Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking

Journal article

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.Full Tex

Authors: Hennessy, J; Klimkowski, P; Singleton, D; Gibney, A; Coche, M

• Publication status: Published
• Peer review status: Peer reviewed
• Publisher: Royal Society of Chemistry
• Journal: RSC Medicinal Chemistry
• Volume: 15
• Issue: 2
• Pages: 485-491
• Publication date: 2023-10-31
• DOI: 10.1039/d3md00548h
• EISSN: 2632-8682
• ISSN: 2632-8682
• Language: English
• Keywords: Biology; Polymer; Monomer; Nucleobase; Combinatorial chemistry; Click chemistry; Chemistry; Organic chemistry; DNA; Stereochemistry; Thiazole; Bifunctional; Fluorophore; Fluorescence; Oligonucleotide; Biochemistry; Carboplatin