DNA containing repeating G-rich sequences can adopt higher-order structures known as a G-quadruplexes (G4). These structures are believed to form at telomeres and within the promoter regions of some genes, particularly in a number of proto-oncogenes, where they may play a role in regulating transcription.  Alternatively, G4 DNA may act as a barrier to replication.  In order to investigate these potential biological roles, probes that combine highly selective G4 DNA targeting with photocleavage activity can allow temporal detection of G4 DNA, providing opportunities to obtain novel insights.  Towards this end, we have designed a library of potential photoactive probes using �click� chemistry to join known G4 DNA interactive groups with moieties known to facilitate photocleavage of DNA . This library is screened using our recently described FRET-based assay for G4 DNA photocleavage activity and preference as well as binding selectivity for G4 DNA.

Rapid screening of a click-based library for G-quadruplex selective photocleavage agents

245th National Meeting (2013)

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