Small-Molecule-Based Self-Assembled Ligands for G-Quadruplex DNA Surface Recognition.

ABSTRACT: Most drugs are small molecules because of their attractive pharmacokinetics, manageable development and manufacturing, and effective binding into the concave crevices of bio-macromolecules. Despite these features, they often fall short when it comes to effectively recognizing the surfaces of bio-macromolecules. One way to overcome the challenge of biomolecular surface recognition is to develop small molecules that become self-assembled ligands (SALs) prior to binding. Herein, we report SALs made from 8-aryl-2'-deoxyguanosine derivatives forming precise hydrophilic supramolecular G-quadruplexes (SGQs) with excellent size, shape, and charge complementarity to G-quadruplex DNA (QDNA). We show that only those compounds forming SGQs act as SALs, which in turn differentially stabilize QDNAs from

SUBMITTER: Rivera-Sanchez MDC 

PROVIDER: S-EPMC5664172 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature