BioInsight Communications, Eastham, Massachusetts, USA.
Ann N Y Acad Sci. 2011 May;1226:34-49. doi: 10.1111/j.1749-6632.2011.06039.x.
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.
在 2010 年 11 月 4 日至 5 日于马萨诸塞州剑桥市举行的第二届 Pepducin 科学研讨会（2nd Pepducin Science Symposium）上，从事 G 蛋白偶联受体（G protein-coupled receptor，GPCR）研究的研究人员齐聚一堂，讨论自去年首届会议以来的进展情况。今年的研讨会重点关注增加对这种普遍存在的膜受体超家族的结构和功能的了解，以及它们在疾病治疗中的潜在调节作用。演讲还重点介绍了如何利用 GPCR 机制来治疗 pepducin 治疗的疾病， pepducin 是一种新型的合成脂肽类药，可调节七螺旋 GPCR 活性。虽然 GPCR 在生理和病理生理过程中的多种作用为新型药物开发提供了重大机会，但它们的全球性活动挑战了特定药物和验证目标的识别。今年的会议强调了对 GPCR 激动剂和拮抗剂配体结合基序、它们的配体非依赖性功能、结构-活性关系（SAR）以及不断发展的独特方法的理解方面的进展，这些方法用于研究 GPCR 的结构和功能。会议总结的研究结果还为如何通过这些受体发挥信号转导机制的观点提供了证据。
