期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 1, 页码 41-71出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm501026z
关键词
-
资金
- Ministry of Health
- University Hospital Hradec Kralove [00179906]
- Faculty of Military Health Sciences, University of Defence [SV/FVZ201402]
- Institutional Grant (Project RVO) [68378050]
- European Social Fund
- State Budget [CZ.1.07/2.3.00/30.0044]
- Lundbeck Foundation [R93-2011-8990] Funding Source: researchfish
- Novo Nordisk Fonden [NNF12OC0002290] Funding Source: researchfish
Phosphatidylinositol 3-kinases (PI3Ks) and phosphatidylinositol 3-kinase-related protein kinases (PIKKs) are two related families of kinases that play key roles in regulation of cell proliferation, metabolism, migration, survival, and responses to diverse stresses including DNA damage. To design novel efficient strategies for treatment of cancer and other diseases, these kinases have been extensively studied. Despite their different nature, these two kinase families have related origin and share very similar kinase domains. Therefore, chemical inhibitors of these kinases usually carry analogous structural motifs. The most common feature of these inhibitors is a critical hydrogen bond to morpholine oxygen, initially present in the early nonspecific PI3K and PIKK inhibitor 3 (LY294002), which served as a valuable chemical tool for development of many additional PI3K and PIKK inhibitors. While several PI3K pathway inhibitors have recently shown promising clinical responses, inhibitors of the DNA damage-related PIKKs remain thus far largely in preclinical development.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据