G protein-coupled receptor modulation with pepducins: moving closer to the clinic

TY - JOUR

T1 - G protein-coupled receptor modulation with pepducins

T2 - moving closer to the clinic

AU - Dimond, Patricia

AU - Carlson, Kenneth

AU - Bouvier, Michel

AU - Gerard, Craig

AU - Xu, Lei

AU - Covic, Lidija

AU - Agarwal, Anika

AU - Ernst, Oliver P

AU - Janz, Jay M

AU - Schwartz, Thue W.

AU - Gardella, Thomas J

AU - Milligan, Graeme

AU - Kuliopulos, Athan

AU - Sakmar, Thomas P

AU - Hunt, Stephen W

N1 - © 2011 New York Academy of Sciences.

PY - 2011/5

Y1 - 2011/5

N2 - At the 2nd Pepducin Science Symposium held in Cambridge, Massachusetts, on November 4-5, 2010, investigators working in G protein-coupled receptor (GPCR) research convened to discuss progress since last year's inaugural conference. This year's symposium focused on increasing knowledge of the structure and function of this ubiquitous superfamily of membrane receptors and their potential modulation for disease treatment. Presentations also focused on how GPCR mechanisms might be exploited to treat diseases with pepducins, novel synthetic lipopeptide pharmacophores that modulate heptahelical GPCR activity. While the multiple roles of GPCRs in physiological and pathophysiological processes offer significant opportunities for novel drug development, the global nature of their activity challenges drug-specific and validated target identification. This year's conference highlighted advances in understanding of GPCR agonist and antagonist ligand-binding motifs, their ligand-independent functions, structure-activity relationships (SARs), and evolving unique methods to probe GPCR structure and function. Study results summarized at the meeting also provided evidence for evolving views of how signaling mechanisms work through these receptors.

AB - At the 2nd Pepducin Science Symposium held in Cambridge, Massachusetts, on November 4-5, 2010, investigators working in G protein-coupled receptor (GPCR) research convened to discuss progress since last year's inaugural conference. This year's symposium focused on increasing knowledge of the structure and function of this ubiquitous superfamily of membrane receptors and their potential modulation for disease treatment. Presentations also focused on how GPCR mechanisms might be exploited to treat diseases with pepducins, novel synthetic lipopeptide pharmacophores that modulate heptahelical GPCR activity. While the multiple roles of GPCRs in physiological and pathophysiological processes offer significant opportunities for novel drug development, the global nature of their activity challenges drug-specific and validated target identification. This year's conference highlighted advances in understanding of GPCR agonist and antagonist ligand-binding motifs, their ligand-independent functions, structure-activity relationships (SARs), and evolving unique methods to probe GPCR structure and function. Study results summarized at the meeting also provided evidence for evolving views of how signaling mechanisms work through these receptors.

KW - Congresses as Topic

KW - Drug Design

KW - Humans

KW - Lipopeptides

KW - Neoplasms

KW - Receptors, G-Protein-Coupled

KW - Signal Transduction

KW - Structure-Activity Relationship

U2 - 10.1111/j.1749-6632.2011.06039.x

DO - 10.1111/j.1749-6632.2011.06039.x

M3 - Journal article

C2 - 21615752

SN - 0077-8923

VL - 1226

SP - 34

EP - 49

JO - Annals of The Lyceum of Natural History of New York

JF - Annals of The Lyceum of Natural History of New York

ER -