Uncovering GPCR heteromer-biased ligands

Sanam Mustafa, Mohammed Akli Ayoub, Kevin D.G. Pfleger

Research output: Contribution to journalReview articlepeer-review

17 Citations (Scopus)


The formation of complexes involving different G-protein-coupled receptors (GPCRs) is now an established phenomenon, termed heteromerization. The relevance of higher order structures, in particular heteromerization, has been demonstrated by differential pharmacology displayed by GPCR heteromers compared to monomers/homomers of the respective constituent receptor units. The concepts of heteromerization and heteromer-selective/biased ligands introduce exciting opportunities for enhancing signal specificity and therefore have the potential to play a crucial role in future drug discovery.

Original languageEnglish
Pages (from-to)e77-e85
JournalDrug Discovery Today: Technologies
Issue number1
Publication statusPublished - 2010
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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