2022 Volume 80 Issue 7 Pages 664-675
Epigenetic mechanisms, including DNA methylation, histone acetylation, and histone methylation, are crucial for regulating cellular functions, cellular differentiation, and developmental changes in organisms. These mechanisms also play key roles in the pathogenesis of various diseases. Conventional drug discovery studies in the field of epigenetics have focused mainly on specific enzymes such as histone deacetylases. However, there has been increasing interest in small molecules targeting the multiprotein enzyme/transcription factor complexes responsible for the epigenetic control of gene expression. Herein, we describe our researches on small molecules that manipulate the epigenetic complexes. The small molecules we identified exhibit significant anticancer activities by inactivating the functions of the specific epigenetic complexes through distinct mechanisms. These small molecules targeting the complexes are expected to expand the potential of drug discovery studies.
