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发明公开
CN110478339A 紫铆因在制备靶向恢复突变p53构象药物中的应用 审中-实审

紫铆因在制备靶向恢复突变p53构象药物中的应用
摘要：
本发明公开了紫铆因在制备靶向恢复突变p53构象药物中的应用，本发明实验结果显示：化合物Butein可以降低突变p53的表达，增加突变p53背景下肿瘤细胞中野生型p53的表达，上调p53下游靶基因puma、p21、noxa；因此化合物Butein可以恢复突变p53构象，发挥抗肿瘤作用；同时，紫铆因可特异性降解突变p53细胞中p53的表达；揭示了天然化合物紫铆因在靶向突变p53并恢复其构象，发挥抗肿瘤功能及其维持干细胞的干性，这些特征表明紫铆因具有针对恢复和降解突变p53功能的个性化治疗药物的应用潜力。
摘要（英）：

The invention discloses an application of butein in preparation of drugs for targeted restoring of conformation of mutant p53. Experimental results show that the compound butein can reduce the expression of the mutant p53, increase the expression of wild-type p53 in tumor cells under the background of the mutant p53, and up-regulate the downstream target genes puma, p21 and noxa of p53; therefore,the compound butein can restore the conformation of the mutant p53 and play an anti-tumor role. At the same time, the butein can specifically decrease the expression of p53 in mutant p53 cells; the natural compound butein is revealed to target to the mutant p53, restore the conformation, play the anti-tumor role and maintain the dryness of stem cells. The characteristics indicate that the buteinhas an application potential as personalized therapy drugs with the functions of restoring and degradation of the mutant p53.

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