GPCRs: Evolving Concepts and Drug Discovery

描述（由申请人提供）： G蛋白偶联受体（GPCR），其包括在人类基因组中鉴定的最大基因家族之一，也代表了目前使用的治疗药物的最大数量的靶标。最近的工作表明了一些有趣的观察在GPCR的结构，功能和调节，包括受体同源二聚体和异源二聚体的存在，孤儿GPCR的遗传鉴定，新的受体相互作用蛋白，临床上重要的多态性和受体突变，参与受体失活/脱敏的机制，和受体靶向/行动的信号微域。有关这些主题的详细资料仍在编制中。本次研讨会将重点讨论这些和相关的主题，重点是使用新的工具，例如，评估GPCR家族成员的生物信息学方法，鉴定GPCR活性配体的新策略，以及来自非哺乳动物/低等真核系统的见解。因此，与会者将有机会学习和讨论有关GPCR的新前沿话题。

DESCRIPTION (provided by applicant): G-protein-coupled receptors (GPCRs), which comprise one of the largest gene families identified in the human genome, also represent the largest number of currently used targets of therapeutic drugs. Recent work has indicated a number of intriguing observations in terms of GPCR structure, function and regulation, including existence of receptor homodimers and heterodimers, genetic identification of orphan GPCRs, novel receptor interacting proteins, clinically important polymorphisms and receptor mutations, mechanisms involved in receptor deactivation/desensitization, and receptor targeting/action in signaling microdomains. Definitive information about each of these topics is still being developed. This symposium will focus on these and related topics with an emphasis on use of new tools, e.g., bioinformatic approaches to evaluate GPCR family members, novel strategies to identify ligands active at GPCRs, and insights from nonmammalian/lower eukaryotic systems. Attendees will thus have the chance to learn and discuss new cutting edge topics regarding GPCRs.