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

Top ▲

cathepsin H

target has curated data in GtoImmuPdb

Target id: 2349

Nomenclature: cathepsin H

Family: C1: Papain

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 335 15q25.1 CTSH cathepsin H
Mouse - 333 9 E3.1 Ctsh cathepsin H
Rat - 333 8q31 Ctsh cathepsin H
Previous and Unofficial Names
ACC-4 | ACC-5 | cathepsin B3 | cathepsin BA | CPSB
Database Links
Specialist databases
MEROPS C01.040 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.22.16

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 Value Parameter Reference
compound 1b [PMID: 16290936] Hs Inhibition 7.4 pKi 1
pKi 7.4 (Ki 4x10-8 M) [1]
compound 1e [PMID: 27285276] 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
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes
GO:0019882 antigen processing and presentation TAS
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 2 GO processes
GO:0001913 T cell mediated cytotoxicity ISS
GO:0002250 adaptive immune response IEP
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 2 GO processes
GO:0001913 T cell mediated cytotoxicity ISS
GO:0002250 adaptive immune response IEP
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0002764 immune response-regulating signaling pathway IDA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes
GO:0002764 immune response-regulating signaling pathway IDA
GO:0043312 neutrophil degranulation TAS
Clinically-Relevant Mutations and Pathophysiology
Disease:  Narcolepsy-cataplexy
Synonyms: Cataplexy and narcolepsy [Disease Ontology: DOID:9199]
Disease Ontology: DOID:9199
Orphanet: ORPHA2073

References

Show »

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 23/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2349.