Fragment-Based Approaches to Enhance GTP Competitive KRAS G12C Inhibitors

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.

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Document Details

Document Type
Technical Report
Publication Date
Oct 01, 2017
Accession Number
AD1053855

Entities

People

  • Kenneth D Westover

Organizations

  • University of Texas at Austin

Tags

DTIC Thesaurus Topics

  • 1-Ring Heterocyclic Compounds
  • Amines
  • Antineoplastic Agents
  • Cancer
  • Capillary Electrophoresis
  • Cell Line
  • Cell Physiological Processes
  • Chemical Synthesis
  • Chemistry
  • Crystallography
  • Mass Spectra
  • Mass Spectrometry
  • Medical Personnel
  • Molecules
  • Neoplasms
  • Oncology
  • Organic Chemistry
  • Proteins
  • Proteomics
  • Spectrometry
  • Therapy
  • X Rays
  • X-Ray Crystallography

Readers

  • Molecular and Cellular Biochemistry
  • Technical Research and Report Writing.