哺乳动物西罗莫司靶蛋白抑制剂依维莫司抗肿瘤作用的研究进展

Adrencer in research of antitumor efficacy of mammalian target of sirolimus inhibitor everolimus

哺乳动物西罗莫司靶蛋白（mTOR）是一种丝氨酸／苏氨酸蛋白激酶，广泛存在于细胞内，已被证实为肿瘤治疗的一个可靠靶点。依维莫司是一种口服mTOR抑制剂，是雷帕霉素衍生物中的一种，其改善了既往雷帕霉素药物特性，主要抑制哺乳动物肿瘤细胞生长和分化有关的mTOR。2009年3月，依维莫司被美国食品药品监督局（FDA）批准用于治疗晚期肾癌。目前其在乳腺癌、肺癌、胃癌等多种肿瘤中应用的临床研究也取得了一定的进展。

Mammalian target of sirolimus （roTOR） is a serine / threonine protein kinase, it widely expresses in cells and has been indicated as a reliable target for tumor treatment. Everolimus, a rapamyein derivative is an oral roTOR inhibitor. It improves the drug properties of rapamycin, and inhibits mammalian tumor cell growth and differentiation. In March 2009, everolimus was approved for the treatment of advanced renal cell carcinoma by US Food and Drug Addministration. At present, some clinical research advances on antitumor efficacy of everolimus in breast cancer, lung cancer, gastric cancer and other tumors have been proceeded.