Efficient discovery of novel antimicrobials through integration of synthesis and testing in crude ribosome extract

Zitai Sang; Yongping Lu; Yuanzheng Zhou; Yuan Ju; Qi An; Silan Shen; Jianyou Shi; Jun He; Tao Yang; Youfu Luo

doi:10.1039/C9CC00144A

Efficient discovery of novel antimicrobials through integration of synthesis and testing in crude ribosome extract†

Zitai Sang,

‡^a Yongping Lu,‡^b Yuanzheng Zhou,‡^a Yuan Ju,^a Qi An,^a Silan Shen,^c Jianyou Shi,^d Jun He,^a Tao Yang*^ae and Youfu Luo

*^a

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* Corresponding authors

^a State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center for Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China
E-mail: luo_youfu@scu.edu.cn

^b Pharmacy College, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China

^c Department of Gastroenterology, West China Hospital, Sichuan University, Chengdu, Sichuan, China

^d Individualized Medication Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610072, Sichuan, China

^e Laboratory of Human Diseases and Immunotherapies, West China Hospital, Sichuan University, Chengdu, Sichuan, China
E-mail: michael_2012@126.com

Abstract

By coupling in situ [2+3] Huisgen cycloaddition with an in vitro transcription/translation luminescence assay in a crude ribosomal extract, a robust and accurate high-throughput platform was successfully developed and applied for efficient identification of novel structural types of ribosomal inhibitors with antimicrobial activity against drug-resistant bacteria.

Chemical Communications

Efficient discovery of novel antimicrobials through integration of synthesis and testing in crude ribosome extract†

Abstract

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Efficient discovery of novel antimicrobials through integration of synthesis and testing in crude ribosome extract

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