2454396-80-4Relevant academic research and scientific papers
KRAS G12D INHIBITORS
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, (2022/02/15)
The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12DInhibitor
Wang, Xiaolun,Allen, Shelley,Blake, James F.,Bowcut, Vickie,Briere, David M.,Calinisan, Andrew,Dahlke, Joshua R.,Fell, Jay B.,Fischer, John P.,Gunn, Robin J.,Hallin, Jill,Laguer, Jade,Lawson, J. David,Medwid, James,Newhouse, Brad,Nguyen, Phong,O'Leary, Jacob M.,Olson, Peter,Pajk, Spencer,Rahbaek, Lisa,Rodriguez, Mareli,Smith, Christopher R.,Tang, Tony P.,Thomas, Nicole C.,Vanderpool, Darin,Vigers, Guy P.,Christensen, James G.,Marx, Matthew A.
, p. 3123 - 3133 (2021/12/27)
KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of KRASG12D presents a significant challenge due to the requirement of inhibitors to bind KRASG12D with high enough affinity to obviate the need for covalent interactions with the mutant KRAS protein. Here, we report the discovery and characterization of the first noncovalent, potent, and selective KRASG12D inhibitor, MRTX1133, which was discovered through an extensive structure-based activity improvement and shown to be efficacious in a KRASG12D mutant xenograft mouse tumor model.
KRAS G12D INHIBITORS
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, (2021/03/05)
The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
KRAS G12C INHIBITORS
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, (2020/07/25)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
