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Monday, July 1 • 10:45am - 11:15am
Attenuating Oncogenic Transcription with Small Molecules

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The Koehler Lab uses chemical biology approaches to investigate deregulated transcriptional programs in cancer. We are taking on the challenge of developing chemical probes that either directly target oncogenic transcription factors (TFs), currently deemed ‘undruggable,’ or that target ‘nearest neighbor’ proteins that indirectly modulate TF function through mechanisms involving alterations in protein production or protein stability. The probes can be used to further understand the functions surrounding any given transcriptional regulator, clarify their relevance as therapeutic targets, and enable credentialing of mechanisms for targeting by small-molecule drugs. As an example of our approach, probes that impact the MYC oncogene, which encodes a master regulator and is causally associated with most human malignancies, will be described.  The lab identified a unique small molecule, KI-MS2-008, that binds to MAX, inhibits MYC-driven transcription, and stabilizes the MAX homodimer in vitroand in cells while reducing MYC protein levels. The compound displays anti-tumor activities in vitro and in vivo using engineered and non-engineered systems.

avatar for Angela Koehler, PhD

Angela Koehler, PhD

Associate Professor, Biological Engineering, MIT
Angela Koehler is the Goldblith Career Development Professor in Applied Biology in the Department of Biological Engineering at MIT and an intramural member of the David H. Koch Institute for Integrative Cancer Research at MIT. She is also an Institute Member of the Broad Institute... Read More →

Monday July 1, 2019 10:45am - 11:15am EDT
Abigail Adams Salon A/B