The human genome is epigenetically organized through a series of modifications to the histone proteins that interact with the DNA. In cancer, many of the proteins that regulate these modifications can be altered in both function and expression. One example of this is the family of histone deacetylases (HDACs), which as their name implies remove acetyl groups from the histone proteins, allowing for more condensed nucleosomal structure. HDACs have increased expression in cancer and are also believed to promote carcinogenesis through the acetylation and interaction with key transcriptional regulators. Given this, small molecule histone deacetylases inhibitors have been identified and developed, which not only inhibit HDACs, but can also lead to growth arrest, differentiation, and/or apoptosis in tumors both in vitro and in vivo. Here, we will discuss some of the recent developments in clinical trials utilizing HDACs inhibitors for the treatment of both hematological malignancies as well as solid tumors.
Histone deacetylase inhibitors in the treatment of hematological malignancies and solid tumors / Federico, Mario; Bagella, Luigi Marco. - In: JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY. - ISSN 1110-7243. - 2011:(2011), pp. 1-12. [10.1155/2011/475641]
Histone deacetylase inhibitors in the treatment of hematological malignancies and solid tumors
Bagella, Luigi Marco
2011-01-01
Abstract
The human genome is epigenetically organized through a series of modifications to the histone proteins that interact with the DNA. In cancer, many of the proteins that regulate these modifications can be altered in both function and expression. One example of this is the family of histone deacetylases (HDACs), which as their name implies remove acetyl groups from the histone proteins, allowing for more condensed nucleosomal structure. HDACs have increased expression in cancer and are also believed to promote carcinogenesis through the acetylation and interaction with key transcriptional regulators. Given this, small molecule histone deacetylases inhibitors have been identified and developed, which not only inhibit HDACs, but can also lead to growth arrest, differentiation, and/or apoptosis in tumors both in vitro and in vivo. Here, we will discuss some of the recent developments in clinical trials utilizing HDACs inhibitors for the treatment of both hematological malignancies as well as solid tumors.File | Dimensione | Formato | |
---|---|---|---|
Federico_M_Histone_deacetylase_inhibitors_in.pdf
accesso aperto
Tipologia:
Versione editoriale (versione finale pubblicata)
Licenza:
Creative commons
Dimensione
1.26 MB
Formato
Adobe PDF
|
1.26 MB | Adobe PDF | Visualizza/Apri |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.