NCIt definition : The besylate form of bocodepsin, an orally bioavailable inhibitor of the histone deacetylase
(HDAC) subtypes 1 and 4, with potential antineoplastic activity. Upon administration,bocodepsin
targets, binds to and inhibits the activity of HDAC1/4. This results in an accumulation
of highly acetylated chromatin histones, the induction of chromatin remodeling and
an altered pattern of gene expression. This consequently results in a selective transcription
of tumor suppressor genes, tumor suppressor protein-mediated inhibition of tumor cell
division and an induction of apoptosis in tumor cells that overexpress HDAC1/4. HDAC,
which is upregulated in many tumor cell types, deacetylates chromatin histone proteins
and plays a key role in transcriptional regulation and cell cycle progression.;
Semantic type(s)