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PI3K信号通路抑制剂研究进展
The Research Progress of PI3K Inhibitors

DOI: 10.12677/HJMCe.2020.83007, PP. 51-65

Keywords: PI3K信号通路抑制剂,结构类型,靶点,研究进展
PI3K Signaling Pathway Inhibitors
, Structural, Targets, Research Progress

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Abstract:

PI3K信号通路是指PI3K/AKT/mTOR信号通路。在本篇综述中,详细介绍了PI3K信号通路抑制剂的不同分类,PI3K信号通路抑制剂与其活性位点的结合模式,以及PI3K抑制剂的研究进展,揭示了PI3K抑制剂的构效关系和设计思路,以期找到活性高、选择性好、副作用小的药物,为癌症治疗带来希望。PI3K信号通路在人类发育过程中起着重要作用,与多种肿瘤的发生发展密切相关。在PI3K信号通路的不同治疗方法中,小分子PI3K抑制剂在分子靶向抗肿瘤方面具有很大的潜力治疗。目前已知的PI3K抑制剂主要有Copanlisib、Idelalisib Dactolisib、Omipalisib等。
PI3K signaling pathway refers to the PI3K/AKT/mTOR signaling pathway. In this review, we briefly summarized the classification of PI3K inhibitors, and the interaction between PI3K inhibitors and PI3K active sites. We also introduced the research progress of PI3K inhibitors in detail, and then revealed the structure-activity relationship and design ideas of PI3K inhibitors in order to find drugs with high activity, good selectivity and small side effects, and bring hope for the cancer ther-apy. PI3K signaling pathway plays an important role in human development and is closely related to the occurrence and development of a variety of tumors. In different treatment methods for PI3K signaling pathway, small molecule PI3K inhibitors have great potential in molecular targeted an-ti-tumor treatment. Currently, the main known PI3K inhibitors are Copanlisib, Idelalisib Dactolisib, Omipalisib, etc.

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