Tackling Undruggable Cancer Targets using Chemoproteomic Platforms

使用化学蛋白质组学平台应对无法成药的癌症靶点

• 批准号: 10670980
• 负责人: Daniel Nomura
• 金额: $ 90.97万
• 依托单位: UNIVERSITY OF CALIFORNIA BERKELEY
• 依托单位国家: 美国
• 财政年份: 2022
• 资助国家: 美国
• 起止时间: 2022-08-01 至 2029-07-31
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10670980
• 关键词: Antineoplastic Agents; Binding; Development; Ligands; Malignant Neoplasms; Modality; Proteins; Proteome; Research; Therapeutic; chemoproteomics; drug discovery; innovative technologies; next generation; novel therapeutics; pharmacologic; targeted treatment

One of the biggest challenges facing cancer drug discovery is that >90 % of the proteome is currently considered “undruggable” because most proteins do not possess known binding pockets or “ligandable hotspots” that can be pharmacologically and functionally targeted for therapeutic benefit 1. Tackling the undruggable proteome requires the development of innovative technologies for ligand discovery AND the discovery of novel therapeutic modalities to functionally manipulate the undruggable proteome for therapeutic benefit. The Nomura Research Group is focused on reimagining druggability by advancing and applying chemoproteomic platforms to tackle the undruggable proteome, towards developing next-generation therapies and therapeutic modalities for cancer.

癌症药物发现面临的最大挑战之一是蛋白质组的90％是 目前被认为是“不可能”的，因为大多数蛋白质都没有已知的约束 口袋或“可韧带热点”，可以在药物上和功能上针对的针对性 治疗益处1。解决不良蛋白质组需要开发 配体发现的创新技术和新型热模式的发现 在功能上操纵不良蛋白质组的治疗益处。野村 研究小组的重点是通过推进和应用来重新想象可药用 化学蛋白质组学平台以应对不良蛋白质组，以开发开发 癌症的下一代疗法和治疗方法。