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Issue 4, 2017
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Quantitative measurement of intracellular HDAC1/2 drug occupancy using a trans-cyclooctene largazole thiol probe

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Abstract

Histone deacetylases (HDACs) regulate diverse cellular processes, and are promising targets for a number of diseases. Here we describe the design and utilization of a largazole-based chemical probe to quantitatively measure the intracellular occupancy of HDAC1 and HDAC2 by dacinostat. Surprisingly, the probe was unable to enrich HDAC3 despite its nanomolar potency in a biochemical assay, further proving the necessity of cell-based target occupancy assays to understand compound potency in physiologically-relevant settings. This occupancy assay has the potential to aid the development of novel HDAC1/2 inhibitors in drug discovery.

Graphical abstract: Quantitative measurement of intracellular HDAC1/2 drug occupancy using a trans-cyclooctene largazole thiol probe

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Publication details

The article was received on 11 Nov 2016, accepted on 23 Dec 2016 and first published on 09 Jan 2017


Article type: Research Article
DOI: 10.1039/C6MD00633G
Citation: Med. Chem. Commun., 2017,8, 767-770
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    Quantitative measurement of intracellular HDAC1/2 drug occupancy using a trans-cyclooctene largazole thiol probe

    H. Xu, L. R. Roberts, S. Chou, B. Pierce, A. Narayanan and L. H. Jones, Med. Chem. Commun., 2017, 8, 767
    DOI: 10.1039/C6MD00633G

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