High throughput application of the NanoBiT Biochemical Assay for the discovery of selective inhibitors of the interaction of PI3K-p110α with KRAS

作者：Mohamed Ismail, Gareth M. Davies, Graham Sproat, Tiziana Monteverde, Jonathan Tart, Marta Acebrón-García-de-Eulate, Andrea Gohlke, David C. Hancock, Santosh Adhikari, Sandra Stefanovic-Barrett, David M. Smith, Vikki Flemington, Emma S Gleave-Hanford, Geoffrey A. Holdgate, Jason G. Kettle, Julian Downward · 发表于：SLAS DISCOVERY · 年份：2024 · DOI：10.1016/j.slasd.2024.100197 · 被引用次数：6 · 研究领域：PI3K/AKT/mTOR signaling in cancer、Protein Kinase Regulation and GTPase Signaling、Chronic Lymphocytic Leukemia Research

< 2 μM. By using Differential Scanning Fluorimetry (DSF) we confirmed several compounds that bind directly to purified p110α. The most potent hits will be followed up by co-crystallization with p110α to aid further elucidation of the nature of the interaction and extended optimisation of these compounds.