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

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).

Aug 2019 – Vet. Comp. Oncology manuscript showing CBFβ inhibitors are effective against canine osteosarcoma (PMID 31381810).

Aug 2019 – Leukemia manuscript showing CBFβ inhibitors synergize with lenalidomide to inhibit the growth of multiple myeloma cells (PMID 30760870).

Aug 2019 – Bushweller lab welcomes Hanuman Kalmode as a new postdoc in the lab, working in the medicinal chemistry area.

July 2019 – Blood manuscript showing CBFβ inhibitors are particularly effective against RUNX1 mutant leukemia cells (PMID: 31023702).

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