G protein-coupled receptor modulation with pepducins: moving closer to the clinic
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G protein-coupled receptor modulation with pepducins: moving closer to the clinic. / Dimond, Patricia; Carlson, Kenneth; Bouvier, Michel ; Gerard, Craig ; Xu, Lei; Covic, Lidija; Agarwal, Anika; Ernst, Oliver P.; Janz, Jay M.; Schwartz, Thue W.; Gardella, Thomas J.; Milligan, Graeme; Kuliopulos, Athan; Sakmar, Thomas P.; Hunt III, Stephen W.
In: New York Academy of Sciences. Annals, Vol. 1226, 05.2011, p. 34-49.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - G protein-coupled receptor modulation with pepducins: 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 III, Stephen W.
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.
U2 - 10.1111/j.1749-6632.2011.06039.x
DO - 10.1111/j.1749-6632.2011.06039.x
M3 - Journal article
C2 - 21615752
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
SN - 0077-8923
ER -
ID: 34355760