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cathepsin G

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2348

Nomenclature: cathepsin G

Family: S1: Chymotrypsin

This target is also described as a ligand entry: cathepsin Gcathepsin Gcathepsin G

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 255 14q12 CTSG cathepsin G
Mouse - 261 14 28.19 cM Ctsg cathepsin G
Rat - 26 15p12 Ctsg cathepsin G
Previous and Unofficial Names Click here for help
vimentin-specific protease | VSP
Database Links Click here for help
Specialist databases
MEROPS S01.133 (Hs)
Other databases
Alphafold
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: 3.4.21.20

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
compound 1 [PMID: 11425539] Small molecule or natural product Hs Inhibition 9.4 pIC50 1
pIC50 9.4 (IC50 3.9x10-10 M) [1]
aloxistatin Small molecule or natural product Hs Inhibition 6.0 pIC50 2
pIC50 6.0 (IC50 1.1x10-6 M) [2]
compound 4g [PMID: 22595175] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.8 pIC50 3
pIC50 4.8 (IC50 1.42x10-5 M) [3]
Immunopharmacology Comments
Cathepsin G is a leukocyte serine protease of the chymotrypsin family, related to neutrophil elastase and the granzymes. It is stored in azurophil granules and acts intracellularly to degrade ingested host pathogens and axtracellularly to breakdown ECM components at sites of inflammation. Cathepsin G is implicated in a number of inflammatory diseases, including chronic obstructive pulmonary disease and rheumatoid arthritis.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cellular signalling
Immuno Process:  Immune regulation

References

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1. Aoyama Y, Uenaka M, Konoike T, Hayasaki-Kajiwara Y, Naya N, Nakajima M. (2001) Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. Bioorg Med Chem Lett, 11 (13): 1691-4. [PMID:11425539]

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. Santana AB, Lucas SD, Gonçalves LM, Correia HF, Cardote TA, Guedes RC, Iley J, Moreira R. (2012) N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases. Bioorg Med Chem Lett, 22 (12): 3993-7. [PMID:22595175]

How to cite this page

S1: Chymotrypsin: cathepsin G. Last modified on 10/03/2020. Accessed on 02/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2348.