Kopin A S, McBride E W, Schaffer K, Beinborn M
Department of Medicine and the GRASP Digestive Disease Center, Tupper Research Institute, New England Medical Center, 750 Washington Street, Boston, MA 02111, USA.
Trends Pharmacol Sci. 2000 Sep;21(9):346-53. doi: 10.1016/s0165-6147(00)01526-1.
Polymorphisms in G-protein-coupled receptors can alter drug affinity and/or activity. In addition, 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 during the course of future drug-development efforts. In this review, the spectrum of pharmacological consequences that result from polymorphisms in the cholecystokinin CCK2 receptor will be discussed, thereby illustrating emerging themes in pharmacogenomics.
G蛋白偶联受体中的多态性可改变药物亲和力和/或活性。此外,氨基酸序列的遗传差异可诱导非配体依赖性信号传导,进而导致疾病。随着药物基因组学领域的不断努力,预计多态性引起的药物和/或受体功能改变将成为未来药物开发过程中越来越受关注的焦点。在本综述中,将讨论胆囊收缩素CCK2受体多态性所导致的一系列药理学后果,从而阐明药物基因组学中出现的新主题。