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cathepsin V

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Target not currently curated in GtoImmuPdb

Target id: 2352

Nomenclature: cathepsin V

Family: C1: Papain

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 334 9q22.33 CTSV cathepsin V
Rat - 334 17p14 Ctsl cathepsin L
Previous and Unofficial Names Click here for help
cathepsin L | cathepsin L1 | CATHL | CatL | CP-2 | cyclic protein 2 | cathepsin L2 | CTSL2 | CTSU | Ctsl1
Database Links Click here for help
Specialist databases
MEROPS C01.009 (Hs)
Other databases
Alphafold O60911 (Hs), P07154 (Rn)
BRENDA 3.4.22.43
ChEMBL Target CHEMBL3272 (Hs), CHEMBL2305 (Rn)
Ensembl Gene ENSG00000136943 (Hs), ENSRNOG00000018566 (Rn)
Entrez Gene 1515 (Hs), 25697 (Rn)
Human Protein Atlas ENSG00000136943 (Hs)
KEGG Enzyme 3.4.22.43
KEGG Gene hsa:1515 (Hs), rno:25697 (Rn)
OMIM 603308 (Hs)
Pharos O60911 (Hs)
RefSeq Nucleotide NM_001201575 (Hs), NM_001333 (Hs), NM_013156 (Rn)
RefSeq Protein NP_001324 (Hs), NP_001188504 (Hs), NP_037288 (Rn)
UniProtKB O60911 (Hs), P07154 (Rn)
Wikipedia CTSV (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF HUMAN CATHEPSIN V COMPLEXED WITH AN IRREVERSIBLE VINYL SULFONE INHIBITOR
PDB Id:  1FH0
Ligand:  K777
Resolution:  1.6Å
Species:  Human
References:  3
Enzyme Reaction Click here for help
EC Number: 3.4.22.43

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
VBY-825 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.6 pKi 1
⤷ pKi 9.6 (Ki 2.5x10-10 M) [1]
citibrasine Small molecule or natural product Hs Inhibition 6.7 pKi 2
⤷ pKi 6.7 (Ki 2x10-7 M) [2]
Citrusinine II Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.4 pKi 2
⤷ pKi 5.4 (Ki 4.2x10-6 M) [2]
Description: Inhibition of human recombinant cathepsin V.
petesicatib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.2 pIC50 4
⤷ pIC50 6.2 (IC50 7x10-7 M) [4]
Immuno Process Associations
Immuno Process:  Antigen presentation

References

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1. Elie BT, Gocheva V, Shree T, Dalrymple SA, Holsinger LJ, Joyce JA. (2010) Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model. Biochimie, 92 (11): 1618-24. [PMID:20447439]

2. Severino RP, Guido RV, Marques EF, Brömme D, da Silva MF, Fernandes JB, Andricopulo AD, Vieira PC. (2011) Acridone alkaloids as potent inhibitors of cathepsin V. Bioorg Med Chem, 19 (4): 1477-81. [PMID:21277783]

3. Somoza JR, Zhan H, Bowman KK, Yu L, Mortara KD, Palmer JT, Clark JM, McGrath ME. (2000) Crystal structure of human cathepsin V. Biochemistry, 39 (41): 12543-51. [PMID:11027133]

4. Tato M, Kumar SV, Liu Y, Mulay SR, Moll S, Popper B, Eberhard JN, Thomasova D, Rufer AC, Gruner S et al.. (2017) Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury. Sci Rep, 7 (1): 2775. [PMID:28584258]

How to cite this page

C1: Papain: cathepsin V. Last modified on 20/04/2021. Accessed on 16/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2352.