New perspectives regarding β(2) -adrenoceptor ligands in the treatment of asthma.


Journal Article (Review)

In the last two decades several significant changes have been proposed in the receptor theory that describes how ligands can interact with G protein-coupled receptors (GPCRs). Here we briefly summarize the evolution of receptor theory and detail recent prominent advances. These include: (i) the existence of spontaneously active GPCRs that are capable of signalling even though they are unoccupied by any ligand; (ii) the discovery of ligands that can inactivate these spontaneously active receptors; (iii) the notion that a ligand may simultaneously activate more than one GPCR signalling pathway; and (iv) the notion that certain ligands may be able to preferentially direct receptor signalling to a specific pathway. Because the data supporting these receptor theory ideas are derived primarily from studies using artificial expression systems, the physiological relevance of these new paradigms remains in question. As a potential example of how these new perspectives in receptor theory relate to drug actions and clinical outcomes, we discuss their relevance to the recent controversy regarding the chronic use of β(2) -adrenoceptor agonists in the treatment of asthma.

Full Text

Duke Authors

Cited Authors

  • Walker, JKL; Penn, RB; Hanania, NA; Dickey, BF; Bond, RA

Published Date

  • May 2011

Published In

Volume / Issue

  • 163 / 1

Start / End Page

  • 18 - 28

PubMed ID

  • 21175591

Pubmed Central ID

  • 21175591

Electronic International Standard Serial Number (EISSN)

  • 1476-5381

International Standard Serial Number (ISSN)

  • 0007-1188

Digital Object Identifier (DOI)

  • 10.1111/j.1476-5381.2010.01178.x


  • eng