Modulators of Secreted ER Ca2+ Monitoring Protein (SERCaMP)

分泌型 ER Ca2 监测蛋白 (SERCaMP) 调节剂

• 批准号: 10691117
• 负责人: Anton Simeonov
• 金额: $ 42.54万
• 依托单位: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10691117
• 关键词: Alkynes; Biotin; Bromocriptine; Calcium; Development; Diabetes Mellitus; Diazomethane; Disease; Functional disorder; Future; Homeostasis; Link; Monitor; Parkinson Disease; Pharmaceutical Chemistry; Progressive Disease; Proteins; Research; Thapsigargin; analog; antagonist; scaffold; tool

This project aims to identify antagonists of the thapsigargin:SERCaMP interaction, providing potential research tools to enable better characterization of these diseases and guide development of future therapies. During this period, the collaborative team continued medicinal chemistry optimization of previously identified and validated hit scaffolds. In addition to medicinal chemistry activities, some biotin PEG-linked bromocriptine, biotin-diazirine-linked NCGC00442155, and alkyne-diazirine-linked NCGC00442155 analogs were also synthesized to aid with target identification efforts.

该项目旨在确定Thapsigargin的拮抗剂：Sercamp相互作用，提供潜在的研究工具，以更好地对这些疾病进行表征，并指导未来疗法的发展。在此期间，协作团队继续对先前识别和验证的HIT脚手架进行药物化学优化。除药物化学活性外，一些生物素PEG连接的溴o不平，生物素 - 二氮氨酸连接的NCGC00442155和烯基二氮杂链接的NCGC00442155类似物也被合成以帮助目标识别工作。