细菌羟基烷基喹啉对药物靶点二氢乳清酸脱氢酶抑制作用的结构见解
Structural insights into inhibition of the drug target dihydroorotate dehydrogenase by bacterial hydroxyalkylquinolines.
作者信息
Horwitz Samantha M, Blue Tamra C, Ambarian Joseph A, Hoshino Shotaro, Seyedsayamdost Mohammad R, Davis Katherine M
机构信息
Department of Chemistry, Emory University Atlanta GA 30322 USA
Department of Chemistry, Princeton University Princeton NJ 08544 USA.
出版信息
RSC Chem Biol. 2022 Feb 7;3(4):420-425. doi: 10.1039/d1cb00255d. eCollection 2022 Apr 6.
Hydroxyalkylquinolines (HAQs) are ubiquitious natural products but their interactions with associated protein targets remain elusive. We report X-ray crystal structures of two HAQs in complex with dihydroorotate dehydrogenase (DHODH). Our results reveal the structural basis of DHODH inhibition by HAQs and open the door to downstream structure-activity relationship studies.
羟基烷基喹啉（HAQs）是普遍存在的天然产物，但其与相关蛋白质靶点的相互作用仍不清楚。我们报告了两种HAQs与二氢乳清酸脱氢酶（DHODH）复合物的X射线晶体结构。我们的结果揭示了HAQs抑制DHODH的结构基础，并为下游构效关系研究打开了大门。
Zotero 插件