FTO inhibitors or for leukemia treatment
April 24, 2019 Source: Science Network
Window._bd_share_config={ "common":{ "bdSnsKey":{ },"bdText":"","bdMini":"2","bdMiniList":false,"bdPic":"","bdStyle":" 0","bdSize":"16"},"share":{ }};with(document)0[(getElementsByTagName('head')[0]||body).appendChild(createElement('script')) .src='http://bdimg.share.baidu.com/static/api/js/share.js?v=89860593.js?cdnversion='+~(-new Date()/36e5)];Recently, the Yang Caiguang research group of the Shanghai Institute of Materia Medica of the Chinese Academy of Sciences has cooperated with the Beckman Institute of the United States Hope City and the University of Florida to make new progress in the direction of chemical intervention in RNA methylation. Related research results have recently been published online in the "Cell" publication "Cell Cancer".
Adipose tissue and obesity-related protein (FTO) have been confirmed as demethylating enzymes that regulate RNA methylation, and FTO is one of the important oncogenes in cancers such as leukemia, breast cancer, and glioblastoma. However, internationally, FTO inhibitors and their intervention in RNA methylation modification in the anti-tumor target drug research are still in the early stage of exploration.
Yang Cai adverts to the Journal of Chinese Academy of Sciences. This study targets FTO, which is highly expressed in acute myeloid leukemia subtypes. Based on the molecular mechanism of FTO recognition of methylated RNA substrates, the design and synthesis optimization of compounds based on crystal structure is applied. By means of other means, FTO small molecule inhibitors are obtained.
The study found that this compound can selectively inhibit the demethylation of FTO in leukemia cells, up-regulate the methylation of key genes in leukemia, increase the abundance of tumor suppressor proteins, and reduce the abundance of oncoproteins. It shows the effect of inhibiting the proliferation of leukemia cells.
"This study has fully characterized the mechanism of action of FTO inhibitors at the molecular and cellular levels, but its intracellular targeting needs to be further explored." Yang Caiguang said that FTO can be used as an anti-tumor drug target and in pharmacological functions. Initial confirmation was obtained, and this study indicates a new direction for molecularly targeted RNA epigenetic anti-tumor research.
Paper related information: https://doi.org/10.1016/j.ccell.2019.03.006
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