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首页> 外文期刊>The Journal of Antibiotics: An International Journal >A guanine derivative as a new MEK inhibitor produced by Streptomyces sp MK63-43F2
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A guanine derivative as a new MEK inhibitor produced by Streptomyces sp MK63-43F2

机译：鸟嘌呤衍生物作为由Streptomyces SP MK63-43F2产生的新MEK抑制剂

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Mitogen-activated protein kinase ( MAPK) pathways that direct cellular responses are involved in various biological processes; the RAS-RAF-MEK-ERK pathway is one of the most important MAPK pathways. It is frequently activated in human malignant tumors such as melanomas, thyroid tumors and colorectal carcinomas. Therefore, targeting this pathway has been considered an attractive strategy for new anticancer drugs. In particular, MEK is a promising target because it is a kinase that directly phosphorylates ERK. We performed a screening to discover new MEK inhibitors, and found a guanine derivative produced by Streptomyces sp. MK63-43F2. This guanine derivative was identified to be 2-amino-4-methoxy-5-cyanopyrrolo[2,3-d] pyrimidine (1) through spectroscopic analysis. Compound 1 inhibited MEK1 kinase activity in an ATP-dependent manner and suppressed the phosphorylation of ERK in cancer cells and cell proliferation. Therefore, 1 might be a potent lead compound for new MEK inhibitors.
机译：直接细胞反应参与各种生物过程的丝裂原激活蛋白激酶（MAPK）途径; RAS-RAF-MEK-ERK途径是最重要的MAPK途径之一。 它经常在人体恶性肿瘤中被激活，如黑色素瘤，甲状腺肿瘤和结肠直肠癌。 因此，靶向该途径已被认为是新的抗癌药物的有吸引力的策略。 特别是Mek是一个有希望的目标，因为它是直接磷酸化ERK的激酶。 我们进行了筛选以发现新的MEK抑制剂，并发现由Streptomyces SP产生的鸟嘌呤衍生物。 MK63-43F2。 通过光谱分析，将这种鸟嘌呤衍生物鉴定为2-氨基-4-甲氧基-5-氰基吡咯并[2,3-D]嘧啶（1）。 化合物1以ATP依赖性方式抑制MEK1激酶活性，并抑制了癌细胞中ERK的磷酸化和细胞增殖。 因此，1可能是新MEK抑制剂的有效铅化合物。

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