Bispecific Aptamer Induced Artificial Protein-Pairing: A Strategy for Selective Inhibition of Receptor Function

• DOI: 10.1021/jacs.9b05123
• Publication Date: 2019-08-05T19:27:10Z
• Authors: Liping Wang; Hong Liang; Jin Sun; Yichang Liu; Jinyu Li; Jingying Li; Juan Li; Huanghao Yang
• Keywords: Aptamer; Cell surface receptor

Cell surface receptors play a critical role in modulating intracellular signal transduction, making them important drug targets. However, it remains challenging to develop selective and efficient strategy for regulating receptor function. Herein, we strategy, called bispecific aptamer induced artificial protein-pairing, selectively regulate In this probes act as molecular mediators bind both target protein paired protein, which brings the two proteins into close proximity on living cell membrane. Importantly, work not only cancer biomarker enhancing selectivity but also blocking assistant inhibit function via strong steric hindrance effect. Compared with single-aptamer-mediated regulation, proposed afford substantial improvement regulation of downstream signaling pathways. This offers versatile methodology design that can modulate function, thereby providing new way developing novel therapeutic drugs.