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目的：我们先前发现的一个新的氯乙基亚硝脲的类似物２氯乙基３肌氨酸酰胺１亚硝基脲（ＳａｒＣＮＵ） ，是一种通过单胺递质的神经元外转运蛋白（ＥＭＴ） 进入细胞内的选择性的细胞毒素。此药已进入Ｉ期临床试验。在本研究中，我们检测ＥＭＴ 在２３ 个人类肿瘤细胞系里的表达水平，以证实ＥＭＴ 的表达是否与ＳａｒＣＮＵ 的细胞毒性有关。方法：应用反转录多聚酶链反应（ＲＴＰＣＲ） 检测ＥＭＴ 在肿瘤细胞系的表达。同时也用蛋白质印迹技术检测ＤＮＡ 修复蛋白Ｏ６甲基鸟嘌呤ＤＮＡ 甲基转移酶（ ＭＧＭＴ） 和切除修复交叉互补鼠修复缺乏基因２（ＥＲＣＣ２） 。其结果与用硫酸若丹明Ｂ（ＳＲＢ） 抗癌药物比色筛选法检测的ＳａｒＣＮＵ 的细胞毒性相关。结果：几乎所有细胞系都呈ＥＭＴ 表达阳性，其中有５ 个细胞系（ ＭＧＲ１ ，ＭＧＲ２ ，Ｔ９８Ｇ，ＳＫ１，和ＧＢＭ） 呈低水平表达。虽然在ＳａｒＣＮＵ 细胞毒性和ＥＭＴ 表达水平之间没有显著性的线性关系， 但多因素回归分析显示ＳａｒＣＮＵ 细胞毒性与ＥＭＴ 加ＭＧＭＴ 及ＥＲＣＣ－ ２ 表达之间的相关性有显著意义。结论：本研结果示提示ＥＭＴ 和ＤＮＡ 修复因子ＭＧＭＴ、ＥＲＣＣ２ 是ＳａｒＣＮＵ 抗人
OBJECTIVE: A new chloroethylnitrosourea analog, 2-chloroethyl- 3 sarcosine amide 1 nitrosourea (SarCNU), which we previously discovered, is a monoamine transmitter Extracellular Extracellular Transporters (EMTs) Enter the Cell’s Selective Cytotoxins This drug has entered Phase I clinical trials. In this study, we examined the expression level of EMT in 23 human tumor cell lines to confirm whether the expression of EMT is related to the cytotoxicity of SarCNU. Methods: The expression of EMT in tumor cell lines was detected by reverse transcriptase polymerase chain reaction (RT-PCR). Western blotting was also used to detect DNA repair protein O6-methylguanine DNA methyltransferase (MGMT) and excision repair cross-complementation mouse repair deficiency gene 2 (ERCC2). The results were related to the cytotoxicity of SarCNU detected by colorimetric screening of rhodamine B (SRB) anticancer drugs. RESULTS: Almost all cell lines showed positive expression of EMT, among which five cell lines (MGR-1, MGR-2, T98-G, SK-1, and GBM) showed low levels of expression. Although there was no significant linear relationship between SarCNU cytotoxicity and EMT expression levels, multivariate regression analysis showed a significant correlation between SarCNU cytotoxicity and EMT plus MGMT and ERCC-2 expression. Conclusion: The results of this study suggest that EMT and DNA repair factors MGMT, ERCC2 are SarCNU anti-human