title: Insider access: pepducin symposium explores a new approach to GPCR modulation.
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.
authors.affiliation: MacDougall Biomedical Communications, Wellesley, Massachusetts, USA.
authors.forename: Jacquelyn
authors.initials: J
authors.lastname: Miller
authors.forename: Anika
authors.initials: A
authors.lastname: Agarwal
authors.forename: Lakshmi A
authors.initials: LA
authors.lastname: Devi
authors.forename: Kellen
authors.initials: K
authors.lastname: Fontanini
authors.forename: James A
authors.initials: JA
authors.lastname: Hamilton
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Pin
authors.forename: Denis C
authors.initials: DC
authors.lastname: Shields
authors.forename: C Arnold
authors.initials: CA
authors.lastname: Spek
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Sakmar
authors.forename: Athan
authors.initials: A
authors.lastname: Kuliopulos
authors.forename: Stephen W
authors.initials: SW
authors.lastname: Hunt
mesh_terms: 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
chemical_list: D008024:Ligands; D004364:Pharmaceutical Preparations; D043562:Receptors, G-Protein-Coupled