2005Journal of Applied BiomedicineOpen access

Inhibitors of histone-deacetylase

Jiřina Vávrová, Martina Řezáčová, Jan Österreicher

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Abstract

Histone acetyltransferase and histone deacetylase activities determine the acetylation status of histones, and have the ability to regulate gene expression through chromatin remodeling. A controlled balance between histone acetylation and histone deacetylation appears to be essential for normal cell growth. In cancer cells, some genes are repressed by inappropriate recruitment of histone deacetylases. The histone deacetylase inhibitors (HDACI) belong to the class of anticancer drugs that are effective in killing proliferating and non-proliferating tumor cells. In this review we discuss molecular mechanisms involved in the induction of cell cycle arrest, differentiation and induction of apoptosis in tumor cells by HDACI.

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Histone acetyltransferase and histone deacetylase activities determine the acetylation status of histones, and have the ability to regulate gene expression through chromatin remodeling. A controlled balance between histone acetylation and histone deacetylation appears to be essential for normal cell growth. In cancer cells, some genes are repressed by inappropriate recruitment of histone deacetylases. The histone deacetylase inhibitors (HDACI) belong to the class of anticancer drugs that are effective in killing proliferating and non-proliferating tumor cells. In this review we discuss molecular mechanisms involved in the induction of cell cycle arrest, differentiation and induction of apoptosis in tumor cells by HDACI.

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Available abstract

Histone acetyltransferase and histone deacetylase activities determine the acetylation status of histones, and have the ability to regulate gene expression through chromatin remodeling. A controlled balance between histone acetylation and histone deacetylation appears to be essential for normal cell growth. In cancer cells, some genes are repressed by inappropriate recruitment of histone deacetylases. The histone deacetylase inhibitors (HDACI) belong to the class of anticancer drugs that are effective in killing proliferating and non-proliferating tumor cells. In this review we discuss molecular mechanisms involved in the induction of cell cycle arrest, differentiation and induction of apoptosis in tumor cells by HDACI.

Key concepts: HDAC11, Histone deacetylase 5, Histone deacetylase, HDAC4, Histone acetyltransferase, Histone deacetylase 2, Acetylation, HDAC10

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