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cathepsin G

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Target id: 2348

Nomenclature: cathepsin G

Family: S1: Chymotrypsin

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

Contents:

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 P08311 (Hs), P28293 (Mm), P17977 (Rn)
BRENDA 3.4.21.20
ChEMBL Target CHEMBL4071 (Hs), CHEMBL5622 (Mm)
Ensembl Gene ENSG00000100448 (Hs), ENSMUSG00000040314 (Mm), ENSRNOG00000020647 (Rn)
Entrez Gene 1511 (Hs), 13035 (Mm), 290257 (Rn)
Human Protein Atlas ENSG00000100448 (Hs)
KEGG Enzyme 3.4.21.20
KEGG Gene hsa:1511 (Hs), mmu:13035 (Mm), rno:290257 (Rn)
OMIM 116830 (Hs)
Pharos P08311 (Hs)
RefSeq Nucleotide NM_001911 (Hs), NM_007800 (Mm), NM_001106041 (Rn)
RefSeq Protein NP_001902 (Hs), NP_031826 (Mm), NP_001099511 (Rn)
UniProtKB P08311 (Hs), P28293 (Mm), P17977 (Rn)
Wikipedia CTSG (Hs)
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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2348.