Akt激酶小分子抑制剂研究进展——ATP竞争性抑制剂研究概述
Research Progress of Small Molecule Inhibitors of Akt Kinase—Overview of ATP Competitive Inhibitor Research
摘要: PI3K-Akt-mTOR信号通路是调节细胞周期活动的重要通路之一，该通路的失调是导致肿瘤产生的原因之一。目前以Akt为靶点的小分子抑制剂已经成为抗肿瘤药物研发的思路之一，在近二十年中，研究人员通过高通量筛选及计算机辅助药物设计等方法，设计、优化并合成了大量有选择性和高活性的Akt小分子抑制剂，本文对近年来文献所报道的ATP竞争性抑制剂按照其结构类型进行综述。
Abstract: The PI3K-Akt-mTOR signaling pathway is one of the important pathways that regulate cell cycle ac-tivities, and the imbalance of this pathway is one of the causes of tumors. Small molecule inhibitors targeting Akt have become one of the ideas for the development of anti-tumor drugs. In the past two decades, researchers have designed, optimized and synthesized a large number of selective and highly active Akt small molecule inhibitors through high-throughput screening and computer-aided drug design. This article reviews the ATP-competitive inhibitors reported in the literature in recent years according to their structure types.
文章引用：王彦凯, 黎文海. Akt激酶小分子抑制剂研究进展——ATP竞争性抑制剂研究概述[J]. 有机化学研究, 2021, 9(2): 13-21. https://doi.org/10.12677/JOCR.2021.92003

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