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Special Chemical Biology Seminar

Wednesday, March 6, 2024
12:00pm to 1:00pm
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Noyes 153 (J. Holmes Sturdivant Lecture Hall)
Next-generation precision medicine through covalent reactivity: from click chemistry to ‘undruggable' targets
Dr. Qinheng Zheng, Postdoctoral Fellow, Department of Chemistry and Chemical Biology, University of California, San Francisco,
  • Internal Event

Covalent chemical reactivity is a powerful means for the discovery of diverse functional molecules. In this talk, I will first focus on the next-generation click chemistry, sulfur fluoride exchange (SuFEx). I will demonstrate how the selectivity, efficiency, and fidelity of modular SuFEx reactions accelerate the discovery of therapeutic and diagnostic molecules. I will then highlight the recent development of in vivo active covalent inhibitors targeting K-Ras(G12D), the most common activating mutation found in human cancer. K-Ras lacks surface topology for reversible small molecule binding, leading to its notorious characterization as ‘undruggable'. I will report on a series of compounds that rely on covalent reaction with mutant aspartic acid for binding and therefore do not affect the wildtype protein (WT). I will discuss the potency and selectivity of the covalent K-Ras(G12D) inhibitors both in vitro and in vivo.

For more information, please contact Annette Luymes by phone at x6016 or by email at [email protected].