摘要
多发性的骨髓瘤是第二大恶性血液肿瘤,在所有血癌患者中超过10%,并且在每年由癌症引起的死亡中2%是由该疾病引起的,主要的原因就是缺乏有效的治疗药物。急需开发新颖的、分子靶向的抗多发性的骨髓瘤药物。(PLSK)/AKT信号传导通路控制多发性骨髓癌的发病病理中起到十分重要的作用,包括存活、增殖、迁移、血管再生以及抗药性,并且已被当做重要的药物作用靶标。诸多以该信号通道为靶标的强效的抑制剂被开发出来,其中一部分已经发展到临床评价阶段。在这篇综述中,我们强调了PI3K/AKT信号通路在多发性的骨髓瘤的发病机制中的作用,和当前的此类抑制剂的药物研究进展,并对基于PI3K/AKT的抑制剂的发掘策略进行了讨论。
关键词: 蛋白激酶,新药研发,雷帕霉素靶蛋白,多发性骨髓瘤,磷脂酰肌醇(-3)激酶
Current Medicinal Chemistry
Title:Targeting the Phosphatidylinositol 3-Kinase/AKT Pathway for the Treatment of Multiple Myeloma
Volume: 21 Issue: 27
Author(s): J. Zhu, M. Wang, B. Cao, T. Hou and X. Mao
Affiliation:
关键词: 蛋白激酶,新药研发,雷帕霉素靶蛋白,多发性骨髓瘤,磷脂酰肌醇(-3)激酶
摘要: Multiple myeloma is the second most hematological malignancy, accounting for more than 10% of all blood cancers and 2% of annual cancer-related deaths due to lack of curable drugs. Novel and molecularly targeted anti-MM drugs are in urgent need. The phosphatidylinositol 3-kinase (PI3K)/AKT signaling pathway plays a critical regulatory role in multiple myeloma pathophysiology, including survival, proliferation, migration, angiogenesis, as well as drug resistance, and has emerged as a key therapeutic target. Many potent inhibitors targeting this pathway have been developed and some have been moved for clinical evaluations for multiple myeloma. In this review, we highlighted the role of the PI3K/AKT pathway in the pathogenesis of multiple myeloma, and current advances in drug discovery for this class of inhibitors. Discovery strategies toward the PI3K/AKT inhibitors were also discussed.
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Cite this article as:
Zhu J., Wang M., Cao B., Hou T. and Mao X., Targeting the Phosphatidylinositol 3-Kinase/AKT Pathway for the Treatment of Multiple Myeloma, Current Medicinal Chemistry 2014; 21 (27) . https://dx.doi.org/10.2174/0929867321666140601204513
DOI https://dx.doi.org/10.2174/0929867321666140601204513 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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