Drugging Challenging Cancer Targets Using Fragment-Based Methods

IF 51.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY
Stephen W. Fesik*, 
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引用次数: 0

Abstract

There are many highly validated cancer targets that are difficult or impossible to drug due to the absence of suitable pockets that can bind small molecules. Fragment-based methods have been shown to be a useful approach for identifying ligands to proteins that were previously thought to be undruggable. In this review, I will give an overview of fragment-based ligand discovery and provide examples from our own work on how fragment-based methods were used to discover high affinity ligands for challenging cancer drug targets.

利用基于片段的方法对癌症靶点进行药物挑战
由于缺乏可以结合小分子的合适口袋,许多高度验证的癌症靶点很难或不可能被药物治疗。基于片段的方法已被证明是一种有用的方法,用于识别以前认为不可药物的蛋白质配体。在这篇综述中,我将概述基于片段的配体发现,并从我们自己的工作中提供如何使用基于片段的方法来发现具有挑战性的癌症药物靶点的高亲和力配体的例子。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Chemical Reviews
Chemical Reviews 化学-化学综合
CiteScore
106.00
自引率
1.10%
发文量
278
审稿时长
4.3 months
期刊介绍: Chemical Reviews is a highly regarded and highest-ranked journal covering the general topic of chemistry. Its mission is to provide comprehensive, authoritative, critical, and readable reviews of important recent research in organic, inorganic, physical, analytical, theoretical, and biological chemistry. Since 1985, Chemical Reviews has also published periodic thematic issues that focus on a single theme or direction of emerging research.
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