qHTS to Identify Activators and Inhibitors of Wip1

qHTS 鉴定 Wip1 激活剂和抑制剂

• 批准号: 10916024
• 负责人: Matthew Hall
• 金额: $ 12.58万
• 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/10916024
• 关键词: Apoptotic; Automobile Driving; Basic Science; Binding; Biological Assay; Chemicals; Clinical; DNA Damage; Drug Kinetics; Environment; Family; Fluorescence; Health; Human; Human Genome; Malignant Neoplasms; Mass Spectrum Analysis; National Center for Advancing Translational Sciences; PPM1D gene; Prognosis; Protein Serine/Threonine Phosphatase; Proteins; Rare Diseases; Reporter; Research; Surface Plasmon Resonance; TP53 gene; Translations; Work; anticancer treatment; drug candidate; improved; inhibitor; member; novel; overexpression; pharmacologic; programs; protein phosphatase 2C; response; scaffold; screening; small molecule; therapeutic development; tool; tumor growth

The NCATS Early Translation Branch (ETB) hosts a broad and comprehensive program for the discovery of drug candidates directed towards rare diseases and pharmacological tools to probe the function of the human genome. ETB conducts research to understand the underlying principles driving the translation of basic research discoveries into tangible improvements in human health. During this period, the project team worked to validate previously identified inhibitors and activators of WIP1. The team confirmed activity of these molecules in a RapidFire mass spectrometry screening assay, fluorescence reporter orthogonal assay, and binding studies by surface plasmon resonance (SPR). These new scaffolds could be candidates for optimization, which may provide better pharmacokinetics.

NCATS 早期翻译分部 (ETB) 主持了一项广泛而全面的计划，旨在发现针对罕见疾病的候选药物和探索人类基因组功能的药理学工具。 ETB 开展研究以了解推动基础研究发现转化为人类健康切实改善的基本原理。 在此期间，项目团队致力于验证先前确定的 WIP1 抑制剂和激活剂。该团队通过 RapidFire 质谱筛选分析、荧光报告正交分析和表面等离子共振 (SPR) 结合研究证实了这些分子的活性。这些新支架可能是优化的候选者，这可能会提供更好的药代动力学。