FASEB SRC on G protein-coupled receptor kinases: From molecules to diseases.

描述（由申请人提供）：该申请要求对“G蛋白偶联受体激酶：从分子到疾病”会议的部分支持，该会议是由美国实验生物学学会联合会（FASEB）赞助的科学研究会议（SRC）计划的一部分。G蛋白偶联受体激酶（GRK）是决定G蛋白偶联受体（GPCR）脱敏的速率和程度的关键调节蛋白，并因此影响GPCR信号传导的强度和持续时间。它们也是通过抑制蛋白以及传统的异源三聚体G蛋白介导的信号传导途径的关键调节剂。考虑到GPCR失调是许多疾病的主要原因，并且GPCR是临床使用的药物的主要靶标，GRK作为多种生理过程的重要调节剂和潜在的关键药物靶标出现，尽管目前未得到充分重视。GRK研究领域在过去10年中经历了相当大的扩展，这是由于GRK的磷酸化独立功能、GRK在非GPCR靶点的作用、GRK在正常生理和疾病过程中的作用以及药物作用的开创性发现。然而，GRK研究面临着相当大的挑战，由于不寻常的生化特性的GRK激酶和缺乏小分子选择性靶向GRK亚型。到目前为止，研究GRK依赖的细胞信号调节的研究人员已经通过出版物进行了交流，并在神经科学学会年会，内分泌学会会议，心脏协会会议等大型多焦点会议上展示了他们的研究。然而，GRK特异性主题，如GRK亚型的受体特异性，GRK通过GPCR激活的机制，GRK表达的调节，降解，亚细胞靶向，以及GRK在人类疾病和治疗中的特定功能，在这些会议上没有得到充分的代表。本次会议将汇集研究GRK生物学从分子以及生理和疾病的观点。鼓励所有演讲者在演讲中展示未发表的前沿数据，以激发讨论。会议还将允许GRK研究的世界领导人与新的研究人员进行交流。会议形式包括全体会议，由成熟的和年轻的研究人员介绍，海报会议和“会见专家”会议。会议设施和会议安排将为来自不同背景的各种经验的与会者提供充分的非正式讨论机会。总之，会议将为公开交流意见提供一个独特的论坛，这将有利于科学界，并为推动该领域的发展提供强大的动力。

DESCRIPTION (provided by applicant): The application requests partial support for the "G protein-coupled receptor kinases: From molecules to diseases" meeting organized as a part of the Science Research Conference (SRC) program sponsored by Federation by American Societies for Experimental Biology (FASEB). G protein-coupled receptor kinases (GRK) are the key regulatory proteins determining the rate and extent of desensitization of G protein-coupled receptors (GPCR) and, consequently, impacting the intensity and duration of the GPCR signaling. They are also critical regulators of signaling pathways mediated through arrestin proteins as well as traditional heterotrimeric G proteins. Considering that GPCR dysregulation is a main contributor to many diseases and that GPCRs are the prime targets of clinically used drugs, GRKs emerge as important regulators of multiple physiological processes and potentially critical, although currently underappreciated, drug targets. The filed of GRK research has undergone considerable expansion in the past 10 years fueled by seminal discoveries of phosphorylation-independent functions of GRKs, GRK action at non- GPCR targets, and GRK roles in normal physiological and disease processes as well as drug effects. However, GRK research faces considerable challenges due to the unusual biochemical properties of GRKs as kinases and the lack of small molecules selectively targeting GRK isoforms. So far, researchers studying GRK-dependent regulation of cell signaling have communicated via publications and presented their research at large multi-focused meetings such as Annual Meeting of Society for Neuroscience, Endocrine Society meeting, Heart Association meeting, etc. However, GRK-specific subjects such as receptor specificity of GRK isoforms, mechanisms of GRK activation by GPCRs, regulation of GRK expression, degradation, subcellular targeting, as well as specific functions of GRKs in human disorders and therapies, have not been not adequately represented at such meetings. This meeting will bring together researches studying GRK biology from molecular as well as physiological and disease standpoint. All speakers will be encouraged to present unpublished cutting edge data in their talk to stimulate discussion. The meeting will also allow for communication between world leaders in GRK research with new investigators. The meeting format includes plenary sessions with presentations from established and young investigators, poster sessions, and "Meet the expert" session. Facilities and the meeting arrangement will provide ample opportunities for informal discussions among participants of all levels of experience coming from diverse backgrounds. In summary, the meeting will offer a unique forum for the open exchange of ideas that will benefit the scientific community and provide a strong momentum to move the field forward.