【作者】 郭士刚； 樊江莉； 王本花； 杜健军； 彭孝军；

【Author】 ShiGang Guo;BenHua Wang;JiangLi Fan;Jianjun Du;Xiaojun Peng;State Key Laboratory of Fine Chemicals,Dalian University of Technology;

【机构】 精细化工国家重点实验室大连理工大学；

【摘要】 靶向到癌细胞中异常表达酶的高选择,高灵敏性荧光探针的不断发展,可以更好地将其应用于癌症诊断,内窥镜以及手术治疗^[1]。原癌蛋白Pim-1激酶在侵略性癌细胞中过量表达,并且研究表明,Pim-1激酶为优异的癌症生物标志物^[2]。因此,本文报道一例靶向到Pim-1激酶,可应用于癌症细胞选择性成像的近红外荧光探针NBP。NBP在正常细胞中只表现出微弱的荧光响应,而在Pim-1激酶过量表达的癌细胞中表现出强烈的荧光响应。当使用Pim-1激酶的高效抑制剂5-溴苯并呋喃-2-羧酸^[3]提前孵育细胞,进行竞争性实验发现,荧光信号强度明显降低,这也证实NBP为Pim-1激酶特异性探针。NBP选择性的标记癌细胞获得荧光信号,具有作为分子荧光工具应用在癌症诊断和荧光手术术中成像的巨大潜能。更多还原

【Abstract】 The continuous development of enzyme-active probes that can yield highly sensitive and selective reporting species associated with cancer cells will allow to be employed in cancer detection,endoscopy and surgery^[1].Pim-1expression is correlated with tumour aggressiveness and is emerging as a biomarker for cancers^[2].Then,we report a novel Pim-1-targeted near-infrared probe（NBP） for cancer cells imaging.The probe’s fluorescence is weak in normal cells,while it emits strong fluorescence in cancer cells that Pim-1 is over-expressed.When pre-treated excess of 5-bromobenzofuran-2-carboxylic acid^[3],a powerful inhibitor of Pim-1,the intensity of fluorescence decreased significantly,indicating that NBP response to Pim-1 specifically.NBP appears to be a promising molecular tool that may have great potential application in early diagnostic imaging and fluorescence-assisted surgical resection.更多还原