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kallikrein related peptidase 6

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Target not currently curated in GtoImmuPdb

Target id: 2376

Nomenclature: kallikrein related peptidase 6

Family: S1: Chymotrypsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 244 19q13.41 KLK6 kallikrein related peptidase 6
Mouse - 253 7 B4-B5 Klk6 kallikrein related-peptidase 6
Rat - 251 1q22 Klk6 kallikrein related-peptidase 6
Previous and Unofficial Names Click here for help
brain serine protease | BSP | kallikrein 29 | kallikrein 6 | Klk29 | Klk7 | MSP | myelencephalon-specific protease | neurosin | protease serine 9 | protease, serine, 18 | Prss18 | Prss9 | kallikrein-related peptidase 6
Database Links Click here for help
Specialist databases
MEROPS S01.236 (Hs)
Other databases
Alphafold Q92876 (Hs)
BRENDA 3.4.21.-
ChEMBL Target CHEMBL4448 (Hs)
Ensembl Gene ENSG00000167755 (Hs), ENSMUSG00000050063 (Mm), ENSRNOG00000031927 (Rn)
Entrez Gene 5653 (Hs), 19144 (Mm), 29245 (Rn)
Human Protein Atlas ENSG00000167755 (Hs)
KEGG Enzyme 3.4.21.-
KEGG Gene hsa:5653 (Hs), mmu:19144 (Mm), rno:29245 (Rn)
OMIM 602652 (Hs)
Pharos Q92876 (Hs)
RefSeq Nucleotide NM_002774 (Hs), NM_001012964 (Hs), NM_001012965 (Hs), NM_001164696 (Mm), NM_019175 (Rn)
RefSeq Protein NP_002765 (Hs), NP_001012982 (Hs), NP_001012983 (Hs), NP_001158168 (Mm), NP_062048 (Rn)
UniProtKB Q92876 (Hs)
Wikipedia KLK6 (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 8.6 pIC50 2
⤷ pIC50 8.6 (IC50 2.5x10-9 M) [2]
DKFZ‐251 Small molecule or natural product Hs Inhibition 6.9 pIC50 1
⤷ pIC50 6.9 (IC50 1.3x10-7 M) [1]
compound 5 {PMID: 24900446] Small molecule or natural product Hs Inhibition 5.8 pIC50 3
⤷ pIC50 5.8 (IC50 1.5x10-6 M) [3]
Immuno Process Associations
Immuno Process:  Tissue repair

References

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1. De Vita E, Schüler P, Lovell S, Lohbeck J, Kullmann S, Rabinovich E, Sananes A, Heßling B, Hamon V, Papo N et al.. (2018) Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity. J Med Chem, 61 (19): 8859-8874. [PMID:30212625]

2. 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]

3. Liang G, Chen X, Aldous S, Pu SF, Mehdi S, Powers E, Giovanni A, Kongsamut S, Xia T, Zhang Y et al.. (2012) Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group. ACS Med Chem Lett, 3 (2): 159-64. [PMID:24900446]

How to cite this page

S1: Chymotrypsin: kallikrein related peptidase 6. Last modified on 06/12/2019. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2376.