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Abstract:
Despite tremendous efforts and progress in combating cancer over the last few decades, many cancers remain undiagnosable at early stage and difficult-to-treat. More than 10 million people die from cancer each year worldwide. In this talk, I will discuss how to creatively design molecules in chemistry and biology to advance cancer therapeutics. I will describe how to develop highly useful C‒H activation reactions by designing novel ligands and directing groups and how these synthetic methods can potentially accelerate early anti-cancer drug discovery. I will then focus on targeting an important DNA repair enzyme MUTYH for targeted cancer therapy by designing activity-based fluorescent probes and applying the probes with high throughput screen (HTS) to identify small-molecule modulators. Lastly, I will demonstrate how to use the probes to diagnose MUTYH-associated polyposis (MAP) which is a genetic disorder that causes a range of cancers.