Therapeutic potential of functional selectivity in the treatment of heart failure

Gitte Lund Christensen, Mark Aplin, Jakob Lerche Hansen

4 Citations (Scopus)

Abstract

Adrenergic and angiotensin receptors are prominent targets in pharmacological alleviation of cardiac remodeling and heart failure, but their use is associated with cardiodepressant side effects. Recent advances in our understanding of seven transmembrane receptor signaling show that it is possible to design ligands with "functional selectivity," acting as agonists on certain signaling pathways while antagonizing others. This represents a major pharmaceutical opportunity to separate desired from adverse effects governed by the same receptor. Accordingly, functionally selective ligands are currently pursued as next-generation drugs for superior treatment of heart failure.
Original languageEnglish
JournalTrends in Cardiovascular Medicine
Volume20
Issue number7
Pages (from-to)221-7
Number of pages7
ISSN1050-1738
DOIs
Publication statusPublished - Oct 2010

Keywords

  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Angiotensin II Type 1 Receptor Blockers
  • Animals
  • Heart Failure
  • Humans
  • Ligands
  • Mice
  • Mice, Transgenic
  • Receptor, Angiotensin, Type 1
  • Receptors, Adrenergic, beta
  • Signal Transduction

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