BIOS group, INRA, UMR85, Unité physiologie de la reproduction et des comportements, 37380 Nouzilly, France.
C R Biol. 2009 Nov;332(11):947-57. doi: 10.1016/j.crvi.2009.09.002. Epub 2009 Oct 14.
G protein-coupled receptors (GPCRs) control all the main physiological functions and are targeted by more than 50% of therapeutics. Our perception of GPCRs signalling has grown increasingly complex since it is now accepted that they activate large signalling networks which are integrating the information fluxes into appropriate biological responses. These concepts lead the way to the development of pathway-selective agonists (or antagonists) with fewer side effects. Systems biology approaches focused on GPCR-mediated signalling would help dealing with the huge complexity of these mechanisms therefore speeding-up the discovery of new drug classes. In this review, we present the various technical and conceptual possibilities allowing a systems approach of GPCR-mediated signalling. The main remaining limitations are also discussed.
G 蛋白偶联受体 (GPCRs) 控制着所有主要的生理功能，并且是超过 50%的治疗药物的靶点。自从人们接受 GPCR 可以激活大型信号网络，这些信号网络将信息流整合为适当的生物反应以来，我们对 GPCR 信号转导的认识变得越来越复杂。这些概念为开发具有更少副作用的途径选择性激动剂（或拮抗剂）铺平了道路。专注于 GPCR 介导的信号转导的系统生物学方法将有助于处理这些机制的巨大复杂性，从而加快新药物类别的发现。在这篇综述中，我们介绍了允许对 GPCR 介导的信号转导进行系统研究的各种技术和概念可能性。还讨论了主要的剩余限制。
