Turning off the signal: desensitization of beta-adrenergic receptor function.

Published

Journal Article (Review)

Cellular responses to many hormones and neurotransmitters wane rapidly despite continuous exposure of cells to these stimuli. This phenomenon, termed desensitization, has been particularly well studied for the stimulation of cAMP levels by plasma membrane beta-adrenergic receptors (beta AR). The molecular mechanisms underlying rapid beta AR desensitization do not appear to require internalization of the receptors, but rather an alteration in the functioning of beta AR themselves that uncouples the receptors from the stimulatory G protein Gs. This uncoupling phenomenon involves phosphorylation of beta AR by at least two kinases, PKA and the beta AR kinase (beta ARK), which are activated under different desensitizing conditions. Receptor phosphorylation by the two kinases leads to desensitization of the receptor response via distinct biochemical mechanisms, and additional cytosolic factors appear to be involved in the case of beta ARK. Numerous experimental approaches have been used recently to elucidate the molecular details of this ubiquitous biological process.

Full Text

Duke Authors

Cited Authors

  • Hausdorff, WP; Caron, MG; Lefkowitz, RJ

Published Date

  • August 1990

Published In

Volume / Issue

  • 4 / 11

Start / End Page

  • 2881 - 2889

PubMed ID

  • 2165947

Pubmed Central ID

  • 2165947

Electronic International Standard Serial Number (EISSN)

  • 1530-6860

International Standard Serial Number (ISSN)

  • 0892-6638

Digital Object Identifier (DOI)

  • 10.1096/fasebj.4.11.2165947

Language

  • eng