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First published on January 31, 2008; DOI: 10.1124/mol.108.045849

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Received for publication January 31, 2008.
Revised January 31, 2008.
Accepted for publication January 31, 2008.

Crystallizing thinking about the {beta}2-adrenergic receptor

Arun K Shukla 1, Jin-Peng Sun 1, Robert J. Lefkowitz 2*

1 Department of Medicine, Duke University Medical Center 2 Department of Medicine, Howard Hughes Medical Institute, Duke University Medical Center

* Address correspondence to: E-mail: lefko001{at}receptor-biol.duke.edu

Abstract

Two recently determined crystal structures of the human {beta}2-adrenergic receptor ({beta}2AR) provide a long awaited advance in the field of G protein coupled receptor (GPCR) research. The {beta}2AR is only the second member of this, the largest family of receptors encoded in the human genome, whose structure has been solved. It follows previously determined structures of rhodopsin. Here we set these developments in historical context, discuss the daunting challenges which have been overcome, and appraise what has and has not been learned.


Key words: Adrenergic, GRKs, barrestins, Structure determinations, X-ray crystallography




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