Target Information

Target General Infomation
Target ID
T79068
Former ID
TTDS00384
Target Name
Enoyl-[acyl-carrier-protein] reductase [NADH]
Gene Name
inhA
Synonyms
InhA; NADH-dependent enoyl-ACP reductase; Fatty acid synthetase I; inhA
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Malaria [ICD10: B54]
Mycobacterium tuberculosis infection [ICD10: A15-A19]
Tuberculosis [ICD9: 010-018; ICD10: A15-A19]
Function
Involved in the resistance against the antituberculosis drugs isoniazid and ethionamide.
BioChemical Class
Oxidoreductases acting on CH-CH group of donors
Target Validation
T79068
UniProt ID
P9WGR1
EC Number
EC 1.3.1.9
Sequence
MTGLLDGKRILVSGIITDSSIAFHIARVAQEQGAQLVLTGFDRLRLIQRITDRLPAKAPL
LELDVQNEEHLASLAGRVTEAIGAGNKLDGVVHSIGFMPQTGMGINPFFDAPYADVSKGI
HISAYSYASMAKALLPIMNPGGSIVGMDFDPSRAMPAYNWMTVAKSALESVNRFVAREAG
KYGVRSNLVAAGPIRTLAMSAIVGGALGEEAGAQIQLLEEGWDQRAPIGWNMKDATPVAK
TVCALLSDWLPATTGDIIYADGGAHTQLL
Structure
1BVR; 1ENY; 1ENZ; 1P44; 1P45; 1ZID; 2AQ8; 2AQH; 2AQI; 2AQK; 2B35; 2B36; 2B37; 2H9I; 2IDZ; 2IE0; 2IEB; 2IED; 2NSD; 2NTJ; 2NV6; 2PR2; 2X22; 2X23; 3FNE; 3FNF; 3FNG; 3FNH; 3OEW; 3OEY; 3OF2; 4BGE; 4BGI; 4BII; 4BQP; 4BQR; 4DQU; 4DRE; 4DTI; 4OHU; 4OXK; 4OXN; 4OXY; 4OYR; 4TRJ; 4TZK; 4TZT; 4U0J; 4U0K
Drugs and Mode of Action
Drug(s) Ethionamide Drug Info Approved Tuberculosis [1], [2]
Isoniazid Drug Info Approved Tuberculosis [1]
Prothionamide Drug Info Approved Tuberculosis [3]
Pyrazinamide Drug Info Approved Mycobacterium tuberculosis infection [1], [4], [2]
AFN-1720 Drug Info Phase 2 Bacterial infections [5]
MMV00/0053 Drug Info Terminated Malaria [6]
Inhibitor (4-benzylpiperidin-1-yl)(2-fluorophenyl)methanone Drug Info [7]
(4-benzylpiperidin-1-yl)(3-chlorophenyl)methanone Drug Info [7]
(4-benzylpiperidin-1-yl)(m-tolyl)methanone Drug Info [7]
(4-benzylpiperidin-1-yl)(p-tolyl)methanone Drug Info [7]
(4-phenylpiperazin-1-yl)(p-tolyl)methanone Drug Info [7]
2-(2-aminophenoxy)-5-hexylphenol Drug Info [8]
2-(3-aminophenoxy)-5-hexylphenol Drug Info [8]
2-(4,6-dimethoxypyrimidin-2-yloxy)-5-hexylphenol Drug Info [8]
2-(4-aminophenoxy)-5-hexylphenol Drug Info [8]
2-(4-hexyl-2-methoxyphenoxy)pyrimidine Drug Info [8]
2-bromo-4-methylphenyl 2-nitrobenzoate Drug Info [9]
2-Hexadecynoic acid Drug Info [10]
2-nitro-N-(2,4,5-trichlorophenyl)benzamide Drug Info [9]
4-(2-Thienyl)-1-(4-Methylbenzyl)-1h-Imidazole Drug Info [11]
4-chloro-N-(2,5-dichlorophenyl)-3-nitrobenzamide Drug Info [9]
5-hexyl-2-(2-nitrophenoxy)phenol Drug Info [8]
5-hexyl-2-(3-nitrophenoxy)phenol Drug Info [8]
5-hexyl-2-(4-nitrophenoxy)phenol Drug Info [8]
5-hexyl-2-(pyrazin-2-yloxy)phenol Drug Info [8]
5-hexyl-2-(pyridin-2-yloxy)phenol Drug Info [8]
5-hexyl-2-(pyridin-3-yloxy)phenol Drug Info [8]
5-hexyl-2-(pyridin-4-yloxy)phenol Drug Info [8]
5-hexyl-2-(pyrimidin-2-yloxy)phenol Drug Info [8]
5-hexyl-2-phenoxyphenol Drug Info [8]
5-octyl-2-phenoxyphenol Drug Info [12]
5-PENTYL-2-PHENOXYPHENOL Drug Info [13]
AFN-1720 Drug Info [14]
Beta-D-Glucose Drug Info [11]
C16-Fatty-Acyl-Substrate-Mimic Drug Info [11]
Diclosan Drug Info [11]
Ethionamide Drug Info [3], [15]
Genz-10850 Drug Info [11]
Indole Naphthyridinone Drug Info [11]
Isoniazid Drug Info [16], [17], [18]
MMV00/0053 Drug Info [19]
N-(2,4-dichlorophenyl)-2-nitrobenzamide Drug Info [9]
N-(2,4-dichlorophenyl)-4-methyl-3-nitrobenzamide Drug Info [9]
N-(2,4-dimethylphenyl)-2-nitrobenzamide Drug Info [9]
N-(2,5-dichlorophenyl)-4-methoxy-3-nitrobenzamide Drug Info [9]
N-(2-(4-hexyl-2-hydroxyphenoxy)phenyl)acetamide Drug Info [8]
N-(3,5-dichlorophenyl)-2-nitrobenzamide Drug Info [9]
N-(3,5-dichlorophenyl)-4-methoxy-3-nitrobenzamide Drug Info [9]
N-(3,5-dimethoxyphenyl)-4-methyl-2-nitrobenzamide Drug Info [9]
N-(3-(4-hexyl-2-hydroxyphenoxy)phenyl)acetamide Drug Info [8]
N-(4-(4-hexyl-2-hydroxyphenoxy)phenyl)acetamide Drug Info [8]
N-(4-(diethylamino)phenyl)-2-nitrobenzamide Drug Info [9]
N-(4-METHYLBENZOYL)-4-BENZYLPIPERIDINE Drug Info [13]
Nicotinamide-Adenine-Dinucleotide Drug Info [11]
Prothionamide Drug Info [3], [20]
Pyrazinamide Drug Info [21]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
DRM DRM Info
References
REF 1Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8.
REF 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3Mechanism of thioamide drug action against tuberculosis and leprosy. J Exp Med. 2007 Jan 22;204(1):73-8. Epub 2007 Jan 16.
REF 4(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: 7287).
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038764)
REF 6Annual report of Medicines for Malaria Venture in 2002.
REF 7Bioorg Med Chem. 2007 Nov 1;15(21):6649-58. Epub 2007 Aug 15.Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.
REF 8Bioorg Med Chem Lett. 2008 May 15;18(10):3029-33. Epub 2008 Apr 18.Synthesis and in vitro antimycobacterial activity of B-ring modified diaryl ether InhA inhibitors.
REF 9Eur J Med Chem. 2009 Sep;44(9):3718-30. Epub 2009 Apr 8.Discovery of potential new InhA direct inhibitors based on pharmacophore and 3D-QSAR analysis followed by in silico screening.
REF 10Bioorg Med Chem. 2010 Nov 1;18(21):7475-85. Epub 2010 Sep 18.2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections.
REF 11How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 12J Med Chem. 2008 May 8;51(9):2606-12. Epub 2008 Apr 5.Natural products, small molecules, and genetics in tuberculosis drug development.
REF 13The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 14Affinium Pharmaceuticals Announces the Initiation of a Phase 1 Intravenous Clinical Trial of a New Antibiotic Prodrug, and the Closing of a Follow-on Financing Round. PR Newswire Sep. 4, 2013 10:16 PM.
REF 15Calcium-activated conductance in skate electroreceptors: current clamp experiments. J Gen Physiol. 1977 Feb;69(2):121-43.
REF 16Screening for novel antituberculosis agents that are effective against multidrug resistant tuberculosis. Curr Top Med Chem. 2007;7(5):499-507.
REF 17Enoyl reductases as targets for the development of anti-tubercular and anti-malarial agents. Curr Drug Targets. 2007 Mar;8(3):399-411.
REF 18Diversity in enoyl-acyl carrier protein reductases. Cell Mol Life Sci. 2009 May;66(9):1507-17.
REF 19SAR and pharmacophore models for the rhodanine inhibitors of Plasmodium falciparum enoyl-acyl carrier protein reductase. IUBMB Life. 2010 Mar;62(3):204-13.
REF 20Ability of the Ca2+ ionophores A23187 and ionomycin to mimic some of the effects of the tumor promoter 12-O-tetradecanoylphorbol-13-acetate on hydroperoxide production, ornithine decarboxylase activity, and DNA synthesis in mouse epidermis in vivo. Cancer Res. 1990 Sep 15;50(18):5806-12.
REF 21Pyrazinamide inhibits the eukaryotic-like fatty acid synthetase I (FASI) of Mycobacterium tuberculosis. Nat Med. 2000 Sep;6(9):1043-7.

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