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TitleDiscovery of a Novel DNMT1 Inhibitor with Improved Efficacy in Treating β-Thalassemia.
Journal, issue, pagesAdv Sci (Weinh), Vol. 13, Issue 11, Page e13469, Year 2026
Publish dateDec 5, 2025
AuthorsYijie Shen / Jiale Wei / Shibing Tang / Dongliang Wu / Liangyi Zong / Shuyuan Ma / Qing Xiong / Ruijie Gong / Siyuan Xu / Chuxuan Peng / Qin Feng / Songchen Liu / Qitong Liu / Yuhua Ye / Quan Zhao / Cheng Luo / Peng Huang / Zhihai Li / Xiangqian Kong / Xianjiang Lan /
PubMed Abstractβ-thalassemia is a recessively inherited blood disorder affecting millions worldwide. Pharmacological induction of fetal hemoglobin (HbF) is an effective therapeutic strategy, yet existing DNA ...β-thalassemia is a recessively inherited blood disorder affecting millions worldwide. Pharmacological induction of fetal hemoglobin (HbF) is an effective therapeutic strategy, yet existing DNA methyltransferase (DNMT) inhibitors, although effective HbF inducers, currently are not approved for β-thalassemia treatment. Here, we report that DMT207, a novel non-nucleoside DNMT1 inhibitor, robustly reactivates HbF in HUDEP-2 cells and adult primary erythroblasts with minimal toxicity. In a mouse model of β-thalassemia, DMT207 effectively elevates the levels of mouse fetal- and embryonic-type hemoglobin, promotes the maturation of erythroid cells, and alleviates the splenomegaly. Further multi-omics analyses expose γ-globin as one of the most sensitive genes with promoter demethylation and transcriptional activation following DMT207 treatment. Mechanistically, DMT207 traps DNMT1 into a catalytically inactive conformation and concurrently enhances its interaction with UHRF1, which partially contributes to DNMT1 degradation. These findings highlight the therapeutic potential of DMT207 for β-thalassemia and support its further preclinical development.
External linksAdv Sci (Weinh) / PubMed:41347631 / PubMed Central
MethodsEM (single particle)
Resolution2.85 Å
Structure data

64791

9v5p

EMDB-64791: CryoEM structure of human DNMT1 (aa 698-1616) in complex with hemimethylated dsDNA and inhibitor DMT207
PDB-9v5p: Human DNMT1 (aa 698-1616) in complex with hemimethylated dsDNA and inhibitor DMT207
Method: EM (single particle) / Resolution: 2.85 Å

Chemicals

ChemComp-ZN:
Unknown entry

ChemComp-SAH:
S-ADENOSYL-L-HOMOCYSTEINE

PDB-1eq2:
THE CRYSTAL STRUCTURE OF ADP-L-GLYCERO-D-MANNOHEPTOSE 6-EPIMERASE

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / DNA methyltransferas 1 / inhibitor

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