Conjugate and application of conjugate in degrading beta-catenin protein

The invention provides application of E3 ubiquitin ligase VHL in degradation of beta-catenin protein or inhibition of a Wnt/beta-catenin signal pathway and a conjugate as well as a preparation methodand application of the conjugate. The conjugate comprises a first peptide fragment suitable for bindi...

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Hauptverfasser: HU HONGGANG, LIU LEI, LIAO HONGWEI, ZHAO LIANZHENG, CHEN YEGUANG, LI XIANG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides application of E3 ubiquitin ligase VHL in degradation of beta-catenin protein or inhibition of a Wnt/beta-catenin signal pathway and a conjugate as well as a preparation methodand application of the conjugate. The conjugate comprises a first peptide fragment suitable for binding to beta-catenin protein; a second peptide fragment suitable for binding to E3 ubiquitin ligase VHL; a connecting arm, wherein the first peptide fragment is connected with second peptide fragment through the connecting arm. The E3 ubiquitin ligase VHL can be used for carrying out ubiquitination modification on beta-catenin protein, so that the ubiquitination beta-catenin protein is degraded by protease, a Wnt/beta-catenin signal channel is inhibited, and the effects of inhibiting cancer cellproliferation and tumor-forming ability are achieved; wide scientific research and clinical application prospects are realized. 本发明提出了E3泛素连接酶VHL在降解β-catenin蛋白或抑制Wnt/β-catenin信号通路中的用途及缀合物及其制备方法和用途,所述缀合物包括:第一肽段,所述第一肽段适于与β-cateni