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cathepsin B

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Target id: 2343

Nomenclature: cathepsin B

Family: C1: Papain

Contents:

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
Alphafold P07858 (Hs), P10605 (Mm), P00787 (Rn)
BRENDA 3.4.22.1
ChEMBL Target CHEMBL4072 (Hs), CHEMBL5187 (Mm), CHEMBL2602 (Rn)
Ensembl Gene ENSG00000164733 (Hs), ENSMUSG00000021939 (Mm), ENSRNOG00000010331 (Rn)
Entrez Gene 1508 (Hs), 13030 (Mm), 64529 (Rn)
Human Protein Atlas ENSG00000164733 (Hs)
KEGG Enzyme 3.4.22.1
KEGG Gene hsa:1508 (Hs), mmu:13030 (Mm), rno:64529 (Rn)
OMIM 116810 (Hs)
Pharos P07858 (Hs)
RefSeq Nucleotide NM_147783 (Hs), NM_147781 (Hs), NM_147782 (Hs), NM_001908 (Hs), NM_147780 (Hs), NM_007798 (Mm), NM_022597 (Rn)
RefSeq Protein NP_680093 (Hs), NP_680092 (Hs), NP_680091 (Hs), NP_680090 (Hs), NP_001899 (Hs), NP_031824 (Mm), NP_072119 (Rn)
UniProtKB P07858 (Hs), P10605 (Mm), P00787 (Rn)
Wikipedia CTSB (Hs)
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 6
⤷ pKi 10.1 (Ki 8.8x10-11 M) [6]
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]
K11777 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.5 pKi 2
⤷ pKi 5.5 (Ki 3x10-6 M) [2]
compound 1 [PMID: 40415551] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 4
⤷ pIC50 6.4 (IC50 4.36x10-7 M) [4]
LHVS Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.9 pIC50 3
⤷ pIC50 5.9 (IC50 1.36x10-6 M) [3]
poststatin Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 5
⤷ [5]
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:  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. 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. Mellott DM, Tseng CT, Drelich A, Fajtová P, Chenna BC, Kostomiris DH, Hsu J, Zhu J, Taylor ZW, Kocurek KI et al.. (2021) A Clinical-Stage Cysteine Protease Inhibitor blocks SARS-CoV-2 Infection of Human and Monkey Cells. ACS Chem Biol, 16 (4): 642-650. [PMID:33787221]

3. 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]

4. Porzberg MRB, Groenewold GJM, Lyoo H, Jakob AKMH, Titulaer WHC, Cavina L, Poelaert KCK, Zwaagstra M, Dieteren CEJ, Lemmers JGH et al.. (2025) Peptidomimetic Phenoxymethyl Ketone Warheads as Potent Dual-Mode Inhibitors against SARS-CoV-2 Mpro and Cathepsin. J Med Chem, [Epub ahead of print]. [PMID:40415551]

5. 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]

6. 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 27/05/2025. Accessed on 02/07/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2343.