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公开(公告)号:EP4385998A1
公开(公告)日:2024-06-19
申请号:EP22848550.4
申请日:2022-07-27
发明人: WU, Gang , LU, Yunyu , WU, Liyong , CHENG, Liuxingxing , LEI, Xiaoxuan
IPC分类号: C07K14/00 , C07K7/56 , C07K7/08 , C07K7/06 , C07K1/04 , C07K1/107 , C07K1/34 , C07K1/14 , A61K38/16 , A61K38/10 , A61K38/08 , A61P17/02 , A61P17/16
CPC分类号: A61K38/10 , A61K38/16 , A61K38/08 , A61P17/02 , A61P17/16 , C07K1/04 , C07K1/14 , C07K1/107 , C07K1/34 , C07K7/06 , C07K7/08 , C07K7/56 , C07K14/00
摘要: The present invention provides a cyclic peptide, and a preparation method and use thereof. The cyclic peptide is a series of head-to-tail cyclic peptides or N-terminal and C-terminal cyclized peptides with triazole rings, which are prepared by an azido-alkyne cycloaddition reaction of the whole sequence of linear histamine or the truncated sequence of a linear Hst1 under specific conditions; where the biological activity of the full-sequence head-to-tail cyclic peptide or N-terminal and C-terminal cyclized peptide is increased by more than 1,000 times compared with that of the linear histamine, can significantly improve a dose-effect ratio and clinical efficacy of the histamine over the existing histamine cyclic peptide; the head-to-tail cyclic peptides or N-terminal and C-terminal cyclized peptides of the truncated sequence of the Hst1 has a molecular weight which is only 1/3 of that of the linear Hst1, biological activity that is 15 times that of the linear Hst1, and the cost for achieving the same activity that is only 1/100 of that of the linear Hst1. The entire cyclization process is gentle, simple, convenient and efficient, and can produce high-purity head-to-tail cyclic peptides or N-terminal and C-terminal cyclized peptides, can be used for preparing anti-aging and repairing skin care products, health care products, or medicines, and has a very good prospect for large-scale industrialization.