Drug name: Vorinostat


Related CSCTT Targets

GSK3-β [ref.1]P49841
microRNA 34a [ref.2]

Vorinostat, SAHA

Cas.no PubChem ID
149647-78-9 5311
Known Target
Histone deacetylase 1Q13547
Histone deacetylase 2Q92769
Histone deacetylase 3O15379
Histone deacetylase 6Q9UBN7
Histone deacetylase 8Q9BY41
Introduction
Vorinostat inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II) at nanomolar concentrations (IC50< 86 nM). These enzymes catalyze the removal of acetyl groups from the lysine residues of histones proteins. In some cancer cells, there is an overexpression of HDACs, or an aberrant recruitment of HDACs to oncogenic transcription factors causing hypoacetylation of core nucleosomal histones. By inhibiting histone deacetylase, vorinostat causes the accumulation of acetylated histones and induces cell cycle arrest and/or apoptosis of some transformed cells. The mechanism of the antineoplastic effect of vorinostat has not been fully characterized.

Vorinostat, SAHA-Structure

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Reference

  • [1] Histone deacetylase inhibitors stimulate dedifferentiation of human breast cancer cells through WNT/β-catenin signaling. Debeb, B. G., et al. (2012).Stem Cells. 30(11):2366-77.
    22961641. [ 22961641 ]
  • [2] Targeting epigenetic regulation of miR-34a for treatment of pancreatic cancer by inhibition of pancreatic cancer stem cells. Nalls, D., et al. (2011).PLoS One. 6(8):e24099.
    21909380. [ 21909380 ]

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