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针对糖原合酶激酶 3 治疗淋巴瘤的研究进展。

Targeting glycogen synthase kinase 3 for therapeutic benefit in lymphoma.

机构信息

Division of Hematology, Department of Medicine.

Department of Molecular Medicine, and.

出版信息

Blood. 2019 Jul 25;134(4):363-373. doi: 10.1182/blood.2018874560. Epub 2019 May 17.

Abstract

Targeting the B-cell receptor and phosphatidylinositol 3-kinase/mTOR signaling pathways has shown meaningful, but incomplete, antitumor activity in lymphoma. Glycogen synthase kinase 3 (GSK3) α and β are 2 homologous and functionally overlapping serine/threonine kinases that phosphorylate multiple protein substrates in several key signaling pathways. To date, no agent targeting GSK3 has been approved for lymphoma therapy. We show that lymphoma cells abundantly express GSK3α and GSK3β compared with normal B and T lymphocytes at the messenger RNA and protein levels. Utilizing a new GSK3 inhibitor 9-ING-41 and by genetic deletion of GSK3α and GSK3β genes using CRISPR/CAS9 knockout, GSK3 was demonstrated to be functionally important to lymphoma cell growth and proliferation. GSK3β binds to centrosomes and microtubules, and lymphoma cells treated with 9-ING-41 become arrested in mitotic prophase, supporting the notion that GSK3β is necessary for the progression of mitosis. By analyzing recently published RNA sequencing data on 234 diffuse large B-cell lymphoma patients, we found that higher expression of GSK3α or GSK3β correlates well with shorter overall survival. These data provide rationale for testing GSK3 inhibitors in lymphoma patient trials.

摘要

针对 B 细胞受体和磷脂酰肌醇 3-激酶/哺乳动物雷帕霉素靶蛋白(mTOR)信号通路的治疗在淋巴瘤中显示出有意义但不完整的抗肿瘤活性。糖原合酶激酶 3(GSK3)α和β是 2 种同源且功能重叠的丝氨酸/苏氨酸激酶,可磷酸化多个关键信号通路中的多种蛋白底物。迄今为止,尚无靶向 GSK3 的药物被批准用于淋巴瘤治疗。我们发现,与正常 B 和 T 淋巴细胞相比,淋巴瘤细胞在信使 RNA 和蛋白质水平上大量表达 GSK3α和 GSK3β。利用新型 GSK3 抑制剂 9-ING-41 以及通过 CRISPR/CAS9 基因敲除技术敲除 GSK3α和 GSK3β 基因,证明 GSK3 对于淋巴瘤细胞的生长和增殖具有重要的功能作用。GSK3β 与中心体和微管结合,用 9-ING-41 处理的淋巴瘤细胞在有丝分裂前期停滞,这支持了 GSK3β 对于有丝分裂进程是必需的观点。通过分析最近发表的 234 例弥漫性大 B 细胞淋巴瘤患者的 RNA 测序数据,我们发现 GSK3α 或 GSK3β 的高表达与总生存期较短密切相关。这些数据为在淋巴瘤患者试验中测试 GSK3 抑制剂提供了依据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c8b/6659256/b51c1b2279b8/blood874560absf1.jpg

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