摘要
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.
出处
《中国病理生理杂志》
CAS
CSCD
北大核心
2011年第7期1438-1444,共7页
Chinese Journal of Pathophysiology
基金
国家自然科学基金资助项目(No.30971081
No.30870932
No.81070961)
山东省自然科学基金资助项目(No.Y2007D01
No.ZR2009DZ004)
关键词
G蛋白偶联受体激酶类
受体
G蛋白偶联
信号转导
G-protein-coupled receptors kinases
Receptors
G-protein-coupled
Signal transduction
