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Novel Opportunities for Drug Development Through Exploration of GPCR Ligand Bias in the Brain

Join academics, researchers, and industry professionals to discuss the development of functionally selective GPCR-biased ligands in disease drug discovery.

Published September 26, 2014

NEW YORK, September 26, 2014 - On September 30, the New York Academy of Sciences will host the symposium, Elucidating GPCR Functional Selectivity: Novel Opportunities for Drug Development. With G protein-coupled receptors (GPCR) being the single largest class of therapeutic drug targets, join Nobel Laureate Robert J. Lefkowitz MD, Duke University Medical Centre, to discuss how GPCR-biased ligands can be used to help discover new drugs for cardiovascular and CNS Lyme disease.

"The realization that ligands interacting with GPCRs can stimulate or block discrete subsets of responses has opened up whole new areas of inquiry with respect to basic receptor theory, biophysics and therapeutic development.  Such ligands are known as biased agonists and have been described over the past few years for dozens of the receptors. The first such biased agonists are currently in clinical trials and have the potential to add a whole new level of specificity to GPCR drug action", says Robert J. Lefkowitz MD.

Discovering ligands with the desired signaling bias at GPCRs will yield molecules with novel activities, and could lead to significantly improved therapeutics by enabling beneficial efficacy while reducing undesirable adverse effects. This symposium examines perspectives from academic and industrial scientists, highlighting basic and translational research.

"Recent breakthroughs in our understanding of how GPCRs signal are providing an entirely new way to create drugs.  This receptor family represents a major future opportunity for drug development since these receptors are easily targeted and they control nearly all known physiological processes.  GPCR targeted drugs comprise roughly 40% of approved medications.  Fine tuning the signaling of GPCRs with small molecules by taking advantage of signaling functional selectivity holds great promise for creating a next generation of receptor targeted drugs", says John Allen PhD, Principal Scientist, Pfizer Neuroscience. Adding: "This approach may eventually benefit patients suffering from a broad spectrum of diseases including immune, psychiatric, neurological and cardiovascular diseases.  In addition, classic GPCR drugs and mechanisms such a morphine for pain, antihistamines for immune activation or beta-blockers for cardiovascular disease may be revisited using this biased signaling concept leading to improvements on these medications and mechanisms."

For a full event agenda, visit

For press inquiries, including press passes to the conference, please contact Stacy-Ann Ashley (; 212-298-8696).

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