cathepsin B | C1: Papain | IUPHAR/BPS Guide to PHARMACOLOGY

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cathepsin B

target has curated data in GtoImmuPdb

Target id: 2343

Nomenclature: cathepsin B

Family: C1: Papain

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
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
cathepsin B1 | CB | RSG-2
Database Links
Specialist databases
MEROPS C01.060 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.22.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
Z-Arg-Leu-Val-Agly-Ile-Val-OMe Hs Inhibition 10.1 pKi 2
pKi 10.1 (Ki 8.8x10-11 M) [2]
LHVS Hs Inhibition 5.9 pIC50 1
pIC50 5.9 (IC50 1.36x10-6 M) [1]
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

References

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1. 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]

2. 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 21/04/2017. Accessed on 27/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2343.