基于化学蛋白质组学的药物靶标鉴定

Drug target deconvolution by chemical proteomics

通过药物靶标鉴定,可以建立药物活性与细胞表型之间的联系,阐明药物的作用机理,还可以发现药物的脱靶效应和耐药性机制,发现治疗药物的新靶点,并在药物开发的早期阶段预测可能存在的毒性,降低药物研发失败的风险。目前虽然科学技术取得了飞速发展,但是鉴定药物靶标依然是一件令人生畏的工作。本文对近10年来药物靶标鉴定方面的研究进展,特别是无化学标记的新技术进行了评述。

Drug target identification can help establish the association between drug activity and phenotypes,elucidate the mechanism of action,discover off-target effects and drug resistance mechanisms,discover new targets for therapeutic drugs,and predict possible side effects and toxicity at an early stage of drug discovery,thereby reducing the risk of failure in drug development.Although rapid progress has been made in scientific discoveries and technological advancements,the identification of drug targets is still a daunting task.Herein,the research progress in drug target identification during the past decade,especially novel technologies without chemical labeling,have been reviewed.