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Acetylation of histories is cooperatively regulated by two groups of enzymes, histone acetyltransferases and histone deacetylases. Histone acetylation status plays a fundamental role in the level of gene transcription; numerous studies have demonstrated that histone deacetylase inhibitors cause cell growth arrest, apoptosis, and differentiation in various cells including human mammary gland and endometrial cells by altering transcription of a small number of genes. A recent study has also shown that a highly acetylated histone status alters cell motility. After the present review of the published reports on the mechanisms underlying histone acetylation and in vitro effects of histone deacetylase inhibitors, we conclude that this class of agents may have potential not only as anticancer drugs, but also as inducers of differentiation and/or motility for benign gynecologic conditions such as endometriosis and disorders of endometrial differentiation and dysfunction.