activates the enzyme
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000006
2-[3'-acetyl-5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000013
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000012
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2'-fluoro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000003
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
-
0.0000005
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-carbamoyl-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000003 - 0.000065
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
0.00001
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-cyano-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000037
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-4'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000006
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methoxybiphenyl-3-yl]butanedioic acid
-
-
0.000006
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methylbiphenyl-3-yl]butanedioic acid
-
-
0.000005
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methoxybiphenyl-3-yl]butanedioic acid
-
-
0.000004
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methylbiphenyl-3-yl]butanedioic acid
-
-
0.000027
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methoxybiphenyl-3-yl]butanedioic acid
-
-
0.000018
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methylbiphenyl-3-yl]butanedioic acid
-
-
0.0000008
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.00000017
human IgG1 monoclonal antibody DX-2930
-
at pH 7.5 and 30°C
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
8
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
gene KLKB1 or PK, plasma kallikrein precursor
SwissProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
additional information
-
at least four promoter regions and diverse transcription start sites can be utilized. Tissue-dependent alternative use of promoters and transcription starts is evident from a comparison of the start sites in liver and kidney
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
plasma
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
cerebral hematoma expansion triggered by intracerebral infusion of autologous blood is increased in diabetic rats, and this response is ameliorated by plasma kallikrein inhibition and deficiency, respectively
physiological function
-
hyperglycemia increases cerebral hematoma expansion by plasma kallikrein-mediated osmotic sensitive inhibition of hemostasis, plasma kallikrein-mediated inhibition of collagen-induced platelet aggregation is enhanced by hyperglycemia
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
KLKB1_RAT
638
1
71274
Swiss-Prot
Secretory Pathway (Reliability: 2)
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Paquin, J.; Benjannet, S.; Sawyer, N.; Lazure, C.; Chretien, M.; Seidah, N.G.
Rat plasma kallikrein: purification, NH2-terminal sequencing and development of a specific radioimmunoassay
Biochim. Biophys. Acta
999
103-110
1989
Rattus norvegicus
Manually annotated by BRENDA team
Boeckmann, B.; Bairoch, A.; Apweiler, R.; Blatter, M.C.; Estreicher, A.; Gasteiger, E.; Martin M.J.; Michoud, K.; O'Donovan, C.; Phan, I.; Pilbout, S.; Schneider, M.
The SWISS-PROT protein knowledgebase and its supplement TrEMBL
Nucleic Acids Res.
31
365-370
2003
Homo sapiens (P03952), Mus musculus (P26262), Rattus norvegicus (P14272)
Manually annotated by BRENDA team
Almeida, P.C.; Chagas, J.R.; Cezari, M.H.; Juliano, M.A.; Juliano, L.
Hydrolysis by plasma kallikrein of fluorogenic peptides derived from prorenin processing site
Biochim. Biophys. Acta
1479
83-90
2000
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Neth, P.; Arnhold, M.; Sidarovich, V.; Bhoola, K.D.; Fink, E.
Expression of the plasma prekallikrein gene: utilization of multiple transcription start sites and alternative promoter regions
Biol. Chem.
386
101-109
2005
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Young, W.B.; Rai, R.; Shrader, W.D.; Burgess-Henry, J.; Hu, H.; Elrod, K.C.; Sprengeler, P.A.; Katz, B.A.; Sukbuntherng, J.; Mordenti, J.
Small molecule inhibitors of plasma kallikrein
Bioorg. Med. Chem. Lett.
16
2034-2036
2006
Rattus norvegicus
Manually annotated by BRENDA team
Phipps, J.A.; Clermont, A.C.; Sinha, S.; Chilcote, T.J.; Bursell, S.E.; Feener, E.P.
Plasma kallikrein mediates angiotensin II type 1 receptor-stimulated retinal vascular permeability
Hypertension
53
175-181
2009
Rattus norvegicus
Manually annotated by BRENDA team
Liu, J.; Gao, B.B.; Clermont, A.C.; Blair, P.; Chilcote, T.J.; Sinha, S.; Flaumenhaft, R.; Feener, E.P.
Hyperglycemia-induced cerebral hematoma expansion is mediated by plasma kallikrein
Nat. Med.
17
206-210
2011
Rattus norvegicus
Manually annotated by BRENDA team
Kenniston, J.; Faucette, R.; Martik, D.; Comeau, S.; Lindberg, A.; Kopacz, K.; Conley, G.; Chen, J.; Viswanathan, M.; Kastrapeli, N.; Cosic, J.; Mason, S.; DiLeo, M.; Abendroth, J.; Kuzmic, P.; Ladner, R.; Edwards, T.; TenHoor, C.; Adelman, B.; Nixon, A.;
Inhibition of plasma kallikrein by a highly specific active site blocking antibody
J. Biol. Chem.
289
23596-23608
2014
Macaca fascicularis, Mus musculus, Rattus norvegicus, Homo sapiens (P03952), Homo sapiens
Manually annotated by BRENDA team
Teufel, D.P.; Bennett, G.; Harrison, H.; van Rietschoten, K.; Pavan, S.; Stace, C.; Le Floch, F.; Van Bergen, T.; Vermassen, E.; Barbeaux, P.; Hu, T.T.; Feyen, J.H.M.; Vanhove, M.
Stable and long-lasting, novel bicyclic peptide plasma kallikrein inhibitors for the treatment of diabetic macular edema
J. Med. Chem.
61
2823-2836
2018
Rattus norvegicus
Manually annotated by BRENDA team