Centre for Cellular and Molecular Biology, Council of Scientific and Industrial Research, Uppal Road, Hyderabad 500 007, India.
Curr Med Chem. 2013;20(1):47-55.
G-protein coupled receptors (GPCRs) are the largest class of molecules involved in signal transduction across membranes, and represent major targets in the development of novel drug candidates in all clinical areas. Since GPCRs are integral membrane proteins, interaction of membrane lipids such as cholesterol and sphingolipids with GPCRs constitutes an emerging area of research in contemporary biology. Cholesterol and sphingolipids represent important lipid components of eukaryotic membranes and play a crucial role in a variety of cellular functions. In this review, we highlight the role of these vital lipids in the function of two representative GPCRs, the serotonin(1A) receptor and the adrenergic receptor. We believe that development in deciphering molecular details of the nature of GPCR-lipid interaction would lead to better insight into our overall understanding of GPCR function in health and disease.
G 蛋白偶联受体(GPCRs)是参与跨膜信号转导的最大分子类别,是所有临床领域新型候选药物开发的主要靶点。由于 GPCR 是整合膜蛋白,因此胆固醇和鞘脂等膜脂与 GPCR 的相互作用是当代生物学中一个新兴的研究领域。胆固醇和鞘脂是真核细胞膜的重要脂质成分,在多种细胞功能中发挥着关键作用。在这篇综述中,我们强调了这些重要脂质在两种代表性 GPCR(5-羟色胺(1A)受体和肾上腺素能受体)功能中的作用。我们相信,在阐明 GPCR-脂质相互作用的本质方面取得的进展将有助于更好地理解 GPCR 在健康和疾病中的功能。