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.
LAB NEWS
February 2022 – Bushweller lab welcomes Prabhakar Reddy as a postdoc in the lab, working on the synthesis of transcription factor inhibitors.
December 2021 – Science Advances manuscript identifying EP300 KIX domain as target in SCLC.
September 2021 – Bushweller lab welcomes Dhanaraju Mandalapu as a postdoc in the lab, working on the synthesis of transcription factor inhibitors.
June 2021 – Journal of Molecular biology review on AF9 and ENL (PMID 34174329).
September 2020 – Blood Cancer Discovery manuscript showing BCOR binding to MLL-AF9 is essential for leukemia via altered EYA1, MYC, and SIX activity (DOI: ).
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