4.4 Article

Pharmacogenetics of beta-1-beta- and 2-adrenergic receptors

Journal

PHARMACOLOGY
Volume 61, Issue 3, Pages 167-173

Publisher

KARGER
DOI: 10.1159/000028397

Keywords

beta-agonist; adenylyl cyclase; desensitization; G protein; tachyphylaxis; heart failure; asthma; polymorphism

Funding

  1. NHLBI NIH HHS [HL 45967, HL 41496] Funding Source: Medline
  2. NATIONAL HEART, LUNG, AND BLOOD INSTITUTE [R01HL045967, R37HL045967, R56HL045967, P01HL041496] Funding Source: NIH RePORTER

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beta(1)- and beta(2)-adrenergic receptors are G protein-coupled receptors expressed throughout the body and serve as receptors for the catecholamines epinephrine and norepinephrine. They are targets for therapeutive agonists and/or antagonists in treatment of heart failure and asthma. Nonsynonymous coding and promoter polymorphisms of both receptors have been identified in the general population. These have been mimicked in transfected cell systems and transgenic mice, and show altered expression, ligand binding, coupling, or regulation phenotypes, Clinical studies to date have revealed that some of these polymorphisms have a significant disease modifying effect or alter the response to treatment. These are some of the first G protein coupled receptor polymorphisms to undergo extensive in vitro study and clinical validation; there are likely to be polymorphisms of other receptors of the superfamily that will have clinical relevance as well, Copyright(C)2000S.KargerAG,Basel.

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