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一个BTK可激活的向共价NIR光探针用于酶监测和B细胞淋巴瘤成像

Xinyue Zhao¹, Yuxin Gu¹, Yingyan Xie¹

¹Department of Chemistry and the MOE Key Laboratory of Spectrochemical Analysis & Instrumentation, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, 361005, China.

Biosensors & bioelectronics

|August 15, 2025

概括

研究人员开发了一种新的近红外光 (NIRF) 探测器Ibt-CyOH,用于监测活细胞中的布鲁顿氨酸激酶 (BTK). 这种探针可以实时成像B细胞淋巴瘤和BTK抑制,帮助诊断和治疗.

科学领域:

生物化学生物化学
分子生物学分子生物学
医疗成像医学成像

背景情况:

B细胞淋巴瘤是一种侵袭性的恶性瘤.
布鲁顿的氨酸激酶 (BTK) 是B细胞淋巴瘤治疗的关键标.
监测活细胞中的BTK表达和活性对于诊断和治疗至关重要.

研究的目的:

开发一种分子探针,用于对活细胞中BTK表达和活性进行定量监测.
为B细胞淋巴瘤成像创建一个向的共价近红外光 (NIRF) 探针.

主要方法:

使用ibrutinib作为向配体,构建一个BTK可激活的NIRF探针 (Ibt-CyOH).
包括一个NIRF报告员和一个α-甲基化烯胺可切割链接器.
评估探针选择性,抑制性和实时成像能力的 in vitro 和 in vivo.

主要成果:

Ibt-CyOH对BTK具有很高的选择性和抑制作用.
在对BTK进行共价结合时,观察到显著的"启动"NIR光信号.
在活小鼠中实现了B细胞淋巴瘤细胞的实时成像和BTK抑制.

结论:

这项研究为分子探针提供了一个有前途的向共价激活策略.
Ibt-CyOH作为一种新的向共价NIR探针,用于体内BTK成像.
这种方法可以有利于B细胞恶性瘤的诊断和治疗,并激发未来NIRF探针的开发.

关键词:

在B细胞淋巴瘤.布鲁顿的氨酸激酶是布鲁顿的氨酸激酶.癌症成像成像癌症成像光发射探测器进行光.有针对性的共价抑制剂.

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