综合文献

METTL3 from target validation to the firstsmall-molecule inhibitors: amedicinal chemistryjourney

发布日期: 2023年
作者: Francesco Fiorentino; Martina Menna; Dante Rotili; Sergio Valente; Antonello Mai

摘要

Abstract Click to copy section link Section link copied! High Resolution Image Download MS PowerPoint Slide RNA methylation is a critical mechanism for regulating the transcription and translation of specific sequences or for eliminating unnecessary sequences during RNA maturation. METTL3, an RNA methyltransferase that catalyzes the transfer of a methyl group to the N 6 -adenosine of RNA, is one of the key mediators of this process. METTL3 dysregulation may result in the emergence of a variety of diseases ranging from cancer to cardiovascular and neurological disorders beyond contributing to viral infections. Hence, the discovery of METTL3 inhibitors may assist in furthering the understanding of the biological roles of this enzyme, in addition to contributing to the development of novel therapeutics. Through this work, we will examine the existing correlations between METTL3 and diseases. We will also analyze the development, mode of action, pharmacology, and structure–activity relationships of the currently known METTL3 inhibitors. They include both nucleoside and non-nucleoside compounds, with the latter comprising both competitive and allosteric inhibitors. This publication is licensed under CC-BY 4.0 . License Summary* You are free to share (copy and redistribute) this

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review the actual license before using these materials. License Summary* You are free to share (copy and redistribute)

this article in any medium or format and to adapt (remix, transform, and build upon) the material for any

purpose, even commercially within the parameters below: Creative Commons (CC): This is a Creative Commons

license. Attribution (BY): Credit must be given to the creator. View

full license *Disclaimer This summary highlights only some of the key features and terms of

the

actual license. It is not a license and has no legal value.

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