Accession Number:

AD1053855

Title:

Fragment-Based Approaches to Enhance GTP Competitive KRAS G12C Inhibitors

Descriptive Note:

Technical Report,30 Sep 2016,29 Sep 2017

Corporate Author:

University of Texas Southwestern Medical Center Dallas United States

Personal Author(s):

Report Date:

2017-10-01

Pagination or Media Count:

62.0

Abstract:

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.

Subject Categories:

  • Medicine and Medical Research
  • Pharmacology

Distribution Statement:

APPROVED FOR PUBLIC RELEASE