Department of Pharmaceutical Sciences, Wayne State University, 259 Mack Avenue, Detroit, MI 48202, USA.
Angew Chem Int Ed Engl. 2012 Aug 27;51(35):8740-3. doi: 10.1002/anie.201203463. Epub 2012 Jul 31.
A bicyclam-based biodegradable polycation with CXCR4 antagonistic activity was developed with potential for combined drug/gene cancer therapies. The dual-function polycation prevents cancer cell invasion by inhibiting CXCL12 stimulated CXCR4 activation, while at the same time efficiently and safely delivers plasmid DNA into cancer cells.
开发了一种基于双环酰胺的可生物降解聚阳离子,具有 CXCR4 拮抗活性,有望用于联合药物/基因癌症治疗。这种双功能聚阳离子通过抑制 CXCL12 刺激的 CXCR4 激活来防止癌细胞侵袭,同时高效、安全地将质粒 DNA 递送至癌细胞内。