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Cathepsin A

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Target id: 1581

Nomenclature: Cathepsin A

Family: S10: Carboxypeptidase Y

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 480 20q13.12 CTSA cathepsin A
Mouse - 474 2 85.27 cM Ctsa cathepsin A
Rat - 456 3q42 Ctsa cathepsin A
Previous and Unofficial Names Click here for help
carboxypeptidase C | GSL | PPGB | carboxypeptidase Y-like kininase | carboxypeptidase-L | deamidase | lysosomal carboxypeptidase A | lysosomal protective protein | urinary kininase | protective protein for beta-galactosidase | PPCA
Database Links Click here for help
Specialist databases
MEROPS S10.002 (Hs)
Other databases
Alphafold P10619 (Hs), P16675 (Mm), Q6AYS3 (Rn)
BRENDA 3.4.16.5
CATH/Gene3D 3.40.50.1820
ChEMBL Target CHEMBL6115 (Hs), CHEMBL3259490 (Mm)
Ensembl Gene ENSG00000064601 (Hs), ENSMUSG00000017760 (Mm), ENSRNOG00000015857 (Rn)
Entrez Gene 5476 (Hs), 19025 (Mm), 296370 (Rn)
Human Protein Atlas ENSG00000064601 (Hs)
KEGG Enzyme 3.4.16.5
KEGG Gene hsa:5476 (Hs), mmu:19025 (Mm), rno:296370 (Rn)
OMIM 613111 (Hs)
Orphanet ORPHA120888
Pharos P10619 (Hs)
RefSeq Nucleotide NM_000308 (Hs), NM_001167594 (Hs), NM_001127695 (Hs), NM_001038492 (Mm), NM_001011959 (Rn)
RefSeq Protein NP_000299 (Hs), NP_001121167 (Hs), NP_001161066 (Hs), NP_001033581 (Mm), NP_001011959 (Rn)
UniProtKB P10619 (Hs), P16675 (Mm), Q6AYS3 (Rn)
Wikipedia CTSA (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.16.5

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 8a [PMID: 22861813] Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.4 pIC50 4
⤷ pIC50 7.4 (IC50 3.8x10-8 M) [4]
example 166 [WO2014154727] Small molecule or natural product Primary target of this compound Hs Inhibition 7.0 pIC50 3
⤷ pIC50 7.0 (IC50 9.2x10-8 M) [3]
telaprevir Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 2
⤷ pIC50 7.0 (IC50 1x10-7 M) [2]
boceprevir Small molecule or natural product Approved drug Hs Inhibition 6.0 pIC50 1
⤷ pIC50 6.0 (IC50 1x10-6 M) [1]
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Galactosialidosis
OMIM: 256540
Orphanet: ORPHA351

References

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1. Ruf S et al.. (2013) Use of boceprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases. Patent number: WO2013072327. Assignee: Sanofi. Priority date: 14/11/2011. Publication date: 23/05/2013.

2. Ruf S et al. (2013) Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases. Patent number: WO2013072328. Assignee: Sanofi. Priority date: 14/11/2011. Publication date: 23/05/2013.

3. Ruf S et al. (2014) Biaryl-propionic acid derivatives and their use as pharmaceuticals. Patent number: WO2014154727. Assignee: Sanofi. Priority date: 20/03/2013. Publication date: 02/10/2014.

4. Ruf S, Buning C, Schreuder H, Horstick G, Linz W, Olpp T, Pernerstorfer J, Hiss K, Kroll K, Kannt A et al.. (2012) Novel β-amino acid derivatives as inhibitors of cathepsin A. J Med Chem, 55 (17): 7636-49. [PMID:22861813]

How to cite this page

S10: Carboxypeptidase Y: Cathepsin A. Last modified on 05/11/2014. Accessed on 03/11/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1581.