Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT4H0V2)

DTT 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
DTT Type	Clinical trial target	[1]
BioChemical Class	Peptidase
UniProt ID	CATC_HUMAN
TTD ID	T70490
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
EC Number	EC 3.4.14.1
Sequence	MGAGPSLLLAALLLLLSGDGAVRCDTPANCTYLDLLGTWVFQVGSSGSQRDVNCSVMGPQ EKKVVVYLQKLDTAYDDLGNSGHFTIIYNQGFEIVLNDYKWFAFFKYKEEGSKVTTYCNE TMTGWVHDVLGRNWACFTGKKVGTASENVYVNIAHLKNSQEKYSNRLYKYDHNFVKAINA IQKSWTATTYMEYETLTLGDMIRRSGGHSRKIPRPKPAPLTAEIQQKILHLPTSWDWRNV HGINFVSPVRNQASCGSCYSFASMGMLEARIRILTNNSQTPILSPQEVVSCSQYAQGCEG GFPYLIAGKYAQDFGLVEEACFPYTGTDSPCKMKEDCFRYYSSEYHYVGGFYGGCNEALM KLELVHHGPMAVAFEVYDDFLHYKKGIYHHTGLRDPFNPFELTNHAVLLVGYGTDSASGM DYWIVKNSWGTGWGENGYFRIRRGTDECAIESIAVAATPIPKL
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.
KEGG Pathway	Lysosome (hsa04142 )
Reactome Pathway	MHC class II antigen presentation (R-HSA-2132295 ) Cargo concentration in the ER (R-HSA-5694530 ) COPII (Coat Protein 2) Mediated Vesicle Transport (R-HSA-204005 )
BioCyc Pathway	MetaCyc:HS03265-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This DTT

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BI 1291583	DMOZGBQ	Non-cystic fibrosis bronchiectasis	CA24	Phase 2	[2]
GSK2793660	DMSGNVK	Bronchiectasis	CA24	Phase 1	[1]
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3 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(S)-2-amino-N-(1-cyano-2-phenylethyl)acetamide	DMN1G8L	Discovery agent	N.A.	Investigative	[3]
GNF-PF-5434	DMP9AIH	Discovery agent	N.A.	Investigative	[4]
PMID3941405C3d	DM6ZOW4	Discovery agent	N.A.	Investigative	[5]
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References

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.
2	Clinical pipeline report, company report or official report of boehringer-ingelheim
3	Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3614-7.
4	Substrate optimization for monitoring cathepsin C activity in live cells. Bioorg Med Chem. 2009 Feb 1;17(3):1064-70.
5	Carboxyl-modified amino acids and peptides as protease inhibitors. J Med Chem. 1986 Jan;29(1):104-11.