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AKT in cancer: new molecular insights and advances in drug development

机译:AKT在癌症中:药物开发的新分子见解和进步

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The phosphatidylinositol-3 kinase (PI3K)-AKT pathway is one of the most commonly dysregulated pathways in all of cancer, with somatic mutations, copy number alterations, aberrant epigenetic regulation and increased expression in a number of cancers. The carefully maintained homeostatic balance of cell division and growth on one hand, and programmed cell death on the other, is universally disturbed in tumorigenesis, and downstream effectors of the PI3K-AKT pathway play an important role in this disturbance. With a wide array of downstream effectors involved in cell survival and proliferation, the well-characterized direct interactions of AKT make it a highly attractive yet elusive target for cancer therapy. Here, we review the salient features of this pathway, evidence of its role in promoting tumorigenesis and recent progress in the development of therapeutic agents that target AKT.
机译:磷脂酰肌醇-3激酶(PI3K)-AKT途径是所有癌症中最常见的疑难生的途径之一,具有体细胞突变,复制数改变,异常表观遗传调控和增加的许多癌症的表达增加。 一方面仔细维持细胞分裂和生长的稳重平衡,另一方面的细胞死亡,在肿瘤发生中普遍不安,PI3K-AKT途径的下游效应在这种干扰中起重要作用。 涉及细胞存活和增殖的各种下游效应,AKT的良好表征直接相互作用使其成为癌症治疗的高度吸引力但难以捉摸的靶点。 在这里,我们审查了该途径的显着特征,证明其在促进肿瘤发生以及近期靶向Akt的治疗剂的进展方面的作用。

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