Vorinostat

Definition

Vorinostat is a histone deacetylase inhibitor (HDACi) that is primarily used as a treatment for certain types of cancer, particularly cutaneous T-cell lymphoma (CTCL). By inhibiting histone deacetylases, vorinostat alters gene expression and promotes cell cycle arrest and apoptosis in cancer cells, making it an important tool in the context of cancer therapy and gene regulation.

5 Must Know Facts For Your Next Test

1. Vorinostat was the first HDAC inhibitor approved by the FDA for the treatment of CTCL in patients who have received prior systemic therapy.
2. By inhibiting histone deacetylases, vorinostat increases the acetylation levels of histones, leading to a more open chromatin structure and enhancing the transcription of tumor suppressor genes.
3. Vorinostat has been shown to have multiple mechanisms of action, including altering the expression of genes involved in cell proliferation, apoptosis, and differentiation.
4. The use of vorinostat has been associated with side effects such as fatigue, nausea, and diarrhea, which can impact patient quality of life.
5. Research is ongoing to explore the potential of vorinostat in combination therapies with other anticancer agents to enhance its effectiveness against various cancers.

Review Questions

• How does vorinostat affect gene regulation in cancer cells?
  • Vorinostat affects gene regulation by inhibiting histone deacetylases, leading to increased acetylation of histones. This change results in a more relaxed chromatin structure, which allows for enhanced transcription of genes that suppress tumor growth. By promoting cell cycle arrest and apoptosis through these mechanisms, vorinostat effectively targets cancer cells while sparing normal cells.
• What are the primary therapeutic applications of vorinostat, and how does it contribute to cancer treatment?
  • Vorinostat is primarily used to treat cutaneous T-cell lymphoma (CTCL) in patients who have not responded to previous treatments. Its role as a histone deacetylase inhibitor allows it to modify gene expression profiles in cancer cells, inducing cell death and reducing tumor size. Vorinostat's effectiveness highlights the importance of gene regulation in developing targeted therapies for specific cancer types.
• Evaluate the significance of vorinostat's mechanism of action compared to traditional cancer therapies.
  • Vorinostat's mechanism as a histone deacetylase inhibitor represents a shift from traditional cytotoxic chemotherapy that targets rapidly dividing cells indiscriminately. Instead, it specifically alters gene expression patterns in cancer cells to induce apoptosis and cell cycle arrest. This targeted approach potentially reduces damage to normal cells and minimizes side effects while enhancing therapeutic efficacy. The growing understanding of epigenetic regulation underscores the significance of compounds like vorinostat in modern cancer therapy.

Related terms

Histone Acetylation: The process of adding an acetyl group to histone proteins, which can lead to a more relaxed chromatin structure and increased gene expression.

Apoptosis: A programmed cell death mechanism that is crucial for eliminating damaged or unwanted cells, and is often disrupted in cancer.

Gene Expression Regulation: The various mechanisms that control the timing and level of gene expression in cells, affecting how genes are turned on or off.