Developing Small Molecules to Target Gene Regulatory Proteins in Cancer

Using a multidisciplinary approach, we study the proteins involved in gene regulatory pathways including epigenetic proteins, chromatin modification enzymes, and transcription factors. Using novel small molecules as chemical probes and chemical biology tools, we seek further understanding of these targets in cancer with the goal of establishing a biological rationale for cancer therapy. 

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Small Molecule Development
The foundation of our research begins with the rational design of small molecules targeting epigenetic proteins. Using iterative medicinal chemistry techniques along with structural and computational biology, we optimize novel small molecules for use as cancer therapeutics, as well as biological probes.

Biological and Mechanistic Probing
​​Epigenetic proteins, classified as readers, writers and erasers, recognize, make, and remove histone modifications, respectively. These modifications can cause chromatin remodeling that can result in sustained proliferation, one of the hallmarks of cancer. Using chemical tools such as inhibitors and degraders, these proteins can be probed for further biological understanding of their role in cancer with the hopes of creating novel therapies.