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Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-03-10 , DOI: 10.1021/acsmedchemlett.9b00655
Bingsong Han 1 , Francesco G Salituro 1 , Maria-Jesus Blanco 1
Affiliation  

Recent years have seen an unprecedented level of innovation in allosteric drug discovery and development, with multiple drug candidates advancing into clinical studies. From early examples of allosteric drugs like GABAA receptor modulators (benzodiazepines) in the 1960s to more recent GPCR negative allosteric modulators of CCR5 (maraviroc) approved in 2007, the opportunities for interrogating allosteric sites in drug discovery have expanded to other target classes such as protein–protein interactions, kinases, and nuclear hormone receptors. In this Innovation Letter, the authors highlight the latest advances of allosteric drug discovery from different target classes and novel emerging chemical modalities beyond small molecules.

中文翻译:

变构调节在药物发现中的影响:新兴化学模式的创新

近年来,变构药物发现和开发的创新水平达到了前所未有的水平,多种候选药物进入临床研究。从1960 年代GABA A受体调节剂(苯二氮卓类)等变构药物的早期实例到 2007 年批准的 CCR5(马拉维罗)的最新 GPCR 负变构调节剂,在药物发现中询问变构位点的机会已扩展到其他目标类别,例如蛋白质-蛋白质相互作用、激酶和核激素受体。在这封创新信函中,作者重点介绍了来自不同目标类别的变构药物发现的最新进展以及小分子以外的新型化学模式。
更新日期:2020-03-10
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