基于结构的LpxC抑制剂发现
Structure-based discovery of LpxC inhibitors.
作者信息
Zhang Jing, Chan Audrey, Lippa Blaise, Cross Jason B, Liu Christopher, Yin Ning, Romero Jan Antoinette C, Lawrence Jonathan, Heney Ryan, Herradura Prudencio, Goss Jennifer, Clark Cynthia, Abel Cassandra, Zhang Yanzhi, Poutsiaka Katherine M, Epie Felix, Conrad Mary, Mahamoon Azard, Nguyen Kien, Chavan Ajit, Clark Edward, Li Tong-Chuan, Cheng Robert K, Wood Michael, Andersen Ole A, Brooks Mark, Kwong Jason, Barker John, Parr Ian Barrie, Gu Yugui, Ryan M Dominic, Coleman Scott, Metcalf Chester A
机构信息
Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
出版信息
Bioorg Med Chem Lett. 2017 Apr 15;27(8):1670-1680. doi: 10.1016/j.bmcl.2017.03.006. Epub 2017 Mar 6.
The emergence and spread of multidrug-resistant (MDR) Gram negative bacteria presents a serious threat for public health. Novel antimicrobials that could overcome the resistance problems are urgently needed. UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) is a cytosolic zinc-based deacetylase that catalyzes the first committed step in the biosynthesis of lipid A, which is essential for the survival of Gram-negative bacteria. Our efforts toward the discovery of novel LpxC inhibitors are presented herein.
多重耐药（MDR）革兰氏阴性菌的出现和传播对公众健康构成了严重威胁。迫切需要能够克服耐药问题的新型抗菌药物。UDP-3-O-（R-3-羟基肉豆蔻酰）-N-乙酰葡糖胺脱乙酰酶（LpxC）是一种基于锌的胞质脱乙酰酶，它催化脂多糖A生物合成中的首个关键步骤，而脂多糖A对革兰氏阴性菌的存活至关重要。本文介绍了我们在发现新型LpxC抑制剂方面所做的努力。
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