Wang Wenchao, Zhang Ying, Zhao Hong, Zhuang Xinlei, Wang Haoting, He Kaifeng, Xu Wanting, Kang Yu, Chen Shuqing, Zeng Su, Qian Linghui
Institute of Drug Metabolism and Pharmaceutical Analysis, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Cancer Center, Zhejiang University Hangzhou 310058 China
Hangzhou Institute of Innovative Medicine, Zhejiang University Hangzhou 310018 China.
Chem Sci. 2021 Sep 16;12(40):13477-13482. doi: 10.1039/d1sc03065e. eCollection 2021 Oct 20.
Cell-surface proteins, working as key agents in various diseases, are the targets for around 66% of approved human drugs. A general strategy to selectively detect these proteins in a real-time manner is expected to facilitate the development of new drugs and medical diagnoses. Although brilliant successes were attained using small-molecule probes, they could cover a narrow range of targets due to the lack of suitable ligands and some of them suffer from selectivity issues. We report herein an antibody-based fluorogenic probe prepared a two-step chemical modification under physiological conditions, to fulfill the selective recognition and wash-free imaging of membrane proteins, establishing a modular strategy with broad implications for biochemical research and for therapeutics.
细胞表面蛋白是多种疾病中的关键因子，约66%已获批的人类药物都以其为靶点。一种能够实时选择性检测这些蛋白的通用策略有望推动新药研发和医学诊断的发展。尽管使用小分子探针取得了显著成功，但由于缺乏合适的配体，它们所能覆盖的靶点范围较窄，而且其中一些还存在选择性问题。我们在此报告一种基于抗体的荧光探针，该探针在生理条件下通过两步化学修饰制备而成，用于实现膜蛋白的选择性识别和免洗成像，建立了一种对生化研究和治疗具有广泛意义的模块化策略。
