GPCR biased ligands as novel heart failure therapeutics

Jonathan D. Violin, David G. Soergel, Guido Boerrigter, John C. Burnett, Michael W. Lark

Research output: Contribution to journalReview articlepeer-review

31 Scopus citations


G protein-coupled receptors have been successfully targeted by numerous therapeutics including drugs that have transformed the management of cardiovascular disease. However, many GPCRs, when activated or blocked by drugs, elicit both beneficial and adverse pharmacology. Recent work has demonstrated that in some cases, the salutary and deleterious signals linked to a specific GPCR can be selectively targeted by "biased ligands" that entrain subsets of a receptor's normal pharmacology. This review briefly summarizes the advances and current state of the biased ligand field, focusing on an example: biased ligands targeting the angiotensin II type 1 receptor. These compounds exhibit unique pharmacology, distinct from classic agonists or antagonists, and one such molecule is now in clinical development for the treatment of acute heart failure.

Original languageEnglish (US)
Pages (from-to)242-249
Number of pages8
JournalTrends in cardiovascular medicine
Issue number7
StatePublished - Oct 2013

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine


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