Fragment-Based Approaches to Enhance GTP Competitive KRAS G12C Inhibitors
Technical Report,30 Sep 2016,29 Sep 2017
University of Texas Southwestern Medical Center Dallas United States
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During the current period we completed work on a series of guanine nucleotide mimetics and published results. As part of this we developed and reported a novel method of measuring small molecule binding to KRAS G12C active site. We also published 2 additional manuscripts about KRAS G12C directed compounds that bind to the switch 2 pocket. Reports of 2 novel assays were also included in these reports. These compounds showed improved potency compared to previously reported compounds. Structural analysis of KRAS using x-ray crystallography was provided in all papers.
- Medicine and Medical Research