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Updated: Apr 28, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Macrocyclic peptoid-Peptide hybrids as inhibitors of class I histone deacetylases
Christian A Olsen1, Ana Montero1, Luke J Leman1
1Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Abstract:
We report the design, synthesis, and biological evaluation of the first macrocyclic peptoid-containing histone deacetylase (HDAC) inhibitors. The compounds selectively inhibit human class I HDAC isoforms in vitro, with no inhibition of the tubulin deacetylase activity associated with class IIb HDAC6 in cultured Jurkat cells. Compared to the natural product apicidin (1), one inhibitor (compound 10) showed equivalent potency against K-562 cells, but was more cytoselective across a panel of cancer cell lines.
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