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| BCR-ABL变构抑制剂阿西米尼及其类似物的研究进展 |
| Research Progress on BCR-ABL Allostery Inhibitor Asciminib and Its Analogues |
| 投稿时间：2025-03-04 修订日期：2025-04-09 |
| DOI： |
| 中文关键词: 慢性粒细胞白血病 阿西米尼 BCR-ABL变构抑制剂 类似物 肉豆蔻酰口袋 |
| 英文关键词:Chronic myeloid leukemia Asciminib BCR-ABL allosteric inhibitor Analogues Myristoyl pocket |
| 基金项目:辽宁省教育厅项目(LQ2020021) |
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| 中文摘要: |
| 小分子BCR-ABL1酪氨酸激酶抑制剂（Tyrosine kinase inhibitors，TKIs)的开发降低了慢性粒细胞白血病（chronic myeloid leukemia, CML）患者的死亡率，但在治疗过程中可能会产生毒性、耐药性。第一个进入临床的肉豆蔻酰口袋变构抑制剂阿西米尼在克服BCR-ABL1酪氨酸激酶抑制剂的耐药性及脱靶效应发挥作用，为CML患者治疗带来选择和希望。本文通过检索CNKI、PubMed、Web of Science等数据库，介绍了阿西米尼的设计、构效关系和耐药性，并对近年来以阿西米尼为先导结构进行结构修饰的工作进行简要归纳，以期为开发新的BCR-ABL抑制剂提供参考。 |
| 英文摘要: |
| Although small molecule BCR-ABL1 tyrosine kinase inhibitors (TKIs) have reduced the mortality of patients with chronic myeloid leukemia (CML), adverse toxicity, drug resistance and off target effect may occur in the process of treatment. Asciminib, the first myristoyl pocket allosteric inhibitor to enter the clinic, has played an important role in overcoming drug resistance and off-target effects, offering choice and hope for the treatment of CML patients. In this paper, we searched CNKI, PubMed, Web of science and other databases, introduced the design, structure-activity relationship and drug resistance of Asciminib. In addition, briefly summarized the work of structural modification with Asciminib as the leading structure in recent years. The review article is expected to provide reference for the development of new BCR-ABL inhibitors. |
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