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Biased agonism

Terry Kenakin1

  • 1Department of Biological Reagents and Assay Development, Molecular Discovery, GlaxoSmithKline Research and Development 5 Moore Drive, Research Triangle Park, NC 27709 USA. terry.p.kenakin@gsk.com

F1000 Biology Reports
|October 16, 2010
PubMed

Insights

Biased agonists reveal that seven-transmembrane receptors activate specific signaling pathways, challenging the traditional model. This discovery opens avenues for targeted therapeutic applications by selectively modulating cellular responses.

Area of Science:

  • Cellular signaling
  • Molecular pharmacology
  • Receptor biology

Background:

  • Seven-transmembrane receptors (7TMRs) traditionally activate multiple cellular pathways uniformly.
  • Emerging data indicate agonists can selectively activate specific 7TMR-linked pathways.

Purpose of the Study:

  • To discuss the concept of biased agonism in 7TMR signaling.
  • To explore the implications of biased agonism for understanding receptor activation.
  • To review potential therapeutic applications of biased agonists.

Main Methods:

  • Review of existing scientific literature and data on 7TMR signaling.
  • Analysis of agonist-biased signaling profiles.
  • Discussion of theoretical frameworks for biased agonism.

Main Results:

  • The traditional model of uniform pathway activation by agonists is insufficient.
  • Certain agonists selectively activate a subset of pathways linked to 7TMRs, termed 'biased agonists'.
  • Evidence supports the mechanism of biased agonism across various 7TMR systems.

Conclusions:

  • Biased agonism represents a significant paradigm shift in understanding 7TMR function.
  • Selective pathway activation by biased agonists offers novel therapeutic strategies.
  • Further research into biased agonism could lead to more precise drug development.

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