Abstract
The InhA-related enoyl-ACP reductase, an enzyme involved in fatty acid synthesis, is one of the best validated targets for the development of anti-tubercular agents. However, the majority of isoniazid (INH)-resistant clinical strains are observed mainly due to the emergence of KatG mutants that do not form an INH-NAD adduct. Thus compounds that directly inhibit InhA avoiding activation by KatG would be promising candidates for combating MDR-TB. Herein, some predominant examples of InhA direct inhibitors recently developed are reviewed and special attention is paid to 3Dstructures of InhA in drug design process.
Keywords: InhA, Anti-tubercular agents, Isoniazid, KatG, INH-NAD adduct, Indirect inhibitors, Direct inhibitors, Drug design
Mini-Reviews in Medicinal Chemistry
Title: Recent Progress in the Identification and Development of InhA Direct Inhibitors of Mycobacterium tuberculosis
Volume: 10 Issue: 3
Author(s): X.Y. Lu, Q.D. You and Y.D. Chen
Affiliation:
Keywords: InhA, Anti-tubercular agents, Isoniazid, KatG, INH-NAD adduct, Indirect inhibitors, Direct inhibitors, Drug design
Abstract: The InhA-related enoyl-ACP reductase, an enzyme involved in fatty acid synthesis, is one of the best validated targets for the development of anti-tubercular agents. However, the majority of isoniazid (INH)-resistant clinical strains are observed mainly due to the emergence of KatG mutants that do not form an INH-NAD adduct. Thus compounds that directly inhibit InhA avoiding activation by KatG would be promising candidates for combating MDR-TB. Herein, some predominant examples of InhA direct inhibitors recently developed are reviewed and special attention is paid to 3Dstructures of InhA in drug design process.
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Cite this article as:
Lu X.Y., You Q.D. and Chen Y.D., Recent Progress in the Identification and Development of InhA Direct Inhibitors of Mycobacterium tuberculosis, Mini-Reviews in Medicinal Chemistry 2010; 10 (3) . https://dx.doi.org/10.2174/138955710791185064
DOI https://dx.doi.org/10.2174/138955710791185064 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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