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cathepsin H

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2349

Nomenclature: cathepsin H

Family: C1: Papain

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 335 15q25.1 CTSH cathepsin H
Mouse - 333 9 47.4 cM Ctsh cathepsin H
Rat - 333 8q31 Ctsh cathepsin H
Previous and Unofficial Names Click here for help
CPSB | ACC-4 | ACC-5 | cathepsin B3 | cathepsin BA
Database Links Click here for help
Specialist databases
MEROPS C01.040 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction Click here for help
EC Number:

Download all structure-activity data for this target as a CSV file go icon to follow link

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 1b [PMID: 16290936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pKi 1
pKi 7.4 (Ki 4x10-8 M) [1]
compound 1e [PMID: 27285276] Small molecule or natural product Hs Inhibition 6.4 pIC50 3
pIC50 6.4 (IC50 4.4x10-7 M) [3]
Immunopharmacology Comments
Cathepsin H may act as a pro-granzyme B convertase [2], granzyme B being the most potent proapoptotic cytotoxin of the granule exocytosis pathway of cytotoxic lymphocytes. It is similarly active in NK cells [4]. However, results from cathepsin H-null mice indicate a high degree of functional redundancy in granzyme B maturation, with enzymes other than cathepsin H active in this process.
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
Immuno Process:  Antigen presentation
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Cellular signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Narcolepsy-cataplexy
Synonyms: Cataplexy and narcolepsy [Disease Ontology: DOID:9199]
Disease Ontology: DOID:9199
Orphanet: ORPHA2073


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1. Adkison KK, Barrett DG, Deaton DN, Gampe RT, Hassell AM, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA et al.. (2006) Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?. Bioorg Med Chem Lett, 16 (4): 978-83. [PMID:16290936]

2. D'Angelo ME, Bird PI, Peters C, Reinheckel T, Trapani JA, Sutton VR. (2010) Cathepsin H is an additional convertase of pro-granzyme B. J Biol Chem, 285 (27): 20514-9. [PMID:20435891]

3. Garg S, Raghav N. (2016) 2,5-Diaryloxadiazoles and their precursors as novel inhibitors of cathepsins B, H and L. Bioorg Chem, 67: 64-74. [PMID:27285276]

4. Magister Š, Tseng HC, Bui VT, Kos J, Jewett A. (2015) Regulation of split anergy in natural killer cells by inhibition of cathepsins C and H and cystatin F. Oncotarget, 6 (26): 22310-27. [PMID:26247631]

How to cite this page

C1: Papain: cathepsin H. Last modified on 21/04/2017. Accessed on 22/07/2024. IUPHAR/BPS Guide to PHARMACOLOGY,