Pepducin symposium explores a new approach to GPCR modulation

Edited by Jacquelyn Miller (MacDougall Biomedical Communications, Wellesley, Massachusetts), Anika Agarwal and Athan Kuliopulos (Tufts Medical Center, Boston, Massachusetts), Lakshmi A. Devi (Mount Sinai School of Medicine, New York, New York), Kellen Fontanini and James A. Hamilton (Boston University School of Medicine, Boston, Massachusetts), Jean-Philippe Pin (University of Montpellier, Montpellier, France), Denis C. Shields (The University College of Dublin, Dublin, Ireland), C. Arnold Spek (University of Amsterdam, Amsterdam, the Netherlands), Thomas P. Sakmar (The Rockefeller University, New York, New York), and Stephen W. Hunt III (Ascent Therapeutics, Cambridge, Massachusetts).
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Pepducin symposium explores a new approach to GPCR modulation

Published: November 2009

Volume 1180

This special Annals meeting report covers new work in the field of pepducins: lipopeptides that modulate heptahelical G-protein coupled receptor activity from inside the cell membrane.
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G protein–coupled receptors (GPCRs) are, arguably, one of the most important molecular targets in drug discovery and pharmaceutical development today. This superfamily of membrane receptors is central to nearly every signaling pathway in the human body and has been the focus of intense research for decades. However, as scientists discover additional properties of GPCRs, it has become clear that much is yet to be understood about how these receptors function. Everyone agrees, however, that tremendous potential remains if specific GPCR signaling pathways can be modulated to correct pathological states. One exciting new approach to this challenge involves pepducins: novel, synthetic lipopeptide pharmacophores that modulate heptahelical GPCR activity from inside the cell membrane.

The special online report below highlights the inaugural Pepducin Science Symposium, held in Cambridge, Massachusetts, March 8-9, 2009. Approximately 30 invited guests from the scientific community attended the program. The symposium offered expert presentations and a poster session featuring current topics related to pepducins, a novel approach to G protein-coupled receptors (GPCR)-targeted therapeutic research and development. This twelve page summary presents an overview of the research presented at the symposium.

As part of its commitment to facilitating research and discussion to advance new therapeutic options for patients, Ascent Therapeutics is pleased to support the Annals of the New York Academy of Sciences by providing to this summary of the Pepducin Science Symposium.

Topics discussed include research on

  • novel models of dynamic GPCR activation and allosteric regulation
  • evidence that morphine-dependence may be mitigated through targeting of heterodimer GPCR complexes in the brain
  • computational screening for novel GPCR ligands
  • inhibition of neutrophil activation through pepducin antagonism in sepsis models
  • targeting signal pathways in ovarian cancer using pepducin lipopeptides