Chemicals Facilitating Reprogramming: Targeting the SAM Binding Site to Identify Novel Methyltransferase Inhibitors
© 2014 John Wiley & Sons, Ltd. Reprogramming of somatic cells to a pluripotent state has been achieved by viral-mediated transduction of defined transcription factors. In order to achieve the goal of clinical application, it is necessary to overcome a variety of limitations, including poor reprogramming efficiencies and viral integration. One strategy is to identify small-molecule inhibitors that can improve reprogramming efficiency or replace defined transcription factors. Several reports have demonstrated that modulation of chromatin-modifying enzymes can significantly improve reprogramming efficiency. Key enzymes include DNA and histone methyltransferases, which utilize the cofactor S-adenosyl methionine (SAM) to transfer a methyl group. In this chapter, we review our efforts to identify SAM analogues by virtual screening.
Publication Source (Journal or Book title)
Chemical Biology in Regenerative Medicine: Bridging Stem Cells and Future Therapies
Kim, J., Rim, J., Crochet, R., Lee, Y., Staszkiewicz, J., Gao, R., & Eilertsen, K. (2014). Chemicals Facilitating Reprogramming: Targeting the SAM Binding Site to Identify Novel Methyltransferase Inhibitors. Chemical Biology in Regenerative Medicine: Bridging Stem Cells and Future Therapies, 163-179. https://doi.org/10.1002/9781118695746.ch10