Reading Cancer: Chromatin Readers as Druggable Targets for Cancer Treatment.
Catia MioStefania BulottaDiego RussoGiuseppe DamantePublished in: Cancers (2019)
The epigenetic machinery deputed to control histone post-translational modifications is frequently dysregulated in cancer cells. With epigenetics being naturally reversible, it represents a good target for therapies directed to restore normal gene expression. Since the discovery of Bromodomain and Extra Terminal (BET) inhibitors, a great effort has been spent investigating the effects of chromatin readers' inhibition, specifically the class of proteins assigned to bind acetylated and methylated residues. So far, focused studies have been produced on epigenetic regulation, dissecting a specific class of epigenetic-related proteins or investigating epigenetic therapy in a specific tumor type. In this review, recent steps toward drug discovery on the different classes of chromatin readers have been outlined, highlighting the pros and cons of current therapeutic approaches.
Keyphrases
- gene expression
- dna methylation
- drug discovery
- genome wide
- dna damage
- papillary thyroid
- transcription factor
- small molecule
- stem cells
- squamous cell
- squamous cell carcinoma
- working memory
- mesenchymal stem cells
- high throughput
- young adults
- bone marrow
- childhood cancer
- smoking cessation
- lymph node metastasis
- case control