Polypeptide inhibitors targeting rna methyltransferase dimers and uses thereof

By designing the peptide inhibitor M14P1, which targets the METTL14 protein binding site, the translational assembly of the METTL3-METTL14 heterodimer was interfered with, thus solving the problems of drug resistance and significant side effects in existing AML treatments and achieving significant inhibition and apoptosis induction in AML cells.

CN120289585BActive Publication Date: 2026-07-24CHINA PHARM UNIV
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Patent Information

Application Number
CN202510465001.1
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-04-15
Publication Date
2026-07-24
Estimated Expiration
2045-04-15

AI Technical Summary

Technical Problem

Current treatments for acute myeloid leukemia (AML) suffer from high drug resistance and significant side effects. Furthermore, the overexpression of METTL3 and METTL14 plays a crucial role in the development and progression of leukemia and the regulation of chemotherapy response, and there is a lack of effective targeted therapies.

Method used

A peptide inhibitor, M14P1, targeting the METTL14 protein binding site was designed. It inhibits the activity of the METTL3-METTL14 heterodimer by interfering with its translational assembly. The specific amino acid sequence is RRRRRRRRGGGLDLGRVCLRKWGYRRCEDI, with the N-terminus fused with the R8 cell penetration peptide to enhance cell penetration.

Benefits of technology

It significantly inhibits the proliferation and survival of AML cells, reduces the m6A level of poly(A)RNA, induces AML cell apoptosis, and reduces the expression of AML-related proteins, showing unique anti-leukemia activity.

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Abstract

The application belongs to the technical field of biological medicine, and discloses a polypeptide inhibitor targeting RNA methyltransferase dimer and application thereof. The polypeptide inhibitor provided by the application targets a binding site required for METTL3-METTL14 heterodimer assembly. The polypeptide inhibitor of the application effectively inhibits the formation of the heterodimer and its functional activity, for example, can significantly reduce the total m 6 A modification level in acute myeloid leukemia (AML) cells, thereby inhibiting cell proliferation and inducing apoptosis. Experimental results show that the polypeptide inhibitor of the application exhibits good antitumor activity in AML cell lines and can significantly reduce the marker protein level related to AML.
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