3.4.21.B12: prostase

This is an abbreviated version!
For detailed information about prostase, go to the full flat file.

Word Map on EC 3.4.21.B12

3.4.21.B12

klk4

kallikreins

amelogenins

amelogenesis

ameloblastin

enamelysin

incisor

imperfecta

maturation-stage

amelx

amelotin

medicine

secretory-stage

hypomineralized

masp-1

hypomaturation

crystallite

metalloproteinase-20

analysis

diagnostics

Reaction

proteolysis of polypeptides =

Synonyms

EM serine proteinase 1, EMSP1, enamel matrix serine protease 1, HK4, K4, kallikrein 1-related peptidase 4, kallikrein 4, kallikrein-4, kallikrein-4 proteinase, kallikrein-like protein 1, kallikrein-related peptidase, kallikrein-related peptidase 4, kallikrein-related peptidase-4, KLK, KLK-4 proteinase, KLK-L1, KLK4, More, peptidase S01.251, prostase, prostate cancer serine protease, PRSS17, S01.251, serine protease 1, serine protease 17, tissue kallikrein-related peptidase 4

ECTree

3 Hydrolases

3.4 Acting on peptide bonds (peptidases)

3.4.21 Serine endopeptidases

3.4.21.B12 prostase

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Results	in table
10	Activating Compound
4	AA Sequence
15	Application
2	CAS Registry Number
20	Cloned(Commentary)
2	Crystallization (Commentary)
255	Disease/ Diagnostics
1	Expression
9	General Information
4	IC50 Value
12	Inhibitors
7	KM Value [mM]
13	Localization
10	Molecular Weight [Da]
27	Natural Substrates/ Products (Substrates)
43	Organism
6	pH Optimum
1	pH Range
1	pI Value
10	Posttranslational Modification
6	Protein Variants
10	Purification (Commentary)
10	Reaction
1	Reaction Type
42	Reference
2	Renatured (Commentary)
92	Source Tissue
4	Specific Activity [micromol/min/mg]
1	Storage Stability
92	Substrates and Products (Substrate)
8	Subunits
71	Synonyms
3	Temperature Optimum [°C]
6	Turnover Number [1/s]

Inhibitors

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Inhibitors on EC 3.4.21.B12 - prostase

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alpha2-antiplasmin

Aprotinin

benzamidine

93% inhibition at 10 mM

Co2+

MCoTI-II

a 34-amino acid cyclic peptide found in the seeds of Momordica cochinchinensis. By grafting a preferred KLK4 cleavage sequence into MCoTI-II, a highly potent KLK4 inhibitor is produced that displays 100000fold selectivity over related kallikreins and the ability to penetrate cells. Additionally, by substituting positively charged noncontact residues in this compound, a potent and selective KLK4 inhibitor is produced that does not penetrate cells. The inhibitors are shown to be nontoxic to human cells and stable in human serum. These KLK4 inhibitors provide useful chemical tools to further define the role(s) of both intracellular and extracellular KLK4 in prostate cancer cell lines and disease models

752370

Nalpha-p-tosyl-L-lysine chloromethyl ketone

Homo sapiens

85% inhibition at 1 mM; i.e. TLCK

Ni2+

siRNA

mediates knockdown of endogenous KLK4 in LNCaP prostate cancer cells whereby inhibiting their proliferation

685946

Soybean trypsin inhibitor

Homo sapiens

99% inhibition at 1 mg/ml

647338

Zn2+

Homo sapiens

enzyme activity is high at zinc concentrations below 0.001 mM and decreases to about 30% at 0.1 mM. Zinc affects the K4 active site via the salt-bridge formed between the N terminus and Asp194 required for a functional active site

681390

additional information

2 entries