Pharmacologic Substance
entinostat
[ en-tih-noh-stat ]
Definitions related to entinostat:
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A substance being studied in the treatment of several types of cancer. It blocks enzymes needed for cell division and may kill cancer cells. It is a type of histone deacetylase (HDAC) inhibitor.NCI Dictionary of Cancer TermsU.S. National Cancer Institute, 2021
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A synthetic benzamide derivative with potential antineoplastic activity. Entinostat binds to and inhibits histone deacetylase, an enzyme that regulates chromatin structure and gene transcription. This agent appears to exert dose-dependent effects in human leukemia cells including cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1)-dependent growth arrest and differentiation at low drug concentrations; a marked induction of reactive oxygen species (ROS); mitochondrial damage; caspase activation; and, at higher concentrations, apoptosis. In normal cells, cyclin-dependent kinase inhibitor 1A expression has been associated with cell-cycle exit and differentiation.NCI ThesaurusU.S. National Cancer Institute, 2021
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