G蛋白偶联受体(G-protein-coupled receptors,GPCRs)是与G蛋白相连接的最大膜受体家族,能够被不同的配体所激活,如激素、多肽等。GPCRs与配体结合后能激活细胞内的G蛋白,通过不同的信号转导通路产生不同的生物学效应。人类基因组中含有1 000多个GPCRs基因,占整个人类基因组的3%左右。GPCRs是药物研发中最广泛应用的药靶,作用于GPCRs的药物对疼痛、高血压和哮喘等各类疾病具有良好的治疗作用。
G-protein-coupled receptor kinases(GRKs) are a family of serine/threonine protein kinases.The investigators pay much attention to the roles of GRKs in the signal transduction through G-protein-coupled receptors(GPCRs) with arrestin ever since a long time ago.Due to the physiological and pathological observations with the methods of deletion or overexpression,GRKs are considered as new drug targets.The kinases play a role in the pathogenesis of hypertension and cell migration through GPCRs and Hedgehog signaling pathways.As the development of research techniques,especially bioluminescence resonance energy transfer(BRET) and fluorescence resonance energy transfer(FRET),the special mechanism of GRKs for GPCRs is more evident.In this review,we discuss the recent achievement in the roles of GRKs signaling and the related newest research techniques.