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基于扭曲分子内电荷转移(TICT)的荧光探针的设计、合成及对蛋白质 HSA 的点亮作用的机理研究。

Design, synthesis and mechanistic studies of a TICT based fluorogenic probe for lighting up protein HSA.

机构信息

School of Pharmacy, Jiangsu University, Zhenjiang 212013, PR China.

School of Pharmacy, Jiangsu University, Zhenjiang 212013, PR China.

出版信息

Bioorg Med Chem Lett. 2021 Dec 1;53:128438. doi: 10.1016/j.bmcl.2021.128438. Epub 2021 Nov 2.

DOI:10.1016/j.bmcl.2021.128438
PMID:34740774
Abstract

Human serum albumin (HSA) in blood serves as an important biomarker for clinical diagnosis, and fluorescence sensing method has attracted extensive attention. In this work, a small organic molecule probe, YS8, involving twisted intramolecular charge transfer (TICT) characteristic, was designed and investigated to detect HSA. YS8 kept silent state in fluorescence under physiological conditions, but the encapsulation of YS8 in the hydrophobic subdomain IB region of HSA inhibited the TICT state and produced a clear light-up fluorescent signal. Especially, YS8 was demonstrated to be an efficient fluorogenic probe to discriminate HSA from other proteins including the bovine serum albumin (BSA). Moreover, YS8/HSA complex could be applied in fluorescence imaging in living cells and is also useful in the study of artificial fluorescent protein (AFP).

摘要

血液中的人血清白蛋白(HSA)是临床诊断的重要生物标志物,荧光传感方法受到了广泛关注。在这项工作中,设计并研究了一种小分子探针 YS8,它涉及扭曲的分子内电荷转移(TICT)特性,用于检测 HSA。YS8 在生理条件下保持荧光沉默状态,但 YS8 被包埋在 HSA 的疏水亚结构域 IB 区域中,抑制了 TICT 状态并产生了清晰的点亮荧光信号。特别是,YS8 被证明是一种有效的荧光探针,可将 HSA 与其他蛋白质(包括牛血清白蛋白(BSA))区分开来。此外,YS8/HSA 复合物可用于活细胞中的荧光成像,并且在人工荧光蛋白(AFP)的研究中也很有用。

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