Target Information

Target General Infomation
Target ID
T05114
Former ID
TTDR00197
Target Name
Chymase
Gene Name
CMA1
Synonyms
Mast cell protease I; CMA1
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]
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.
BioChemical Class
Peptidase
Target Validation
T05114
UniProt ID
P23946
EC Number
EC 3.4.21.39
Sequence
MLLLPLPLLLFLLCSRAEAGEIIGGTECKPHSRPYMAYLEIVTSNGPSKFCGGFLIRRNF
VLTAAHCAGRSITVTLGAHNITEEEDTWQKLEVIKQFRHPKYNTSTLHHDIMLLKLKEKA
SLTLAVGTLPFPSQFNFVPPGRMCRVAGWGRTGVLKPGSDTLQEVKLRLMDPQACSHFRD
FDHNLQLCVGNPRKTKSAFKGDSGGPLLCAGVAQGIVSYGRSDAKPPAVFTRISHYRPWI
NQILQAN
Drugs and Mode of Action
Drug(s) ASB17061 Drug Info Phase 2 Atopic dermatitis [524171]
JNJ-10311795 Drug Info Phase 2 Asthma; Chronic obstructive pulmonary disease [541688]
SUN13834 Drug Info Phase 2 Gram-positive bacterial infection [536094]
BAY 11-42524 Drug Info Phase 1 Heart failure [549544]
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
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 524171ClinicalTrials.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 536094Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.
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 549544Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040276)
Ref 525207ClinicalTrials.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 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 528779Bioorg 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 532439Immunology of atopic eczema: overcoming the Th1/Th2 paradigm. Allergy. 2013 Aug;68(8):974-82.
Ref 535508Chymase inhibitor ameliorates eosinophilia in mice infected with Nippostrongylus brasiliensis. Int Arch Allergy Immunol. 2002 Jul;128(3):235-9.
Ref 535651Development 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 535652Therapeutic potential of a specific chymase inhibitor in atopic dermatitis. Jpn J Pharmacol. 2002 Nov;90(3):214-7.
Ref 535865Impact of chymase inhibitor on cardiac function and survival after myocardial infarction. Cardiovasc Res. 2003 Nov 1;60(2):413-20.
Ref 543597(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 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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