MS-275
MS-275 (also known as entinostat) is a Benzamide Histone deacetylase inhibitor with Antineoplastic properties. It is a synthetic compound that inhibits Histone deacetylase (HDAC), leading to an accumulation of acetylated histones. This can result in chromatin disruption and transcriptional activation of certain genes, which may induce differentiation or apoptosis in tumor cells.
Mechanism of Action[edit | edit source]
MS-275 inhibits class I HDACs, such as HDAC1, HDAC2, and HDAC3, with a higher selectivity over other HDAC classes. The inhibition of HDACs leads to an increase in acetylation levels of histone proteins. This results in the relaxation of chromatin, allowing transcription factors to access DNA and activate gene transcription. The activation of these genes can lead to cell cycle arrest, differentiation, and apoptosis of cancer cells.
Clinical Trials[edit | edit source]
MS-275 has been studied in clinical trials for the treatment of various types of cancer, including breast, lung, ovarian, and colorectal cancers. It has shown promising results in preclinical studies, demonstrating antitumor activity in both in vitro and in vivo models.
Side Effects[edit | edit source]
Common side effects of MS-275 include fatigue, nausea, vomiting, and decreased appetite. More serious side effects can include neutropenia, thrombocytopenia, and anemia.
See Also[edit | edit source]
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Contributors: Prab R. Tumpati, MD
