Bacterial Transferase MraY, a Source of Inspiration towards New Antibiotics

doi:10.2174/0929867325666180330095154

摘要

细菌对抗生素的耐药性比以往任何时候都更加严重。参与细菌肽聚糖生物合成的酶是开发新抗生素的相关靶标，特别是未被任何市售药物靶向的MraY转移酶。许多研究小组目前正在研究或抑制这种酶。在简要概述了MraY的作用，机制和抑制之后，我们将介绍我们之前合成的含5''-三唑的氨基三糖基尿苷抑制剂的结构 - 活性关系。最近发布的MraY X射线结构使我们能够对商业数据库和我们的内部库进行分子虚拟高通量筛选，从而确定有希望的化合物，以进一步开发新的抗生素。

关键词: MraY，核苷类抗生素，三唑类，分子模拟，对接，生物学评价，诱变。

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Current Medicinal Chemistry

Title:Bacterial Transferase MraY, a Source of Inspiration towards New Antibiotics

Volume: 25 Issue: 42

关键词: MraY，核苷类抗生素，三唑类，分子模拟，对接，生物学评价，诱变。

摘要: The bacterial resistance to antibiotics constitutes more than ever a severe public health problem. The enzymes involved in bacterial peptidoglycan biosynthesis are pertinent targets for developing new antibiotics, notably the MraY transferase that is not targeted by any marketed drug. Many research groups are currently working on the study or the inhibition of this enzyme. After a concise overview of the role, mechanism and inhibition of MraY, the structure–activity relationships of 5’-triazole-containing aminoribosyluridine inhibitors, we previously synthetized, will be presented. The recently published MraY X-ray structures allowed us to achieve a molecular virtual high-throughput screening of commercial databases and our in-house library resulting in the identification of promising compounds for the further development of new antibiotics.

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Bacterial Transferase MraY, a Source of Inspiration towards New Antibiotics, Current Medicinal Chemistry 2018; 25 (42) . https://dx.doi.org/10.2174/0929867325666180330095154

DOI https://dx.doi.org/10.2174/0929867325666180330095154	Print ISSN 0929-8673
Publisher Name Bentham Science Publisher	Online ISSN 1875-533X