Target Information

Target General Infomation
Target ID
T70490
Former ID
TTDR00571
Target Name
Dipeptidyl-peptidase I
Gene Name
CTSC
Synonyms
Cathepsin C; Cathepsin J; Cysteine protease dipeptidyl peptidase I; DPP-I; DPPI; Dipeptidyl peptidase I; Dipeptidyl transferase; CTSC
Target Type
Clinical Trial
Disease Bronchiectasis [ICD9: 494, 748.61; ICD10: J47, Q33.4]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Function
Thiol protease. Has dipeptidylpeptidase activity. Can act as both an exopeptidase and endopeptidase. Activates serine proteases such as elastase, cathepsin g and granzymes a and b. Can also activateneuramindase and factor xiii.
BioChemical Class
Peptidase
Target Validation
T70490
UniProt ID
P53634
EC Number
EC 3.4.14.1
Sequence
MGAGPSLLLAALLLLLSGDGAVRCDTPANCTYLDLLGTWVFQVGSSGSQRDVNCSVMGPQ
EKKVVVYLQKLDTAYDDLGNSGHFTIIYNQGFEIVLNDYKWFAFFKYKEEGSKVTTYCNE
TMTGWVHDVLGRNWACFTGKKVGTASENVYVNIAHLKNSQEKYSNRLYKYDHNFVKAINA
IQKSWTATTYMEYETLTLGDMIRRSGGHSRKIPRPKPAPLTAEIQQKILHLPTSWDWRNV
HGINFVSPVRNQASCGSCYSFASMGMLEARIRILTNNSQTPILSPQEVVSCSQYAQGCEG
GFPYLIAGKYAQDFGLVEEACFPYTGTDSPCKMKEDCFRYYSSEYHYVGGFYGGCNEALM
KLELVHHGPMAVAFEVYDDFLHYKKGIYHHTGLRDPFNPFELTNHAVLLVGYGTDSASGM
DYWIVKNSWGTGWGENGYFRIRRGTDECAIESIAVAATPIPKL
Drugs and Mode of Action
Drug(s) GSK2793660 Drug Info Phase 1 Bronchiectasis [524641]
Inhibitor (S)-2-amino-N-(1-cyano-2-phenylethyl)acetamide Drug Info [528170]
Cathepsin C inhibitors Drug Info [543599]
compound 3d Drug Info [533497]
GNF-PF-5434 Drug Info [529350]
Modulator GSK2793660 Drug Info [524641]
Pathways
KEGG Pathway Lysosome
NetPath Pathway IL2 Signaling Pathway
IL4 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Reactome COPII (Coat Protein 2) Mediated Vesicle Transport
MHC class II antigen presentation
Cargo concentration in the ER
WikiPathways miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in leukocytes - TarBase
miR-targeted genes in epithelium - TarBase
References
Ref 524641ClinicalTrials.gov (NCT02058407) A Study to Evaluate the Safety, Tolerability, Pharmacokinetics (PK), Pharmacodynamics (PD) and Food Effect of Single or Repeat Doses of GSK2793660 in Healthy Subjects. U.S. National Institutes of Health.
Ref 524641ClinicalTrials.gov (NCT02058407) A Study to Evaluate the Safety, Tolerability, Pharmacokinetics (PK), Pharmacodynamics (PD) and Food Effect of Single or Repeat Doses of GSK2793660 in Healthy Subjects. U.S. National Institutes of Health.
Ref 528170Bioorg Med Chem Lett. 2006 Jul 1;16(13):3614-7. Epub 2006 May 2.Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.
Ref 529350Bioorg Med Chem. 2009 Feb 1;17(3):1064-70. Epub 2008 Feb 7.Substrate optimization for monitoring cathepsin C activity in live cells.
Ref 533497Carboxyl-modified amino acids and peptides as protease inhibitors. J Med Chem. 1986 Jan;29(1):104-11.
Ref 543599(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2344).

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