A covalent compound selectively inhibits RNA demethylase ALKBH5 rather than FTO-Reference-Cited by-同舟云学术

A covalent compound selectively inhibits RNA demethylase ALKBH5 rather than FTO

Published:2024 Issue:4 Volume:5 Page:335-343
ISSN:2633-0679
Container-title:RSC Chemical Biology
language:en
Short-container-title:RSC Chem. Biol.

Author:

Lai Gan-Qiang¹²,Li Yali¹,Zhu Heping³,Zhang Tao¹^ORCID,Gao Jing¹,Zhou Hu¹³²^ORCID,Yang Cai-Guang¹³²⁴^ORCID

Affiliation:

1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China

2. University of Chinese Academy of Sciences, Beijing 100049, China

3. School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China

4. Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, China

Abstract

We discovered that TD19 covalently and selectively inhibits ALKBH5 rather than FTO demethylase in both protein-based and tumor cell-based assays.

Funder

National Natural Science Foundation of China

National Key Research and Development Program of China

Publisher

Royal Society of Chemistry (RSC)

Link

http://pubs.rsc.org/en/content/articlepdf/2024/CB/D3CB00230F

Reference48 articles.

1. Grand Challenge Commentary: RNA epigenetics?

2. Dynamic RNA Modifications in Gene Expression Regulation

3. A METTL3–METTL14 complex mediates mammalian nuclear RNA N6-adenosine methylation

4. A Light‐Controllable Chemical Modulation of m 6 A RNA Methylation

5. N6-Methyladenosine in nuclear RNA is a major substrate of the obesity-associated FTO

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