Miller Jacquelyn, Agarwal Anika, Devi Lakshmi A, Fontanini Kellen, Hamilton James A, Pin Jean-Philippe, Shields Denis C, Spek C Arnold, Sakmar Thomas P, Kuliopulos Athan, Hunt Stephen W
MacDougall Biomedical Communications, Wellesley, Massachusetts, USA.
Ann N Y Acad Sci. 2009 Nov;1180 Suppl 1:E1-12. doi: 10.1111/j.1749-6632.2009.05326.x.
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.
首届肽导向激动剂科学研讨会于2009年3月8日至9日在马萨诸塞州剑桥市召开，为国际知名科学家群体提供了一个展示和讨论G蛋白偶联受体相关研究的机会。G蛋白偶联受体（GPCRs）可以说是当今药物发现和制药开发中最重要的分子靶点之一。这个膜受体超家族几乎是人体每个信号通路的核心，并且几十年来一直是深入研究的焦点。然而，随着科学家们发现GPCRs的更多特性，很明显对于这些受体如何发挥功能仍有许多有待了解之处。不过，大家都认同，如果能够调节特定的GPCR信号通路以纠正病理状态，仍存在巨大的潜力。应对这一挑战的一种令人兴奋的新方法涉及肽导向激动剂：新型合成脂肽药效基团，可从细胞膜内部调节七螺旋GPCR活性。
