摘要
背景:磷酸肌醇3-激酶(PI3Ks)是细胞内脂质激酶的成员,参与细胞增殖,分化和存活的调节。已经报道了在各种形式的癌症中过表达PI3K / Akt / mTOR信号传导,尤其是在结肠直肠癌(CRC)中。由于它们在结肠直肠癌的起始和发展事件中的重要作用,它们被认为是引人注目的治疗靶标。 目的:本综述旨在详细介绍PI3K / Akt / mTOR通路在结直肠癌发生和发展过程中的作用及其在耐药中的作用。此外,还讨论了PI3K / Akt / mTOR抑制剂单独和与其他化学治疗药物组合在减轻结肠直肠癌中的作用。该综述包含临床前和临床证据以及天然和合成来源的途径抑制剂的专利文献。 方法:数据来自PubMed / Medline数据库,Scopus和Google专利文献。 结果:PI3K / Akt / mTOR信号通路是结直肠癌发生的重要事件。此外,它在获得CRC的耐药性和转移性起始事件中起重要作用。已经发现几种天然和合成来源的小分子通过有效地下调该途径而成为CRC的有效抑制剂。来自各种临床研究的数据也支持这些途径抑制剂,其中一些是专利的。 结论:PI3K / mTOR通路的抑制剂已经成功地用于治疗原发性和转移性结直肠癌,使该途径成为有希望的临床癌症治疗靶点。
关键词: 抗癌活性,转移,PI3K途径,天然产物,结肠癌,合成抑制剂。
图形摘要
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