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cathepsin B

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2343

Nomenclature: cathepsin B

Family: C1: Papain

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 339 8p23.1 CTSB cathepsin B
Mouse - 339 14 D1 Ctsb cathepsin B
Rat - 339 15p12 Ctsb cathepsin B
Previous and Unofficial Names Click here for help
cathepsin B1 | CB | RSG-2
Database Links Click here for help
Specialist databases
MEROPS C01.060 (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: 3.4.22.1

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
Z-Arg-Leu-Val-Agly-Ile-Val-OMe Peptide Hs Inhibition 10.1 pKi 4
pKi 10.1 (Ki 8.8x10-11 M) [4]
VBY-825 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.5 pKi 1
pKi 9.5 (Ki 3.3x10-10 M) [1]
LHVS Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.9 pIC50 2
pIC50 5.9 (IC50 1.36x10-6 M) [2]
poststatin Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 3
[3]
Description: IC50 is 2.1 μg/ml in vitro.
Immunopharmacology Comments
Cathepsins B, H and L have become important therapeutic targets as their proteolytic activity has been implicated in several pathological inflammatory conditions, such as arthritis and periodontitis. Therefore, pharmacological inhibitors of these enzymes are in development as novel therapeutics.
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Barrier integrity
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0046718 viral entry into host cell IEA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 2 GO processes
GO:0034097 response to cytokine IEP
GO:0070670 response to interleukin-4 IEP

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. Méthot N, Rubin J, Guay D, Beaulieu C, Ethier D, Reddy TJ, Riendeau D, Percival MD. (2007) Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. J. Biol. Chem., 282 (29): 20836-46. [PMID:17535802]

3. Tsuda M, Muraoka Y, Nagai M, Aoyagi T, Takeuchi T. (1996) Poststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues. J. Antibiot., 49 (9): 890-9. [PMID:8931723]

4. Wieczerzak E, Drabik P, Łankiewicz L, Ołdziej S, Grzonka Z, Abrahamson M, Grubb A, Brömme D. (2002) Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. J. Med. Chem., 45 (19): 4202-11. [PMID:12213061]

How to cite this page

C1: Papain: cathepsin B. Last modified on 05/06/2020. Accessed on 03/03/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2343.