FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases.

By R. Furumai, Akihisa Matsuyama, N. Kobashi, Kun-Hyung Lee, M. Nishiyama, H. Nakajima, A. Tanaka, Y. Komatsu, N. Nishino, Minoru Yoshida and 1 more. Cancer Research, 2002

732 citations recorded by the source corpus.

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Citations in the corpus

Erasers of histone acetylation: the histone deacetylase enzymes. (2014, background): “Although crystal structure of the HDAC-FK228 (a cyclic peptide inhibitor) complex has not yet been solved, computer-modeling studies suggest that one of the thiol groups generated by reduction can coordinate to the active site zinc ion (Furumai et al. 2002).”
HDAC family: What are the cancer relevant targets? (2009, background): “The cyclic tetrapeptide depsipeptide (FK228, romidepsine) is particularly active against HDAC1 and to a lesser extent against HDAC2 [89].”
Histone Deacetylase Inhibitors as Anticancer Drugs (2017, background): “It is a prodrug, which is reductively activated to a metabolite containing a thiol group that chelates the zinc ions in the active center of the HDAC of class I [29].”
Anticancer activities of histone deacetylase inhibitors (2006, background): “For example, depsipeptide reportedly possesses stronger activity against HDAC1 and HDAC2 than against the class II HDAC4 and HDAC”
Romidepsin in the treatment of cutaneous T-cell lymphoma (2011, unknown): “…have also reported that in patients with acute myelogenous leukemia (AML) and CLL treated with 13 mg/m 2 of romidepsin intravenously on days 1, 8, and 15, HDAC inhibition and histone acetylation of at least 100% were observed, and the levels of H3 and H4 histone deacetylation were higher at…”
The role of histone deacetylases (HDACs) in human cancer (2007, background): “Other studies have reported high levels of HDAC3 and HDAC6 expression in colon and breast cancer specimens, respectively (Zhang et al., 2004; Wilson et al., 2006).”