Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 32, Issue 4, Pages 213-218Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2011.02.005
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Funding
- NIGMS NIH HHS [R01 GM083118, R01 GM083118-03] Funding Source: Medline
- NINDS NIH HHS [R37 NS028471, R37 NS028471-20] Funding Source: Medline
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It has been over 50 years since Sir James Black developed the first beta adrenergic receptor (BAR) blocker to treat heart disease. At that time, the concept of cell surface receptors was relatively new and not widely accepted, and most of the tools currently used to characterize plasma membrane receptors had not been developed. There has been remarkable progress in receptor biology since then, including the development of radioligand binding assays, the biochemical characterization of receptors as discrete membrane proteins, and the cloning of the first G-protein-coupled receptors (GPCRs), which led to the identification of other members of the large family of GPCRs. More recently, progress in GPCR structural biology has led to insights into the three-dimensional structures of beta ARs in both active and inactive states. Despite all of this progress, the process of developing a drug for a particular GPCR target has become more complex, time-consuming and expensive.
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