Insider access: pepducin symposium explores a new approach to GPCR modulation.

Annals of the New York Academy of Sciences
Jacquelyn MillerStephen W Hunt

Abstract

The inaugural Pepducin Science Symposium convened in Cambridge, Massachusetts on March 8-9, 2009 provided the opportunity for an international group of distinguished scientists to present and discuss research regarding G protein-coupled receptor-related research. 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.

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Citations

Feb 9, 2011·The Journal of Cell Biology·Rinshi S KasaiAkihiro Kusumi
Jun 22, 2012·Expert Opinion on Drug Discovery·Linjie ChenNaiming Zhou
Feb 1, 2011·Pharmacology & Therapeutics·Mark N AdamsJohn D Hooper
May 28, 2011·Annals of the New York Academy of Sciences·Patricia DimondStephen W Hunt
Jun 17, 2015·Journal of Molecular Graphics & Modelling·Jesús M PlanesasJordi Teixidó
Jan 19, 2016·The Journal of Black Psychology·Germine H AwadCollette Chapman-Hilliard
Nov 29, 2014·Bulletin of Experimental Biology and Medicine·K V DerkachA O Shpakov
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Aug 2, 2018·International Journal of Molecular Sciences·Lidija Covic, Athan Kuliopulos
Apr 17, 2020·ACS Pharmacology & Translational Science·Claes DahlgrenHuamei Forsman

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