药学实践杂志
藥學實踐雜誌
약학실천잡지
THE JOURNAL OF PHARMACEUTICAL PRACTICE
2014年
5期
332-336,359
,共6页
陈颖%韩进松%王重庆%宋云龙%周永刚%朱驹
陳穎%韓進鬆%王重慶%宋雲龍%週永剛%硃駒
진영%한진송%왕중경%송운룡%주영강%주구
磷脂酰肌醇3激酶-哺乳动物雷帕霉素靶蛋白%双重抑制剂%小分子%抗肿瘤
燐脂酰肌醇3激酶-哺乳動物雷帕黴素靶蛋白%雙重抑製劑%小分子%抗腫瘤
린지선기순3격매-포유동물뢰파매소파단백%쌍중억제제%소분자%항종류
PI3K-mTOR%dual inhibitors%small molecules%anticancer
PI3 K脂激酶家族介导的细胞信号转导通路,调节细胞增殖、分化、凋亡等一系列活动,已经成为治疗肿瘤、炎症等疾病的重要靶标。近来出现了多种结构类型的该通路抑制剂,笔者总结了近年内进入临床研究的具有PI3K-mTOR双重抑制活性的小分子化合物。
PI3 K脂激酶傢族介導的細胞信號轉導通路,調節細胞增殖、分化、凋亡等一繫列活動,已經成為治療腫瘤、炎癥等疾病的重要靶標。近來齣現瞭多種結構類型的該通路抑製劑,筆者總結瞭近年內進入臨床研究的具有PI3K-mTOR雙重抑製活性的小分子化閤物。
PI3 K지격매가족개도적세포신호전도통로,조절세포증식、분화、조망등일계렬활동,이경성위치료종류、염증등질병적중요파표。근래출현료다충결구류형적해통로억제제,필자총결료근년내진입림상연구적구유PI3K-mTOR쌍중억제활성적소분자화합물。
Objective The phosphoinositide 3-kinase (PI3K) constituted an important family of lipid kinase enzymes that control a range of cellular proliferation , differentiation and apoptosis through their regulation of a network of signal transduction path -ways, which had emerged as important therapeutic targets in the context of cancer and inflammation .Considerable progress had been made in the discovery and development of small molecular inhibitors targeting PI 3K.Progress in dual PI3K-mTOR inhibitors, a number of which had entered early phase clinical trials over recent years was summarized .