摘要
CCK受体属于G蛋白偶联受体。CCK受体多态性可改变药物的亲和力与(或)生物学效应,其氨基酸序列的改变可能诱导非配基依赖性信号转导,从而引起疾病。随着遗传药理学的发展,多态性引起的药物与(或)受体功能的改变在新药开发中将日益受到关注。研究CCK受体的多态性可能反映G蛋白偶联受体家族的一些普遍规律。该文从分子生物学和遗传药理学角度综述了CCK受体多态性对受体功能与(或)药物效能的影响,并提出开发受体相关性药物的一些策略。
CCK receptor belongs to G-protein-coupled receptor (GPCR) superfamily. Polymorphism of CCK receptors can alter drug affinity and/or biological efficacy, and its genetic differences in amino acid sequences can induce ligand-independent signaling, which in turn can lead to disease. With growing efforts in the field of pharmacogenomics, it is anticipated that polymorphism-induced alterations in drug and/or receptor function will be a focus of increasing concern in the future drug-development project. Study of CCK receptor polymorphism may reveal some universal rules in GPCR superfamily. In this review, the alterations of receptor function and/or drug efficacy resulted from polymorphism in CCK receptors will be discussed in the viewpoint of molecular biology and pharmacogenomics, and some strategies in development of receptor-specific drugs will be put forward.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2005年第8期914-917,共4页
Chinese Pharmacological Bulletin
基金
国家自然科学基金资助课题(No3027059)
河北省自然科学基金资助课题(No303452)
关键词
受体
胆囊收缩素
多态性
药物设计
receptor
cholecystokinin
polymorphism
drug design