Title:Selective Inhibitors of Zinc-Dependent Histone Deacetylases. Therapeutic Targets Relevant to Cancer
Volume: 21
Issue: 11
Author(s): Jakub Kollar and Vladimir Frecer
Affiliation:
Keywords:
Epigenetic regulation and cancer, histone deacetylases (HDACs), HDAC inhibitors as anticancer agents, isoform selective HDAC
inhibitors, role of HDAC isoforms in cancer.
Abstract: Histone deacetylases (HDACs), which act on acetylated histones and/or other non-histone protein substrates, represent
validated epigenetic targets for the treatment of cancer and other human diseases. The inhibition of HDAC activity
was shown to induce cell cycle arrest, differentiation, apoptosis as well as a decrease in proliferation, angiogenesis, migration,
and cell resistance to chemotherapy. Targeting single HDAC isoforms with selective inhibitors will help to reveal the
role of individual HDACs in cancer development or uncover further biological consequences of protein acetylation. This review
focuses on conventional zinc-containing HDACs. In its first part, the biological role of individual HDACs in various types of cancer
is summarized. In the second part, promising HDAC inhibitors showing activity both in enzymatic and cell-based assays are surveyed
with an emphasis on the inhibitors selective to the individual HDACs.
