Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T05114
|
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| Former ID |
TTDR00197
|
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| Target Name |
Chymase
|
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| Gene Name |
CMA1
|
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| Synonyms |
Mast cell protease I; CMA1
|
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| Target Type |
Clinical Trial
|
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| 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] | |||||
| Cardiovascular disorder [ICD10: I00-I99] | |||||
| Gram-positive bacterial infection [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104] | |||||
| Heart failure [ICD9: 428; ICD10: I50] | |||||
| Function |
Major secreted protease of mast cells with suspected roles in vasoactive peptide generation, extracellular matrix degradation, and regulation of gland secretion.
|
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| BioChemical Class |
Peptidase
|
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| Target Validation |
T05114
|
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| UniProt ID | |||||
| EC Number |
EC 3.4.21.39
|
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| Sequence |
MLLLPLPLLLFLLCSRAEAGEIIGGTECKPHSRPYMAYLEIVTSNGPSKFCGGFLIRRNF
VLTAAHCAGRSITVTLGAHNITEEEDTWQKLEVIKQFRHPKYNTSTLHHDIMLLKLKEKA SLTLAVGTLPFPSQFNFVPPGRMCRVAGWGRTGVLKPGSDTLQEVKLRLMDPQACSHFRD FDHNLQLCVGNPRKTKSAFKGDSGGPLLCAGVAQGIVSYGRSDAKPPAVFTRISHYRPWI NQILQAN |
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| Drugs and Mode of Action | |||||
| Drug(s) | ASB17061 | Drug Info | Phase 2 | Atopic dermatitis | [1] |
| JNJ-10311795 | Drug Info | Phase 2 | Asthma; Chronic obstructive pulmonary disease | [2] | |
| SUN13834 | Drug Info | Phase 2 | Gram-positive bacterial infection | [3] | |
| BAY 11-42524 | Drug Info | Phase 1 | Heart failure | [4] | |
| Inhibitor | 2-(N-Morpholino)-Ethanesulfonic Acid | Drug Info | [5] | ||
| BAY 11-42524 | Drug Info | [6] | |||
| BCEAB | Drug Info | [7] | |||
| Benzylsulfinic Acid | Drug Info | [8] | |||
| CHYMOSTATIN | Drug Info | [9] | |||
| JNJ-10311795 | Drug Info | [10] | |||
| KM-01221 | Drug Info | [11] | |||
| NK3201 | Drug Info | [12] | |||
| Phenylalanylmethane | Drug Info | [5] | |||
| Rac-2q | Drug Info | [9] | |||
| SUN-C8257 | Drug Info | [13] | |||
| Y-40613 | Drug Info | [14] | |||
| Modulator | ASB17061 | Drug Info | [15] | ||
| SUN13834 | Drug Info | ||||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Renin-angiotensin system | ||||
| Reactome | Activation of Matrix Metalloproteinases | ||||
| Metabolism of Angiotensinogen to Angiotensins | |||||
| WikiPathways | ACE Inhibitor Pathway | ||||
| Metabolism of Angiotensinogen to Angiotensins | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT01756898) A Study to Evaluate the Efficacy, Safety and Pharmacokinetics of ASB17061 Capsules in Adult Subjects With Atopic Dermatitis. U.S. National Institutes of Health. | ||||
| REF 2 | (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 3 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | ||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040276) | ||||
| REF 5 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 6 | ClinicalTrials.gov (NCT02452515) A Single-blind Pilot Study to Investigate Safety and Tolerability of the Chymase Inhibitor BAY1142524 in Clinically Stable Patients With Left-ventricular Dysfunction. | ||||
| REF 7 | Development of a chymase inhibitor: pharmacological characterization of a chymase inhibitor in inflamed tissue remodeling and fibrosis. Jpn J Pharmacol. 2002 Nov;90(3):206-9. | ||||
| REF 8 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
| REF 9 | Bioorg Med Chem Lett. 2007 Jun 15;17(12):3431-4. Epub 2007 Mar 16.Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors. | ||||
| REF 10 | 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. | ||||
| REF 11 | (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: 2340). | ||||
| REF 12 | Impact of chymase inhibitor on cardiac function and survival after myocardial infarction. Cardiovasc Res. 2003 Nov 1;60(2):413-20. | ||||
| REF 13 | Chymase inhibitor ameliorates eosinophilia in mice infected with Nippostrongylus brasiliensis. Int Arch Allergy Immunol. 2002 Jul;128(3):235-9. | ||||
| REF 14 | Therapeutic potential of a specific chymase inhibitor in atopic dermatitis. Jpn J Pharmacol. 2002 Nov;90(3):214-7. | ||||
| REF 15 | Immunology of atopic eczema: overcoming the Th1/Th2 paradigm. Allergy. 2013 Aug;68(8):974-82. | ||||
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