The Sound of Evolution
Romidepsin
Mechanism of action:
Romidepsin is a histone deacetylase inhibitor. Romidepsin is a cyclic peptide prodrug. After entering the cell, its disulfide bond is reduced, releasing an active thiol group that binds to the zinc ion, Zn2+, at the catalytic center of class I histone deacetylases and inhibits their deacetylase activity. Once histone deacetylases are inhibited, histones remain highly acetylated, and chromatin becomes more relaxed in structure.
Reference(s):
1. VanderMolen KM et al. (2011). Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma. J Antibiot (Tokyo).
2. Valdez BC et al. (2015). Romidepsin targets multiple survival signaling pathways in malignant T cells. Blood Cancer J.