Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking
RSC Medicinal Chemistry2023Vol. 15(2), pp. 485–491
Citations Over TimeTop 22% of 2023 papers
Joseph Hennessy, Piotr Klimkowski, Daniel Singleton, Alex Gibney, Malou Coche, Nicholas P. Farrell, Afaf H. El‐Sagheer, Tom Brown, Andrew Kellett
Abstract
We report a new class of carboplatin-TFO hybrid that incorporates a bifunctional alkyne-amine nucleobase monomer called AP-C3-dT that enables dual 'click' platinum(ii) drug conjugation and thiazole orange fluorophore coupling. Thiazole orange enhances the binding of Pt(ii)-TFO hybrids and provides an intrinsic method for monitoring triplex formation. These hybrid constructs possess increased stabilisation and crosslinking properties in comparison to earlier Pt(ii)-TFOs, and demonstrate sequence-specific binding at neutral pH.
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