Class I phosphatidylinositol 3-kinase inhibitors for cancer therapy

来源 :Acta Pharmaceutica Sinica B | 被引量 : 0次 | 上传用户:ludongyan900209
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
The phosphatidylinositol 3-kinase(PI3K) pathway is frequently activated in human cancers.Class I PI3 Ks are lipid kinases that phosphorylate phosphatidylinositol 4,5-bisphosphate(PIP2) at the 3-OH of the inositol ring to generate phosphatidylinositol 3,4,5-trisphosphate(PIP3), which in turn activates Akt and the downstream effectors like mammalian target of rapamycin(m TOR) to play key roles in carcinogenesis. Therefore, PI3 K has become an important anticancer drug target, and currently there is very high interest in the pharmaceutical development of PI3 K inhibitors. Idelalisib has been approved in USA and Europe as the first-in-class PI3 K inhibitor for cancer therapy. Dozens of other PI3 K inhibitors including BKM120 and ZSTK474 are being evaluated in clinical trials. Multifaceted studies on these PI3 K inhibitors are being performed, such as single and combinational efficacy, resistance, biomarkers,etc. This review provides an introduction to PI3 K and summarizes key advances in the development of PI3 K inhibitors. The phosphatidylinositol 3-kinase (PI3K) pathway is frequently activated in human cancers. Class I PI3 Ks are lipid kinases that phosphorylate phosphatidylinositol 4,5-bisphosphate (PIP2) at the 3-OH of the inositol ring to generate phosphatidylinositol 3,4, 5-trisphosphate (PIP3), which in turn activates Akt and the downstream effectors like mammalian target of rapamycin (m TOR) to play key roles in carcinogenesis. Thus, PI3 K has become an important anticancer drug target, and currently there is very high interest in the pharmaceutical development of PI3 K inhibitors. Idelalisib has been approved in USA and Europe as the first-in-class PI3 K inhibitor for cancer therapy. Dozens of other PI3 K inhibitors including BKM120 and ZSTK474 are being evaluated in clinical trials. Multifaceted studies on these PI3 K inhibitors are being performed, such as single and combinational efficacy, resistance, biomarkers, etc. This review provides an introduction to PI3 K and summarizes key advances in t he development of PI3 K inhibitors.
其他文献
自《现代营销》、《大众投资》、《致富时代》等媒体报道韩典庆老师研发人体塑像和变形娃娃的创业事迹后,从2005年9月至今已有众多人靠此技术走上了致富路,此项目投资小,见效
课堂小结是教师在课堂教学结束时对所教内容进行针对性的回顾、整理、归纳、深化。它既是对教学内容的再现,又是对课堂内容的高度提炼、精要概括和系统整理,对整节课的教学内
近几年来,随着文艺事业的繁荣和发展,上海很多剧场、影院开辟了“观众园地”。这块“园地”最直接和广大观众见面,对观众有着很大的吸引力。很多观众是先看了“观众园地”的
开放教育法学专业是一门实践性应用性很强的学科,它需要理论联系实际的教学方法。在适应开放教育人才培养模式的需要,探索新的教学方法时,开放教育法学专业的案例教学法,以其
铜陵省黄梅戏剧团是个老团,三十多年来为黄梅戏事业做过一些贡献。可是,十年动乱给剧团造成了青黄不接、后继乏人的严重后果。县委根据黄梅戏事业发展的需要和剧团的现状,决
企业概述》北京资源勘查分公司是中煤地质工程总公司从事固体和气体矿产地质勘查、水工环地质勘查、物探测井的直属专业分公司。该公司工程技术力量雄厚,拥有众多各类高、中
翁牛特旗广德公乡郝家窝铺村农民康富,从1981年开始承包350亩荒山、荒沟,搞小流域治理,治山闸沟,植树种草,已得收益,在贫困山区开始走上了致富道路。1981年全家人均收入达到
从经济发展的现实看,人们讲求经济效果而且愈来愈重视提高经济效果,已在生产实践中取得了可喜成果。本讲拟就什么是经济效果,以及评价林业生产经济效果的指标体系等问题,谈一
生物教学作为初中阶段的一门课程之一,对学生了解自然常识、生命奥秘等起着十分重要的作用.发散思维是创造性思维的核心,也是提高学生创造力的基础,在生物学科中培养发散思维
鸡西矿业集团公司张辰煤矿西三采区3
期刊