Nitrogen-terminal fatty acid modified anticancer peptide and application thereof

The anticancer peptide modified with N-terminal fatty acids solves the problems of complex structure and limited activity of existing anticancer peptides, achieving significant inhibition of various tumor cells and low toxicity, and is suitable for combination therapy of various cancers.

CN121914213APending Publication Date: 2026-04-24HENAN UNIV OF SCI & TECH
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Patent Information

Application Number
CN202610185365.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-02-09
Publication Date
2026-04-24

AI Technical Summary

Technical Problem

Existing anticancer peptides have complex structures, limited anticancer activities, and significant toxicity to normal cells, making it difficult to effectively inhibit various tumor cells.

Method used

A class of anticancer peptides modified with nitrogen-terminal fatty acids were designed. Short peptides at the 8-position were constructed by modifying lysine, tryptophan and glutamic acid with straight-chain fatty acids. The carbon-terminus was an amide structure. The peptides were prepared by conventional solid-phase synthesis, which simplified the synthesis process and reduced the cost.

Benefits of technology

This anticancer peptide exhibits significant antitumor activity against a variety of tumor cells, possesses broad-spectrum anticancer activity, and has low toxicity to normal cells. It is suitable for the preparation of clinical antitumor drugs, especially for cervical cancer, non-small cell lung cancer, liver cancer, and breast cancer, and has promising application prospects.

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Abstract

The invention belongs to the field of polypeptides, and particularly relates to a nitrogen-terminal fatty acid modified anticancer peptide and application thereof. The nitrogen terminal of the anti-cancer peptide is modified by straight-chain fatty acid, the carbon terminal of the anti-cancer peptide is of an amide structure, and the structural general formula of the anti-cancer peptide is Cn-KaWbEc, wherein Cn represents a fatty acid chain with n carbon atoms, a is the number of lysine K, b is the number of tryptophan W, and c is the number of glutamic acid E; n is equal to 6-18; a + b + c = 8; a = 3 or 4, b = 3 or 4, and c = 0, 1 or 2. According to the anti-cancer peptide modified by the nitrogen-terminal fatty acid, lysine, tryptophan and glutamic acid are used for constructing 8-bit oligopeptide, a nitrogen-terminal fatty acid modification strategy and a carbon-terminal amide structure are matched, and the anti-cancer peptide is simple in structure and low in synthesis cost. In-vitro anti-tumor experiments and toxicity experiments show that the anti-cancer peptide has remarkable anti-tumor activity on various tumor cells such as 4T1, Hela, A549, HCCLM3 and the like, and shows broad-spectrum anti-cancer activity.
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