[Histone deacetylase inhibitors as a new generation of anti-cancer agents]

Author(s): Stepulak A, Stryjecka-Zimmer M, Kupisz K, Polberg K

Affiliation(s): Katedra i Zaklad Biochemii i Biologii Molekularnej, Akademii Medycznej, Lublin. andrzej.stepulak@am.lublin.pl

Publication date & source: 2005-03-11, Postepy Hig Med Dosw (Online)., 59:68-74.

Publication type: Review

The acetylation and deacetylation of histones mediated by histone acetylases and deacetylases influence DNA accessibility to factors regulating replication, repair, and transcription. Histone deacetylases inhibitors (HDI) are inducers of growth arrest, differentiation, and/or apoptosis of many tumors cells by altering the transcription of a small number of genes. The selective tumor specificity of these compounds underscores their potential as new agents for the treatment of cancer. Several HDI have shown anti-tumor activity in vitro and in vivo with remarkably low toxicity in preclinical studies and are currently in phase I and II clinical trials. This review summarizes the molecular mechanism of action of HDI and its clinical application in the treatment of cancer.