Beijing Key Laboratory of Construction Tailorable Advanced Functional Materials and Green Applications, School of Materials Science and Engineering, Beijing Institute of Technology, Beijing, 100081, China.
Department of Chemistry, Korea University, Seoul, 02841, Korea.
Angew Chem Int Ed Engl. 2020 May 25;59(22):8435-8439. doi: 10.1002/anie.201916524. Epub 2020 Mar 5.
Heteroatom-containing spiropolymers were constructed in a facile manner by a catalyst-free multicomponent spiropolymerization route. P1a2b as the most potent of these spiropolymers, demonstrates cluster-triggered emission resulting from strong interactions with the MDM2 protein. By preventing the anti-apoptotic p53/MDM2 interaction, P1a2b triggers apoptosis in cancerous cells, while demonstrating a good biocompatibility and non-toxicity in non-cancerous cells. The combined results from solution and cell-based cluster-triggered emission studies, docking, protein expression experiments and cytotoxicity data strongly support the MDM2-binding hypothesis and indicate a potential application as a fluorescent cancer marker as well as therapeutic for this spiropolymer.
通过无催化剂的多组分螺环聚合途径，简便地构建了含杂原子的螺环聚合物。这些螺环聚合物中，P1a2b 的活性最强，其表现出团簇引发的发射，这源于与 MDM2 蛋白的强烈相互作用。通过阻止抗凋亡的 p53/MDM2 相互作用，P1a2b 可引发癌细胞凋亡，同时在非癌细胞中表现出良好的生物相容性和低毒性。溶液和基于细胞的团簇引发发射研究、对接、蛋白表达实验和细胞毒性数据的综合结果，强烈支持 MDM2 结合假说，并表明该螺环聚合物作为荧光癌症标志物以及治疗剂具有潜在应用。
