G蛋白偶联受体
受体
背景(考古学)
计算生物学
功能(生物学)
视紫红质样受体
生物
药物发现
鉴定(生物学)
细胞生物学
生物信息学
生物化学
兴奋剂
代谢受体
生态学
古生物学
作者
Céline Laschet,Nadine Dupuis,Julien Hanson
标识
DOI:10.1016/j.bcp.2018.02.016
摘要
G protein-coupled receptors (GPCRs) are usually highlighted as being both the largest family of membrane proteins and the most productive source of drug targets. However, most of the GPCRs are understudied and hence cannot be used immediately for innovative therapeutic strategies. Besides, there are still around 100 orphan receptors, with no described endogenous ligand and no clearly defined function. The race to discover new ligands for these elusive receptors seems to be less intense than before. Here, we present an update of the various strategies employed to assign a function to these receptors and to discover new ligands. We focus on the recent advances in the identification of endogenous ligands with a detailed description of newly deorphanized receptors. Replication being a key parameter in these endeavors, we also discuss the latest controversies about problematic ligand-receptor pairings. In this context, we propose several recommendations in order to strengthen the reporting of new ligand-receptor pairs.
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