功能选择性
逮捕
G蛋白偶联受体
受体
信号转导
痛苦
兴奋剂
跨膜结构域
G蛋白
跨膜蛋白
视紫红质样受体
细胞生物学
生物
化学
生物化学
代谢受体
政治
政治学
法学
作者
Éric Reiter,Seungkirl Ahn,Arun K. Shukla,R.J. Lefkowitz
出处
期刊:Annual Review of Pharmacology and Toxicology
[Annual Reviews]
日期:2012-02-10
卷期号:52 (1): 179-197
被引量:534
标识
DOI:10.1146/annurev.pharmtox.010909.105800
摘要
The concept of biased agonism has recently come to the fore with the realization that seven-transmembrane receptors (7TMRs, also known as G protein–coupled receptors, or GPCRs) activate complex signaling networks and can adopt multiple active conformations upon agonist binding. As a consequence, the “efficacy” of receptors, which was classically considered linear, is now recognized as pluridimensional. Biased agonists selectively stabilize only a subset of receptor conformations induced by the natural “unbiased” ligand, thus preferentially activating certain signaling mechanisms. Such agonists thus reveal the intriguing possibility that one can direct cellular signaling with unprecedented precision and specificity and support the notion that biased agonists may identify new classes of therapeutic agents that have fewer side effects. This review focuses on one particular class of biased ligands that has the ability to alter the balance between G protein–dependent and β-arrestin-dependent signal transduction.
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