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Targeting G protein-coupled receptors for heart failure treatment

Bui San Thai1, Ling Yeong Chia1, Anh T N Nguyen1

  • 1Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.

British Journal of Pharmacology
|April 24, 2023
PubMed

Insights

Despite current treatments, many heart failure patients experience persistent symptoms. Exploring new G protein-coupled receptor (GPCR) targets offers potential for novel heart failure therapeutics to improve patient outcomes.

Area of Science:

  • Pharmacology
  • Cardiovascular Medicine
  • Drug Discovery

Background:

  • Heart failure is a major global health burden with significant morbidity and mortality.
  • Current treatments targeting G protein-coupled receptors (GPCRs), such as beta-blockers, are insufficient for many patients.
  • Persistent symptoms and disease progression occur despite existing therapies that reduce mortality.

Purpose of the Study:

  • To review current challenges in developing novel heart failure therapeutics targeting GPCRs.
  • To identify emerging GPCR targets for potential heart failure treatments.
  • To discuss strategies for overcoming limitations in clinical translation of GPCR-based therapies.

Main Methods:

  • Literature review of current and emerging GPCR targets for heart failure.
  • Analysis of challenges in clinical translation of GPCR drug candidates.
  • Discussion of potential solutions to improve therapeutic efficacy and safety.

Main Results:

  • Several novel GPCR targets are under investigation, including adenosine, formyl peptide, relaxin/insulin-like family peptide, vasopressin, endothelin, and glucagon-like peptide 1 receptors.
  • Many drug candidates face limitations due to insufficient efficacy and dose-limiting side effects.
  • Understanding translational challenges is crucial for future drug development.

Conclusions:

  • Novel GPCR targets hold promise for developing more effective heart failure treatments.
  • Overcoming efficacy and safety limitations is key to successful clinical translation.
  • Further research into GPCR-mediated pathways is essential for advancing heart failure therapy.

Keywords:
G protein‐coupled receptordrug discoveryheart failuremyocardial infarction

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