2024-11-21 21:21:40

akt的抑制剂有很多种,该怎样选择?

我现在做的是小胶质细胞,要做akt信号通路,但现在查到akt抑制剂有很多种,应该怎样选择?谢谢。


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生物化学× 凋亡坏死与自噬×

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一般来说某个靶点抑制剂的研究也是不断进展的,随着化工技术和计算机模拟分析模拟技术进步,许多靶点上新的抑制剂都比早期的更为有效、更加具有特异性,水溶解性更好、性质更稳定等优点。除了靶点的活性外,其毒性也是决定它是否现在应用于动物体内实验,将来应用于临床成功与否的关键。如NF-kB抑制剂、AKT抑制剂等都是如此。对于你的困惑,其实并不难解决,查找资料和文献上近年来在神经科研究所用的AKT抑制剂有哪些,自己做一总结,一般是参考较高IF上发表的杂志,选择研究用的较多的、溶解性较好的某种新近药物。同时,需要注意总结同一类疾病模型研究中,其他研究者常用的给药方式、给药剂量等信息。


2024-11-21 21:50:49

现在比较常用的有两种,可以用AZD235或BEZ8055。


2024-11-21 21:56:34

可以用于小胶质细胞的有:MK-2206;AT7867;CCT128930; 

已经用于临床试验的有MK-2206
现给大家介绍一下主要的AKT抑制剂:
MK-2206:a highly selective, potent non-ATP competitive allosteric Akt inhibitor with IC50 of 8 nM,12 nM, 65 mM for Akt1, Akt2 and Akt3 respectively;
The phase II clinical trials of MK-2206 against the treatment of endometrial cancer are recruiting participant Dana-Farber Cancer Institute.
Perifosine:A p.o.-bioavailable ALK(Alkylphospholipids),inhibits Akt activation。

AT7867 is a potent and oral AKT and p70 S6 kinase inhibitor with an IC50 of 17 nM.
GSK690693:selective for the Akt isoforms(inhibits Akt kinases 1, 2, and 3 with IC50 values of 2, 13, and 9 nM respectively)。
PHT-427:inhibited Akt and PDPK1 signaling and their downstream targets.
CCT128930:a novel potent ATP-competitive, AKT inhibitor with an IC50 of 6 nM.
Palomid 529 (P529) a novel potent antitumour PI3K/Akt/mTOR inhibitor with a GI50 of <35 μM in the NCI-60 cell lines panel.
Triciribine phosphate (NSC-280594):prevents the phosphorylation of Akt.
A-674563: a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.
Triciribine: selectively inhibits the phosphorylation and activation of Akt1, -2 and -3.


2024-11-21 21:57:29

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