Preparation method and application of tachyplesin I derivative TPI-Se modified by two pairs of diselenide bonds

The invention provides a tachyplesin I derivative TPI-Se modified by two pairs of diselenide bonds, the structural formula of the tachyplesin I derivative TPI-Se is as follows: imgabs0 #, and the invention also provides a preparation method of the tachyplesin I derivative TPI-Se modified by the two...

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Hauptverfasser: LIANG RUI, LUAN XIN, ZHANG XIAOKUN, REN MAOMAO, WU YE, LU SHENGXIN, ZHANG WEIDONG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a tachyplesin I derivative TPI-Se modified by two pairs of diselenide bonds, the structural formula of the tachyplesin I derivative TPI-Se is as follows: imgabs0 #, and the invention also provides a preparation method of the tachyplesin I derivative TPI-Se modified by the two pairs of diselenide bonds, and the method can be used for modifying peptide compounds containing multiple pairs of diselenide bonds. The tachyplesin I derivative TPI-Se has significantly improved reduction stability, and in-vivo and in-vitro pharmacological experiments show that compared with prototype peptide Tachyplesin I, the TPI-Se not only has the functions of dissolving tumors and inducing tumor immunogen cell death, but also can promote activation of dendritic cells and cytotoxic T cells, effectively inhibit tumor growth of melanoma-bearing mice, and has a good application prospect. And complete ablation of 66% of tumors is realized. The compound TPI-Se has the potential of being developed into a novel oncol