Target Information

Target General Infomation
Target ID
T86385
Former ID
TTDC00019
Target Name
Cathepsin G
Gene Name
CTSG
Synonyms
CG; CTSG
Target Type
Clinical Trial
Disease Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45]
Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Function
Serine protease with trypsin- and chymotrypsin-like specificity. Cleaves complement C3. Has antibacterial activity against the Gram-negative bacterium P.aeruginosa, antibacterial activity is inhibited by LPS from P.aeruginosa, Z-Gly-Leu-Phe- CH2Cl and phenylmethylsulfonyl fluoride.
BioChemical Class
Peptidase
Target Validation
T86385
UniProt ID
P08311
EC Number
EC 3.4.21.20
Sequence
MQPLLLLLAFLLPTGAEAGEIIGGRESRPHSRPYMAYLQIQSPAGQSRCGGFLVREDFVL
TAAHCWGSNINVTLGAHNIQRRENTQQHITARRAIRHPQYNQRTIQNDIMLLQLSRRVRR
NRNVNPVALPRAQEGLRPGTLCTVAGWGRVSMRRGTDTLREVQLRVQRDRQCLRIFGSYD
PRRQICVGDRRERKAAFKGDSGGPLLCNNVAHGIVSYGKSSGVPPEVFTRVSSFLPWIRT
TMRSFKLLDQMETPL
Drugs and Mode of Action
Drug(s) JNJ-10311795 Drug Info Phase 2 Asthma; Chronic obstructive pulmonary disease [541688]
Aloxistatin Drug Info Discontinued in Phase 3 Neurological disease [545202]
Dermolastin Drug Info Discontinued in Phase 2 Atopic dermatitis [547642]
Inhibitor Aloxistatin Drug Info [528870]
Bis-Napthyl Beta-Ketophosphonic Acid Drug Info [551393]
compound 1 Drug Info [526092]
compound 4g Drug Info [531910]
Dermolastin Drug Info [536190], [536840], [537435], [551533]
JNJ-10311795 Drug Info [528733]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Lysosome
Renin-angiotensin system
Amoebiasis
Systemic lupus erythematosus
Pathway Interaction Database Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
Reactome Degradation of the extracellular matrix
Activation of Matrix Metalloproteinases
Metabolism of Angiotensinogen to Angiotensins
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
WikiPathways ACE Inhibitor Pathway
Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
References
Ref 541688(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. (Ligand id: 6563).
Ref 545202Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002441)
Ref 547642Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071)
Ref 526092Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.
Ref 528733J Med Chem. 2007 Apr 19;50(8):1727-30. Epub 2007 Mar 16.Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
Ref 528870J Biol Chem. 2007 Jul 20;282(29):20836-46. Epub 2007 May 29.Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Ref 531910N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3993-7.
Ref 536190rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82.
Ref 536840Bioreactor strategies for improving production yield and functionality of a recombinant human protein in transgenic tobacco cell cultures. Biotechnol Bioeng. 2009 Feb 1;102(2):508-20.
Ref 537435Optimization of the bioprocessing conditions for scale-up of transient production of a heterologous protein in plants using a chemically inducible viral amplicon expression system. Biotechnol Prog. 2009 May-Jun;25(3):722-34.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551533Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.

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