Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia
Leopold Garnar-Wortzel, Timothy R. Bishop, Seiya Kitamura, Natalia Milosevich, Joshua N. Asiaban, Xiaoyu Zhang, Qinheng Zheng, Emily Chen, Anissa R. Ramos, Christopher J. Ackerman, Eric Hampton, Arnab K. Chatterjee, Travis S. Young, Mitchell Hull, K. Barry Sharpless, Benjamin F. Cravatt, Dennis W. Wolan, Michael A. Erb
Abstract
, and a number of other leukemia proto-oncogenes. Cumulatively, our study establishes YEATS domain inhibition as a viable approach to disrupt the pathogenic function of ENL in acute leukemia and provides the first thoroughly characterized chemical probe for the ENL YEATS domain.
Topics & Concepts
ChromatinLeukemiaFunction (biology)Small moleculeBiologyGeneComputational biologyDrug discoveryCell biologyChemistryGeneticsBiochemistryProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysHistone Deacetylase Inhibitors Research