AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway-Mutant Cancers with Wild-Type KRAS and BRAF by Destabilizing Aurora Kinase B

AKT 降解通过破坏 Aurora 激酶 B 的稳定性选择性抑制具有野生型 KRAS 和 BRAF 的 PI3K/PTEN 通路突变癌症的生长

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作者:Jia Xu #, Xufen Yu #, Tiphaine C Martin, Ankita Bansal, Kakit Cheung, Abigail Lubin, Elias Stratikopoulos, Kaitlyn M Cahuzac, Li Wang, Ling Xie, Royce Zhou, Yudao Shen, Xuewei Wu, Shen Yao, Ruifang Qiao, Poulikos I Poulikakos, Xian Chen, Jing Liu, Jian Jin, Ramon Parsons

Significance

MS21 depletes cells of phosphorylated AKT (pAKT) and a newly identified AKT substrate, AURKB, to inhibit tumor growth in mice. MS21 is superior to prior agents that target PI3K and AKT due to its ability to selectively target active, pAKT and sustain repression of signaling to deplete AURKB. This article is highlighted in the In This Issue feature, p. 2945.

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