Target General Infomation
Target ID
T70490 (Former ID: TTDR00571)
Target Name
Dipeptidyl peptidase I (CTSC)
Synonyms
Dipeptidyl transferase; Dipeptidyl peptidase 1; DPPI; DPP-I; Cysteine protease dipeptidyl peptidase I; Cathepsin J; Cathepsin C; CPPI
Gene Name
CTSC
Target Type
Clinical trial target
[1]
Disease [+] 1 Target-related Diseases +
1 Bronchiectasis [ICD-11: CA24]
Function
Has dipeptidylpeptidase activity. Active against a broad range of dipeptide substrates composed of both polar and hydrophobic amino acids. Proline cannot occupy the P1 position and arginine cannot occupy the P2 position of the substrate. Can act as both an exopeptidase and endopeptidase. Activates serine proteases such as elastase, cathepsin G and granzymes A and B. Can also activate neuraminidase and factor XIII. Thiol protease.
BioChemical Class
Peptidase
UniProt ID
CATC_HUMAN
EC Number
EC 3.4.14.1
Sequence
MGAGPSLLLAALLLLLSGDGAVRCDTPANCTYLDLLGTWVFQVGSSGSQRDVNCSVMGPQ
EKKVVVYLQKLDTAYDDLGNSGHFTIIYNQGFEIVLNDYKWFAFFKYKEEGSKVTTYCNE
TMTGWVHDVLGRNWACFTGKKVGTASENVYVNIAHLKNSQEKYSNRLYKYDHNFVKAINA
IQKSWTATTYMEYETLTLGDMIRRSGGHSRKIPRPKPAPLTAEIQQKILHLPTSWDWRNV
HGINFVSPVRNQASCGSCYSFASMGMLEARIRILTNNSQTPILSPQEVVSCSQYAQGCEG
GFPYLIAGKYAQDFGLVEEACFPYTGTDSPCKMKEDCFRYYSSEYHYVGGFYGGCNEALM
KLELVHHGPMAVAFEVYDDFLHYKKGIYHHTGLRDPFNPFELTNHAVLLVGYGTDSASGM
DYWIVKNSWGTGWGENGYFRIRRGTDECAIESIAVAATPIPKL
Drugs and Modes of Action
Clinical Trial Drug(s) [+] 1 Clinical Trial Drugs +
1 GSK2793660 Drug Info Phase 1 Bronchiectasis [1]
Mode of Action [+] 2 Modes of Action +
Modulator [+] 1 Modulator drugs +
1 GSK2793660 Drug Info [1]
Inhibitor [+] 4 Inhibitor drugs +
1 (S)-2-amino-N-(1-cyano-2-phenylethyl)acetamide Drug Info [2]
2 Cathepsin C inhibitors Drug Info [3]
3 GNF-PF-5434 Drug Info [4]
4 PMID3941405C3d Drug Info [5]
Target Regulators
Target-regulating microRNAs
Target Affiliated Biological Pathways
KEGG Pathway [+] 1 KEGG Pathways +
1 Lysosome
NetPath Pathway [+] 3 NetPath Pathways +
1 IL2 Signaling Pathway
2 IL4 Signaling Pathway
3 TGF_beta_Receptor Signaling Pathway
Reactome [+] 3 Reactome Pathways +
1 COPII (Coat Protein 2) Mediated Vesicle Transport
2 MHC class II antigen presentation
3 Cargo concentration in the ER
WikiPathways [+] 4 WikiPathways +
1 miR-targeted genes in muscle cell - TarBase
2 miR-targeted genes in lymphocytes - TarBase
3 miR-targeted genes in leukocytes - TarBase
4 miR-targeted genes in epithelium - TarBase
Target-Related Models and Studies
Target Validation
References
REF 1 ClinicalTrials.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 2 Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3614-7.
REF 3 URL: 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).
REF 4 Substrate optimization for monitoring cathepsin C activity in live cells. Bioorg Med Chem. 2009 Feb 1;17(3):1064-70.
REF 5 Carboxyl-modified amino acids and peptides as protease inhibitors. J Med Chem. 1986 Jan;29(1):104-11.

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