Seven transmembrane receptors: something old, something new.

Journal Article (Journal Article;Review)

Receptors for hormones, neurotransmitters, drugs, sensory stimuli and many other agents represent the gateway to cellular metabolism and activity. They regulate virtually all physiological processes in mammals. Yet as recently as 40 years ago their very existence was still in question. One class of receptors, those coupled to G proteins (also known as GPCRs or seven transmembrane receptors) comprise by far the largest group (approx. 1000), and are the most important target of clinically used drugs. Here I provide a very personal retrospective of research over the past 35 years which ultimately led to the identification, purification, reconstitution and cloning of the adrenergic receptors; the discovery of their homology with the seven transmembrane spanning visual light receptor rhodopsin and the realization that there was a large gene family of G protein coupled receptors; the elucidation of the molecular mechanisms of receptor desensitization and signalling through G protein-coupled receptor kinases and beta-arrestins; and the appreciation that the structure, signalling, and regulatory mechanisms of the receptors are all highly conserved across the large receptor superfamily.

Full Text

Duke Authors

Cited Authors

  • Lefkowitz, RJ

Published Date

  • May 2007

Published In

Volume / Issue

  • 190 / 1

Start / End Page

  • 9 - 19

PubMed ID

  • 17428228

International Standard Serial Number (ISSN)

  • 1748-1708

Digital Object Identifier (DOI)

  • 10.1111/j.1365-201X.2007.01693.x


  • eng

Conference Location

  • England