Issue 2, 2024

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

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.

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

Supplementary files

Article information

Article type
Research Article
Submitted
03 Oct 2023
Accepted
27 Oct 2023
First published
31 Oct 2023
This article is Open Access
Creative Commons BY license

RSC Med. Chem., 2024,15, 485-491

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

J. Hennessy, P. Klimkowski, D. Singleton, A. Gibney, M. Coche, N. P. Farrell, A. H. El-Sagheer, T. Brown and A. Kellett, RSC Med. Chem., 2024, 15, 485 DOI: 10.1039/D3MD00548H

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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