Journal
JOURNAL OF ANTIBIOTICS
Volume 64, Issue 8, Pages 525-531Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/ja.2011.35
Keywords
Chromobacterium violaceum; cutaneous T-cell lymphoma; depsipeptide; histone deacetylase inhibitor; Istodax; romidepsin
Funding
- National Cancer Institute/National Institutes of Health, Bethesda, MD, USA [P01-CA125066]
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Romidepsin (Istodax), a selective inhibitor of histone deacetylases (HDACs), was approved for the treatment of cutaneous T-cell lymphoma in November 2009 by the US Food and Drug Administration. This unique natural product was discovered from cultures of Chromobacterium violaceum, a Gram-negative bacterium isolated from a Japanese soil sample. This bicyclic compound acts as a prodrug, its disulfide bridge being reduced by glutathione on uptake into the cell, allowing the free thiol groups to interact with Zn ions in the active site of class I and II HDAC enzymes. Due to the synthetic complexity of the compound, as well as the low yield from the producing organism, analogs are sought to create synthetically accessible alternatives. As a T-cell lymphoma drug, romidepsin offers a valuable new treatment for diseases with few effective therapies. The Journal of Antibiotics (2011) 64, 525-531; doi:10.1038/ja.2011.35; published online 18 May 2011
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