Structural insights into adrenergic receptor function and pharmacology

Brian K. Kobilka

Research output: Contribution to journalReview ArticleResearchpeer-review

128 Citations (Scopus)

Abstract

It has been over 50 years since Sir James Black developed the first beta adrenergic receptor (βAR) 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 βARs 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.

Original languageEnglish
Pages (from-to)213-218
Number of pages6
JournalTrends in Pharmacological Sciences
Volume32
Issue number4
DOIs
Publication statusPublished - Apr 2011
Externally publishedYes

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