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An update on DOT1LWT/MUT modulators as a promising anticancer strategy.

Bioorganic & medicinal chemistry - 1 Oct 2026

Fan Xue, Liu Shuyu, Wang Luyao, Tan Zehui, Zhai Xin

Abstract excerpt

Disruptor of telomeric silencing 1-like (DOT1L) is the only identified H3K79 methyltransferase and its dysregulation, mutations, or aberrant activity are closely implicated in the pathogenesis and progression of various diseases. Due to their key roles in leukemogenesis and lung carcinogenesis, DOT1L and its mutations have been studied as attractive therapeutic targets for over a decade, resulting in the...

Topics

Humans
Antineoplastic Agents
Histone-Lysine N-Methyltransferase
Enzyme Inhibitors
Mutation
Allosteric Regulation
Animals
Molecular Structure

Source

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Identifiers

PMID: 42424823
DOI: 10.1016/j.bmc.2026.118748

Genes

DOT1L

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 31 Aug 2026.

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An update on DOT1LWT/MUT modulators as a promising anticancer strategy.PMID 42424823Read ↗

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Molecular pathways: protein methyltransferases in cancer.Semantic proximity Read ↗

Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein–Protein Interactions between DOT1L and MLL-AF9/MLL-ENLSemantic proximity Read ↗

Targeting Recruitment of Disruptor of Telomeric Silencing 1-like (DOT1L)Semantic proximity Read ↗

DOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia.Semantic proximity Read ↗

The histone methyltransferase DOT1L is required for proper DNA damage response, DNA repair, and modulates chemotherapy responsivenessSemantic proximity Read ↗

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