VORINOSTAT

new epigenetic drug

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  • Created by: ava.scott
  • Created on: 12-04-18 10:57
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  • VORINOSTAT
    • WHAT?
      • A histone deacetylase (HDAC) inhibitor
      • molecular weight
        • 264
      • Treats cutaneous T cell lymphoma
        • CTCL
    • ref
      • Bubna 2015
    • HOW DOES IT DO IT?
      • Transcriptional activity
        • causes acetylation of Bcl-6, a TF
          • inhibits the represseing effect of Bcl-6
            • this would presumably work on expressing tumor suppressor genes
        • acetylation of lysine residues
          • such as alpha tubulin
          • such as heat-shock protein 90
          • decreases pro-growth activity and pro-survival clients
            • such as Brc-abl
            • such as c-raf
            • such as AKT in human leukemia
      • Non-transcriptional
        • cell cycle arrest
          • upregulates cyclin-independent kinase inhibtor p 21
            • antagonises cyclin-CDK complexes
              • causes G1 cycle arrest
        • apoptosis
          • changes balance of pro and anti-apoptosis enzymes
          • enhances external signals for cell death
          • down regulates cell survival proteins such as
            • BCL-1 and BCL-2
              • THESE REGULATE MITOCHONDRIAL ACTIVITY
          • vorinostat stabilises p53 which is important in CTCL lines
        • inhibits angiogenesis
          • induces hypoxia-inducible factor (HIF) and blocks angiogenesis.
      • Inhibits class I and II HDAC enzymes
        • causes acetylated proteins to accumulate, such as histones
      • we dont know:
        • how it is selective for tumor cells
          • the presence of thioredoxin in normla cells may buffer the drugs effect
        • Untitled

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