m6A readers: Promising therapeutic targets in cancer treatment

<i>N</i> <sup>6</sup>-methyladenosine (m<sup>6</sup>A) represents the most abundant and functionally significant RNA modification implicated in epigenetic regulation, significantly impacting gene expression through the selective recognition by m<sup>6</sup>A reader proteins. Aberrant expression of m<sup>6</sup>A readers has been associated with cancer progression, contributing to tumor growth, metastasis, drug resistance, and immune evasion. With the increasing research on m<sup>6</sup>A readers, the discovery of small-molecule inhibitors targeting these proteins has emerged as a promising avenue for cancer therapy. This review delineates the classification and functional roles of m<sup>6</sup>A readers across various cancers. Furthermore, we summarize and discuss the recent progress in the development of small-molecule inhibitors, with a focus on the medicinal chemistry perspectives. We hope to provide valuable insights to guide future efforts in drug discovery and rational design targeting m<sup>6</sup>A readers for innovative cancer therapeutics.

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Publication Details

Journal
Acta Pharmaceutica Sinica B
Published
2025-10-15
DOI
https://doi.org/10.1016/j.apsb.2025.10.004
Citations
2
Primary Topic
RNA modifications and cancer
Type
article
Field-Weighted Citation Impact
1.61
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article

m6A readers: Promising therapeutic targets in cancer treatment

Xiaoke Guo, Zhengyu Jiang, Xuetao Chen, Xinyue Wang et al.
2 citations
Acta Pharmaceutica Sinica B
RNA modifications and cancer
1.61
article

m6A readers: Promising therapeutic targets in cancer treatment

Xiaoke Guo, Zhengyu Jiang, Xuetao Chen, Xinyue Wang, Yi Mou, Shuai Wen
article en
2 citations

Abstract

<i>N</i> <sup>6</sup>-methyladenosine (m<sup>6</sup>A) represents the most abundant and functionally significant RNA modification implicated in epigenetic regulation, significantly impacting gene expression through the selective recognition by m<sup>6</sup>A reader proteins. Aberrant expression of m<sup>6</sup>A readers has been associated with cancer progression, contributing to tumor growth, metastasis, drug resistance, and immune evasion. With the increasing research on m<sup>6</sup>A readers, the discovery of small-molecule inhibitors targeting these proteins has emerged as a promising avenue for cancer therapy. This review delineates the classification and functional roles of m<sup>6</sup>A readers across various cancers. Furthermore, we summarize and discuss the recent progress in the development of small-molecule inhibitors, with a focus on the medicinal chemistry perspectives. We hope to provide valuable insights to guide future efforts in drug discovery and rational design targeting m<sup>6</sup>A readers for innovative cancer therapeutics.

Acta Pharmaceutica Sinica BVol. 15(12)
China Pharmaceutical University (CN), State Key Laboratory of Natural Medicine, Taizhou University (CN)
Openalex Percentile: Top 14%
RNA modifications and cancer
1.61
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