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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

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
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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 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
GO Annotations:  Associated to 1 GO processes
GO:0042246 tissue regeneration NAS

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 28/02/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2376.