Target Information
Target General Infomation | |||||
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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 | |||||
Inhibitor | 2-(N-Morpholino)-Ethanesulfonic Acid | Drug Info | [551393] | ||
BAY 11-42524 | Drug Info | [525207] | |||
BCEAB | Drug Info | [535651] | |||
Benzylsulfinic Acid | Drug Info | [551374] | |||
CHYMOSTATIN | Drug Info | [528779] | |||
JNJ-10311795 | Drug Info | [528733] | |||
KM-01221 | Drug Info | [543597] | |||
NK3201 | Drug Info | [535865] | |||
Phenylalanylmethane | Drug Info | [551393] | |||
Rac-2q | Drug Info | [528779] | |||
SUN-C8257 | Drug Info | [535508] | |||
Y-40613 | Drug Info | [535652] | |||
Modulator | ASB17061 | Drug Info | [532439] | ||
SUN13834 | Drug Info | ||||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 524171 | 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 536094 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | ||||
Ref 525207 | 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 528733 | 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 528779 | 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 532439 | Immunology of atopic eczema: overcoming the Th1/Th2 paradigm. Allergy. 2013 Aug;68(8):974-82. | ||||
Ref 535508 | Chymase inhibitor ameliorates eosinophilia in mice infected with Nippostrongylus brasiliensis. Int Arch Allergy Immunol. 2002 Jul;128(3):235-9. | ||||
Ref 535651 | 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 535652 | Therapeutic potential of a specific chymase inhibitor in atopic dermatitis. Jpn J Pharmacol. 2002 Nov;90(3):214-7. | ||||
Ref 535865 | Impact of chymase inhibitor on cardiac function and survival after myocardial infarction. Cardiovasc Res. 2003 Nov 1;60(2):413-20. |
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