可药性
药物发现
背景(考古学)
化学生物学
蛋白质降解
纳米技术
化学
小分子
化学空间
生物
计算生物学
生物化学
材料科学
基因
古生物学
作者
Laura M. Luh,U. Scheib,Katrin Juenemann,Lars Wortmann,Michael Brands,Philipp M. Cromm
标识
DOI:10.1002/anie.202004310
摘要
Abstract Targeted protein degradation (TPD), the ability to control a proteins fate by triggering its degradation in a highly selective and effective manner, has created tremendous excitement in chemical biology and drug discovery within the past decades. The TPD field is spearheaded by small molecule induced protein degradation with molecular glues and proteolysis targeting chimeras (PROTACs) paving the way to expand the druggable space and to create a new paradigm in drug discovery. However, besides the therapeutic angle of TPD a plethora of novel techniques to modulate and control protein levels have been developed. This enables chemical biologists to better understand protein function and to discover and verify new therapeutic targets. This Review gives a comprehensive overview of chemical biology techniques inducing TPD. It explains the strengths and weaknesses of these methods in the context of drug discovery and discusses their future potential from a medicinal chemist's perspective.
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