典型文献
Targeting PP2A for cancer therapeutic modulation
文献摘要：
Protein phosphatases play essential roles as negative regulators of kinases and signaling cascades involved in cytoskeletal organization. Protein phosphatase 2A (PP2A) is highly conserved and is the predominant serine/threonine phosphatase in the nervous system, constituting more than 70％ of all neuronal phosphatases. PP2A is involved in diverse regulatory functions, including cell cycle progression, apoptosis, and DNA repair. Although PP2A has historically been identified as a tumor suppressor, inhibition of PP2A has paradoxically demonstrated potential as a therapeutic target for various cancers. LB100, a water-soluble, small-molecule competitive inhibitor of PP2A, has shown particular promise as a chemo- and radio-sensitizing agent. Preclinical success has led to a profusion of clinical trials on LB100 adjuvant therapies, including a phase Ⅰ trial in extensive-stage small-cell lung cancer, a phase Ⅰ/Ⅱ trial in myelodysplastic syndrome, a phase Ⅱ trial in recurrent glioblastoma, and a completed phase Ⅰ trial assessing the safety of LB100 and docetaxel in various relapsed solid tumors. Herein, we review the development of LB100, the role of PP2A in cancer biology, and recent advances in targeting PP2A inhibition in immunotherapy.
文献关键词：
中图分类号：
作者姓名：
Halle Ronk;Jared S.Rosenblum;Timothy Kung;Zhengping Zhuang
作者机构：
Neuro-Oncology Branch,National Cancer Institute,National Institutes of Health,Bethesda,MD 20892,USA
文献出处：
引用格式：
[1]Halle Ronk;Jared S.Rosenblum;Timothy Kung;Zhengping Zhuang-.Targeting PP2A for cancer therapeutic modulation)[J].癌症生物学与医学（英文版）,2022(10):1428-1439
A类：
paradoxically,LB100,profusion
B类：
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AB值：
0.576627
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