摘要
在细胞二型脂肪酸生物合成酶中,β-酮酰-ACP缩合酶Ⅲ(FabH)启动了第一个酰基辅酶A与丙二酰-ACP的连接,形成了乙酰乙酰基-ACP。它对细菌有机体生存和特异性的关键作用使它成为新型抗菌药物至关重要的一个靶点。在过去的十年中,许多FabH的结构在多种微生物中被发现,描述了它们催化口袋的三维立体结构的详细信息。这有利于FabH抑制剂的合理设计,这将为对抗耐多种药物菌种的药物研究提供框架。这个综述涵盖了在脂肪酸合成酶生化和结构研究中最新的研究进展,并更新了相关的主要抑制剂。
关键词: 抗菌,活性中心,β-酮酰-ACP缩合酶Ⅲ(FabH),抑制剂,二型脂肪酸生物合成酶
Current Medicinal Chemistry
Title:Bacterial β-Ketoacyl-Acyl Carrier Protein Synthase III (FabH) as a Target for Novel Antibacterial Agents Design
Volume: 22 Issue: 5
Author(s): X.Y. Lu, J. Tang, Z. Zhang and K. Ding
Affiliation:
关键词: 抗菌,活性中心,β-酮酰-ACP缩合酶Ⅲ(FabH),抑制剂,二型脂肪酸生物合成酶
摘要: In bacterial type II fatty acid biosynthesis (FAS-II), β-ketoacyl-acyl carrier protein (ACP) synthase III (FabH) initiates the first condensation of acyl-CoA and malonyl-ACP to form acetoacetyl-ACP. Its key role for organism survival and specificity to bacteria make it as an essential target for the discovery of novel antibacterial agents. Over the last decade, several structures of FabH from diverse microorganisms have been solved, giving detailed information about the three-dimensional features of the catalytic pocket. This has facilitated the rational design of FabH inhibitors, which provides a framework for future development of antibiotics against multi-drug resistant strains. This review covers recent advances in the biochemical and structural research of FabH and updates the main families of related inhibitors.
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Cite this article as:
X.Y. Lu, J. Tang, Z. Zhang and K. Ding , Bacterial β-Ketoacyl-Acyl Carrier Protein Synthase III (FabH) as a Target for Novel Antibacterial Agents Design, Current Medicinal Chemistry 2015; 22 (5) . https://dx.doi.org/10.2174/0929867322666141212115236
DOI https://dx.doi.org/10.2174/0929867322666141212115236 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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