Journal article
An efficient high-throughput screening method for MYST family acetyltransferases, a new class of epigenetic drug targets
H Falk, T Connor, H Yang, KJ Loft, JL Alcindor, G Nikolakopoulos, RN Surjadi, JD Bentley, MK Hattarki, O Dolezal, JM Murphy, BJ Monahan, TS Peat, T Thomas, JB Baell, JP Parisot, IP Street
Journal of Biomolecular Screening | SAGE PUBLICATIONS INC | Published : 2011
Abstract
Epigenetic aberrations are increasingly regarded as key factors in cancer progression. Recently, deregulation of histone acetyltransferases (HATs) has been linked to several types of cancer. Monocytic leukemia zinc finger protein (MOZ) is a member of the MYST family of HATs, which regulate gene expression in cell proliferation and differentiation. Deregulation of these processes through constitutively active MOZ fusion proteins gives rise to the formation of leukemic stem cells, rendering MOZ an excellent target for treating myeloid leukemia. The authors implemented a hit discovery campaign to identify small-molecule inhibitors of MOZ-HAT activity. They developed a robust, homogeneous assay ..
View full abstractGrants
Awarded by Australian Research Council
Funding Acknowledgements
The authors acknowledge the financial support of the Cancer Therapeutics CRC, established and supported under the Australian Government's Cooperative Research Centre's Program and a fellowship from the Australian Research Council (FT100100100) for JMM.