FASEB SRC on G Protein-Coupled Receptor Kinases and Arrestins: From Structure to Disease

摘要 G蛋白偶联受体(GPCRs)及其下游信号通路对 调节许多基本的细胞过程，是一些最常用的处方的靶点 药物，如用于治疗疼痛、心力衰竭和高血压的药物(如吗啡、阻滞剂和 分别为血管紧张素抑制剂)。GPCRK(GRKs)和阻滞素共同调节GPCRs 通过降低受体与G蛋白偶联的能力和通过靶向活性的GPCRs来传递信号 内吞作用。尽管这些脱敏机制对于细胞恢复到生理状态很重要 休息状态、GRK和阻滞剂也被认为在成瘾和心血管疾病中起着重要作用 疾病，至少部分是通过激发其他非规范的信号级联反应。这项提案寻求资金用于 一个论坛，将汇聚研究GRK和ARRESING不同方面的世界领先的研究人员 生物学及其在G蛋白偶联受体激酶和阻滞素疾病中的作用：从结构到 会议的两大亮点将是2012年诺贝尔奖获得者的主旨演讲，他们是 GPCR、GRK和arrestin结构、功能和细胞生物学方面的专家。预计这次会议不仅将 促进新的假设、协作和方法论的产生，这些假设、协作和方法可用于研究 打击药物滥用和心血管疾病，但也提供职业发展和演讲 初级调查人员和代表性不足的科学家群体的机会。

Summary G protein-coupled receptors (GPCRs) and their downstream signaling pathways are important for the regulation of many essential cellular processes and are targets of some of the most commonly prescribed drugs, such as those used to treat pain, heart failure, and high blood pressure (e.g. morphine,  blockers, and angiotensin inhibitors, respectively). GPCR kinases (GRKs) and arrestins work together to regulate GPCR signaling by reducing the ability of receptors to couple with G proteins and by targeting active GPCRs for endocytosis. Although these desensitization mechanisms are important for returning cells to their physiological resting states, GRKs and arrestins are also thought to play prominent roles in addiction and cardiovascular disease, at least in part by instigating other, non-canonical signaling cascades. This proposal seeks funding for a forum that would bring together world-leading researchers who study different aspects of GRK and arrestin biology and their roles in disease called "G Protein-Coupled Receptor Kinases and Arrestins: From Structure to Disease". Two major highlights of the meeting will be keynote lectures by 2012 Nobel laureates who are experts in GPCR, GRK, and arrestin structure, function, and cell biology. The meeting is expected to not only stimulate the generation of new hypotheses, collaborations, and methodologies that can be used to study and combat drug abuse and cardiovascular disease, but also provide career advancement and speaking opportunities for junior investigators and underrepresented groups of scientists.