PI3K抑制剂与非小细胞性肺癌

发布时间：2018-04-12 11:10

本文选题：PIK/Akt/m + TOR信号通路　；参考：《中国肿瘤生物治疗杂志》2017年05期

【摘要】：磷脂酰肌醇3-激酶(phosphatidylinositol 3-kinase,PI3K)/蛋白激酶B(protein kinase B,Akt)/哺乳动物雷帕霉素靶蛋白(mammalian target of rapamycin,m TOR)信号通路是人体中的重要信号通路,通过逐级磷酸化下游蛋白发挥作用。非小细胞肺癌(non-small cell lung cancer,NSCLC)中存在该信号通路的异常活化。活化的信号通路可以改变NSCLC细胞的增殖、凋亡、侵袭和迁移等生物学特性从而影响其对治疗药物的反应及预后。针对该通路抑制剂的研究很多,部分抑制剂已进入临床研究阶段。PI3K抑制剂包括广谱PI3K抑制剂、亚型特异性的PI3K抑制剂和PI3K/m TOR双重抑制剂。PI3K抑制剂单药有效率较低,但与化疗药物或其他靶向药物联用取得了不错的临床效果,目前往往将PIK3CA突变以及抑癌基因PTEN的缺失作为预测疗效的指标,但准确性欠佳,进一步筛选疗效预测指标是目前面临的重要问题。
[Abstract]:Phosphatidylinositol 3-kinase- PI3KN / protein kinase B(protein kinase / mammalian rapamycin target of rapamycin target of rapamycin tome signaling pathway is an important signal pathway in human body, which plays a role by step by step phosphorylation of downstream proteins.Abnormal activation of this signaling pathway exists in non-small cell lung cancer of non-small cell lung cancer (NSCLC).Activated signaling pathway can change the biological characteristics of NSCLC cells such as proliferation, apoptosis, invasion and migration, thus affecting its response to therapeutic drugs and prognosis.There have been many studies on the inhibitors of this pathway. Some of the inhibitors have entered the clinical research stage. PI3K inhibitors include broad-spectrum PI3K inhibitors, subtype-specific PI3K inhibitors and PI3K/m TOR dual inhibitors .PI3K inhibitors have a low effective rate.But the combination of chemotherapeutic drugs and other targeted drugs has achieved good clinical results. At present, the mutation of PIK3CA and the deletion of tumor suppressor gene PTEN are often used as predictors of therapeutic effect, but the accuracy is not good.It is an important problem to screen the prognostic index of curative effect.
【作者单位】：解放军济南军区总医院肿瘤科;
【分类号】：R734.2

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