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Research Article

新型BCR-ABL/T315I酪氨酸激酶抑制剂的筛选及活性评价

卷 31, 期 20, 2024

发表于: 14 July, 2023

页: [2872 - 2894] 页: 23

弟呕挨: 10.2174/0929867330666230519105900

价格: $65

摘要

介绍：慢性髓系白血病(Chronic myeloid leukemia, CML)是一种由骨髓造血干细胞克隆增殖形成的恶性肿瘤。BCR-ABL融合蛋白存在于90%以上的患者中，是发现抗CML药物的重要靶点。迄今为止，伊马替尼是第一个被FDA批准用于治疗CML的BCR-ABL酪氨酸激酶抑制剂(TKI)。然而，出现耐药问题的原因是多方面的，尤其是BCR-ABL的“看门人”T135I突变。目前临床上还没有长期有效、低副作用的药物。 方法：本研究拟结合人工智能技术，结合细胞生长曲线、细胞毒性、流式细胞术和Western blot实验，寻找对T315I突变蛋白具有高抑制活性的靶向BCR-ABL的新型TKIs。 结果：所得化合物对白血病细胞有杀伤作用，对BaF3/T315I细胞有良好的抑制作用。化合物4可诱导细胞周期阻滞，引起细胞自噬和凋亡，抑制BCR-ABL酪氨酸激酶、STAT5和Crkl蛋白的磷酸化。 结论：结果表明，所筛选的化合物可作为先导化合物进行进一步研究，以发现理想的慢性髓性白血病治疗药物。

关键词: 慢性髓性白血病，BCR-ABL，酪氨酸激酶，T315I，抑制剂，虚拟筛选，化合物。

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