CYCLIC PEPTIDE AND PREPARATION METHOD AND USE THEREOF
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United States of America Patent
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Oct 10, 2024
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Jul 27, 2022
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Jul 27, 2021
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Abstract
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. 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.
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