Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T86385
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| Former ID |
TTDC00019
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| Target Name |
Cathepsin G
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| Gene Name |
CTSG
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| Synonyms |
CG; CTSG
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| Target Type |
Clinical Trial
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| Disease | Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99] | ||||
| Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45] | |||||
| 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.
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| BioChemical Class |
Peptidase
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| Target Validation |
T86385
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| UniProt ID | |||||
| EC Number |
EC 3.4.21.20
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| Sequence |
MQPLLLLLAFLLPTGAEAGEIIGGRESRPHSRPYMAYLQIQSPAGQSRCGGFLVREDFVL
TAAHCWGSNINVTLGAHNIQRRENTQQHITARRAIRHPQYNQRTIQNDIMLLQLSRRVRR NRNVNPVALPRAQEGLRPGTLCTVAGWGRVSMRRGTDTLREVQLRVQRDRQCLRIFGSYD PRRQICVGDRRERKAAFKGDSGGPLLCNNVAHGIVSYGKSSGVPPEVFTRVSSFLPWIRT TMRSFKLLDQMETPL |
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| Drugs and Mode of Action | |||||
| Drug(s) | JNJ-10311795 | Drug Info | Phase 2 | Asthma; Chronic obstructive pulmonary disease | [1] |
| Aloxistatin | Drug Info | Discontinued in Phase 3 | Neurological disease | [2] | |
| Dermolastin | Drug Info | Discontinued in Phase 2 | Atopic dermatitis | [3] | |
| Inhibitor | Aloxistatin | Drug Info | [4] | ||
| Bis-Napthyl Beta-Ketophosphonic Acid | Drug Info | [5] | |||
| compound 1 | Drug Info | [6] | |||
| compound 4g | Drug Info | [7] | |||
| Dermolastin | Drug Info | [8], [9], [10], [11] | |||
| JNJ-10311795 | Drug Info | [12] | |||
| 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 1 | (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 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002441) | ||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071) | ||||
| REF 4 | J 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 5 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 6 | Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. | ||||
| REF 7 | N-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 8 | rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82. | ||||
| REF 9 | Bioreactor 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 10 | Optimization 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 11 | Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009. | ||||
| REF 12 | J 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. | ||||
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