Welcome to the Bushweller Lab

We are a chemical biology and a structural biology lab. We are fundamentally interested in understanding the role of transcription factor drivers in cancer, particularly in leukemia but in other cancers as well. Our structural biology efforts focus on structure/function studies to understand how transcription factor drivers mediate disease. These studies combine structure determination (NMR, X-ray) and detailed biochemical characterization with functional studies that include effects on gene expression, transcription factor occupancy, epigenetic changes, and effects in relevant mouse models.

The structure/function studies lead to validation of specific binding interactions of these transcription factor drivers as targets for drug development. Our chemical biology efforts focus on the development of small molecule inhibitors of well-validated protein-protein and protein-nucleic acid interactions we have identified. These studies combine medicinal/synthetic chemistry, biochemical assays, and structural studies with functional studies that include effects on gene expression, transcription factor occupancy, epigenetic changes, and effects in relevant mouse models.

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LAB NEWS

September 2020 – Blood Cancer Discovery manuscript showing BCOR binding to MLL-AF9 is essential for leukemia via altered EYA1, MYC, and SIX activity (DOI: ).

August 2020 – Oncotarget manuscript showing effects of CBFβ inhibitors on mammary epithelial cell identity (PMID 32655837).

June 2020 – Bushweller lab welcomes Ashish Kabra as a postdoc in the lab, working on structure-function studies and inhibitor development projects.

May 2020 – Journal of Molecular Biology manuscript on DsbB, DsbD, and CcdA (PMID 32305461)

May 2020 – Bushweller lab welcomes Sudhakar Athe as a postdoc in the lab, working in the medicinal chemistry area on inhibitors of the leukemia fusion protein AML1-ETO.

Sep 2019 – Nature Reviews Cancer manuscript on targeting transcription factor drivers in cancer (PMID 31511663).

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