受体
计算生物学
药品
药物发现
结构生物学
小分子
G蛋白偶联受体
配体(生物化学)
生物
药理学
化学
生物信息学
生物化学
作者
Miles Congreve,João M. Dias,Fiona H. Marshall
出处
期刊:Progress in Medicinal Chemistry
日期:2014-01-01
卷期号:: 1-63
被引量:62
标识
DOI:10.1016/b978-0-444-63380-4.00001-9
摘要
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.
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