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kallikrein related peptidase 4

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Target id: 2374

Nomenclature: kallikrein related peptidase 4

Family: S1: Chymotrypsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 254 19q13.41 KLK4 kallikrein related peptidase 4
Mouse - 255 7 B4 Klk4 kallikrein related-peptidase 4 (prostase, enamel matrix, prostate)
Rat - 256 1q22 Klk4 kallikrein-related peptidase 4
Previous and Unofficial Names Click here for help
EMSP | ESMP1 | kallikrein 4 | KLK-L1 | Prss17 | PSTS | kallikrein related-peptidase 4 (prostase, enamel matrix, prostate) | kallikrein related-peptidase 4 (prostase
Database Links Click here for help
Specialist databases
MEROPS S01.251 (Hs)
Other databases
Alphafold Q9Y5K2 (Hs)
BRENDA 3.4.21.-
ChEMBL Target CHEMBL4446 (Hs)
Ensembl Gene ENSG00000167749 (Hs), ENSMUSG00000006948 (Mm), ENSRNOG00000018864 (Rn)
Entrez Gene 9622 (Hs), 56640 (Mm), 408210 (Rn)
Human Protein Atlas ENSG00000167749 (Hs)
KEGG Enzyme 3.4.21.-
KEGG Gene hsa:9622 (Hs), mmu:56640 (Mm), rno:408210 (Rn)
OMIM 603767 (Hs)
Orphanet ORPHA139168 (Hs)
Pharos Q9Y5K2 (Hs)
RefSeq Nucleotide NM_004917 (Hs), NM_019928 (Mm), NM_001004101 (Rn)
RefSeq Protein NP_004908 (Hs), NP_064312 (Mm), NP_001004101 (Rn)
UniProtKB Q9Y5K2 (Hs)
Wikipedia KLK4 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.-

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 32 [PMID: 31675166] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 pIC50 1
⤷ pIC50 6.8 (IC50 1.58x10-7 M) [1]
compound 33 [PMID: 19908842] Small molecule or natural product Hs Inhibition 5.0 pIC50 2
⤷ pIC50 5.0 (IC50 9.772x10-6 M) [2]
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Amelogenesis imperfecta, hypomaturation type, IIA1; AI2A1
Synonyms: Amelogenesis imperfecta [Disease Ontology: DOID:2187]
Hypomaturation amelogenesis imperfecta [Orphanet: ORPHA100033]
Disease Ontology: DOID:2187
OMIM: 204700
Orphanet: ORPHA100033

References

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1. De Vita E, Smits N, van den Hurk H, Beck EM, Hewitt J, Baillie G, Russell E, Pannifer A, Hamon V, Morrison A et al.. (2020) Synthesis and Structure-Activity Relationships of N-(4-Benzamidino)-Oxazolidinones: Potent and Selective Inhibitors of Kallikrein-Related Peptidase 6. ChemMedChem, 15 (1): 79-95. [PMID:31675166]

2. Mott BT, Ferreira RS, Simeonov A, Jadhav A, Ang KK, Leister W, Shen M, Silveira JT, Doyle PS, Arkin MR et al.. (2010) Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. J Med Chem, 53 (1): 52-60. [PMID:19908842]

How to cite this page

S1: Chymotrypsin: kallikrein related peptidase 4. Last modified on 06/12/2019. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2374.