Modulators of Secreted ER Ca2+ Monitoring Protein (SERCaMP)

分泌型 ER Ca2 监测蛋白 (SERCaMP) 调节剂

• 批准号: 10011381
• 负责人: Anton Simeonov
• 金额: $ 25.03万
• 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/10011381
• 关键词: Biotin; Bromocriptine; Calcium; Development; Diabetes Mellitus; Disease; Functional disorder; Future; Homeostasis; Link; Monitor; Parkinson Disease; Pharmaceutical Chemistry; Progressive Disease; Proteins; Research; Thapsigargin; analog; 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 analogs were also synthesized to aid with target identification efforts.

该项目旨在鉴定毒胡萝卜素：SERCaMP 相互作用的拮抗剂，提供潜在的研究工具，以便更好地表征这些疾病并指导未来疗法的开发。 在此期间，合作团队继续对先前识别和验证的命中支架进行药物化学优化。 除了药物化学活性外，还合成了一些生物素 PEG 连接的溴隐亭类似物以帮助靶标识别工作。