---
title: Small-Molecule Inhibition of METTL3 as a Strategy Against Myeloid Leukaemia
description: "hide gateway
Read our publication! Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature 2021.
methyltransferase, epigenetics, AML, SBDD, crystallography"
image: https://news.cyprotex.com/hubfs/shutterstock_1463056829-lab-blue-04%20(1).jpg
---

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# Science Pool

# Small-Molecule Inhibition of METTL3 as a Strategy Against Myeloid Leukaemia

Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Dec 21, 2021 1:49:54 PM

This article published in Nature describes a first-in-class METTL3 inhibitor for the treatment of acute Myeloid Leukaemia.

The publication covers:

- Development of STM2457 following high-throughput screen
- Selectivity screening across the panel of 45 human methyltransferases
- Crystal structure of METTL3-14 complex with STM2457, part of structure-based drug design strategy for this target
- Compound validation in cellular assays and *in vivo* efficacy

[LEARN MORE](https://www.nature.com/articles/s41586-021-03536-w)

 Tags: [Medicinal Chemistry](https://news.cyprotex.com/sciencepool/tag/medicinal-chemistry), [Oncology](https://news.cyprotex.com/sciencepool/tag/oncology), [Articles & Whitepapers](https://news.cyprotex.com/sciencepool/tag/articles-whitepapers), [SBDD](https://news.cyprotex.com/sciencepool/tag/sbdd), [crystallography](https://news.cyprotex.com/sciencepool/tag/crystallography), [epigenetics](https://news.cyprotex.com/sciencepool/tag/epigenetics)