Jibin Abraham Punnoose, Yue Ma, Yuanyuan Li, Mai Sakuma, Shankar Mandal, Kazuo Nagasawa, Hanbin Mao
Targeting DNA G-quadruplexes using small-molecule ligands has shown to modulate biological functions mediated by G-quadruplexes inside cells. Given >716 000 G-quadruplex hosting sites in human genome, the specific binding of ligands to quadruplex becomes problematic. Here, we innovated a polyvalency based mechanism to specifically target multiple telomeric G-quadruplexes. We synthesized a tetrameric telomestatin derivative and evaluated its complex polyvalent binding with multiple G-quadruplexes by single-molecule mechanical unfolding in laser tweezers...
June 7, 2017: Journal of the American Chemical Society