EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73122_C
mTOR通路抑制剂；抑制FKBP-12
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总览
依维莫司是一种哺乳动物雷帕霉素靶蛋白（mTOR）抑制剂。它是一种羟乙基醚取代的雷帕霉素衍生物，具有更优的药代动力学和药效学性质。它通过结合FK506结合蛋白（FKBP-12）结合，随后该复合物与 mTOR 结合，从而抑制 mTORC1 和 mTORC2 复合物，导致复合物不稳定并阻断激酶功能(Zeng等人；Lebwohl等人；Sedrani等人；Huang & Houghton)。
癌症研究
·在体外和体内模型中，抑制多种癌症中的细胞增殖、代谢和血管生成（Zhu等人；Lane等人；O 'Reilly等人；Lebwohl等人)。
免疫学
·在器官移植背景下，Everolimus 可作为免疫抑制剂使用（Lebwohl 等人；Wullschleger 等人）。
细胞类型
癌细胞及细胞系
种属
人，小鼠，非人灵长类，其他物种，大鼠
研究领域
癌症，免疫，移植研究
CAS 编号
159351-69-6
化学式
C₅₃H₈₃NO₁₄
纯度
≥ 95 %
通路
mTOR
靶点
FKBP-12
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
相关材料与文献
技术资料 (3)
文献 (7)
Targeting mTOR signaling for cancer therapy.
Current opinion in pharmacology 2003 AUG
Abstract
The mammalian target of rapamycin (mTOR),an atypical serine/threonine kinase,plays a central role in the regulation of cell proliferation,growth,differentiation,migration and survival. Dysregulation of mTOR signaling occurs in diverse human tumours,and can confer higher susceptibility to inhibitors of mTOR. Rapamycin and its derivatives,CCI-779 and RAD001 (designated rapamycins),specifically inhibit the function of mTOR,leading to inactivation of ribosomal S6K1 and inhibition of cap-dependent translation initiation through the 4E-BP1/eIF4E pathway. The overall effect is an accumulation of cells in the G1 phase of the cell-cycle,and potential apoptosis. Preclinical studies indicate that rapamycins are potent inhibitors of the proliferation of numerous tumour cell lines in culture and of murine syngeneic tumour models or human xenografts. RAD001 and CCI-779 are in phase I and II trials,respectively,as anti-cancer agents. These trials have demonstrated promising anti-cancer activity and relatively mild side effects of CCI-779. Emerging results suggest that inhibition of mTOR signaling can be exploited as a potential tumour-selective therapeutic strategy.
TOR signaling in growth and metabolism.
Cell 2006
Abstract
The target of rapamycin (TOR) is a conserved Ser/Thr kinase that regulates cell growth and metabolism in response to environmental cues. Here,highlighting contributions from studies in model organisms,we review mammalian TOR complexes and the signaling branches they mediate. TOR is part of two distinct multiprotein complexes,TOR complex 1 (TORC1),which is sensitive to rapamycin,and TORC2,which is not. The physiological consequences of mammalian TORC1 dysregulation suggest that inhibitors of mammalian TOR may be useful in the treatment of cancer,cardiovascular disease,autoimmunity,and metabolic disorders.
Rapamycin derivatives reduce mTORC2 signaling and inhibit AKT activation in AML.
Blood 2007
Abstract
The mTOR complex 2 (mTORC2) containing mTOR and rictor is thought to be rapamycin insensitive and was recently shown to regulate the prosurvival kinase AKT by phosphorylation on Ser473. We investigated the molecular effects of mTOR inhibition by the rapamycin derivatives (RDs) temsirolimus (CCI-779) and everolimus (RAD001) in acute myeloid leukemia (AML) cells. Unexpectedly,RDs not only inhibited the mTOR complex 1 (mTORC1) containing mTOR and raptor with decreased p70S6K,4EPB1 phosphorylation,and GLUT1 mRNA,but also blocked AKT activation via inhibition of mTORC2 formation. This resulted in suppression of phosphorylation of the direct AKT substrate FKHR and decreased transcription of D-cyclins in AML cells. Similar observations were made in samples from patients with hematologic malignancies who received RDs in clinical studies. Our study provides the first evidence that rapamycin derivatives inhibit AKT signaling in primary AML cells both in vitro and in vivo,and supports the therapeutic potential of mTOR inhibition strategies in leukemias.
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | 159351-69-6 |
| Chemical Formula | C₅₃H₈₃NO₁₄ |
| 纯度 | ≥ 95 % |
| Target | FKBP-12 |
| Pathway | mTOR |
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