Structure-based drug design for G protein-coupled receptors.

Q1 Pharmacology, Toxicology and Pharmaceutics
Miles Congreve, João M Dias, Fiona H Marshall
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引用次数: 71

Abstract

Our understanding of the structural biology of G protein-coupled receptors has undergone a transformation over the past 5 years. New protein-ligand complexes are described almost monthly in high profile journals. Appreciation of how small molecules and natural ligands bind to their receptors has the potential to impact enormously how medicinal chemists approach this major class of receptor targets. An outline of the key topics in this field and some recent examples of structure- and fragment-based drug design are described. A table is presented with example views of each G protein-coupled receptor for which there is a published X-ray structure, including interactions with small molecule antagonists, partial and full agonists. The possible implications of these new data for drug design are discussed.

基于结构的G蛋白偶联受体药物设计。
在过去的5年中,我们对G蛋白偶联受体的结构生物学的理解发生了转变。新的蛋白质配体复合物几乎每月都会在高知名度的期刊上发表。对小分子和天然配体如何与受体结合的认识有可能极大地影响药物化学家如何处理这类主要受体靶点。概述了这一领域的关键主题,并描述了一些最近的基于结构和片段的药物设计的例子。表格给出了每个G蛋白偶联受体的示例视图,其中有已发表的x射线结构,包括与小分子拮抗剂,部分和完全激动剂的相互作用。讨论了这些新数据对药物设计的可能影响。
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来源期刊
Progress in medicinal chemistry
Progress in medicinal chemistry Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
15.60
自引率
0.00%
发文量
6
期刊介绍: This series has a long established reputation for excellent coverage of almost every facet of Medicinal Chemistry and is one of the most respected and instructive sources of information on the subject. The latest volume certifies to the continuing success of a unique series reflecting current progress in a broadly developing field of science.
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