Experimental research to verify the effect of targeted drugs in epigenetic cancers

Abstract

Epigenetic regulation plays a key role in the development of cancer, and drugs targeting epigenetic modifications (such as DNA methyltransferase inhibitors, histone deacetylase inhibitors, etc.) [2] have become new strategies for cancer treatment. This study aims to verify the anti-tumor effect and mechanism of action of a novel epigenetically targeted drug LSD1 in vitro and in vivo models. Through cell proliferation assays, epigenetic modification detection, transcriptome analysis, and xenograft tumor models, we have confirmed that LSD1 can significantly inhibit cancer cell growth and reverse abnormal epigenetic modifications. This study provides an experimental basis for the development of epigenetic anticancer drugs. Epigenetics is a theory proposed by Waddington in 1942, which refers to heritable changes caused by the unchanged DNA sequence. Many phenomena that cannot be explained by traditional genetics can be well explained by epigenetics. For example, identical twins have exactly the same DNA sequence, but sometimes they can show very different phenotypes; inactivation of female X chromosome and gene silencing. Epigenetic research mainly includes DNA modification, histone modification, chromatin remodeling, and regulation of non-coding RNAs. Among them, DNA methylation and histone modification are the most thoroughly studied, and many inhibitors have been produced for protein factors involved in these modifications.