Insider access: pepducin symposium explores a new approach to GPCR modulation.
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.
Miller
Jacquelyn
J
MacDougall Biomedical Communications, Wellesley, Massachusetts, USA.
Agarwal
Anika
A
Devi
Lakshmi A
LA
Fontanini
Kellen
K
Hamilton
James A
JA
Pin
Jean-Philippe
JP
Shields
Denis C
DC
Spek
C Arnold
CA
Sakmar
Thomas P
TP
Kuliopulos
Athan
A
Hunt
Stephen W
SW
D000494:Allosteric Regulation / Q000187:drug effects / Q000502:physiology; D000818:Animals; D019295:Computational Biology; D016503:Drug Delivery Systems / Q000379:methods*; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D008024:Ligands; D008954:Models, Biological; D008958:Models, Molecular; D009021:Morphine Dependence / Q000209:etiology / Q000378:metabolism; D010051:Ovarian Neoplasms / Q000188:drug therapy; D004364:Pharmaceutical Preparations / Q000302:isolation & purification; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D018805:Sepsis / Q000188:drug therapy; D009435:Synaptic Transmission / Q000187:drug effects
D008024:Ligands; D004364:Pharmaceutical Preparations; D043562:Receptors, G-Protein-Coupled