@article{Lo:2022:10.1016/j.bmc.2022.117097,
author = {Lo, R and Majid, A and Fruhwirth, GO and Vilar, R},
doi = {10.1016/j.bmc.2022.117097},
journal = {Bioorganic and Medicinal Chemistry},
pages = {1--9},
title = {Radiolabelling Pt-based quadruplex DNA binders via click chemistry.},
url = {http://dx.doi.org/10.1016/j.bmc.2022.117097},
volume = {76},
year = {2022}
}

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TY  - JOUR
AB  - Guanine-rich sequences of DNA and RNA can fold into intramolecular tetra-helical assemblies known as G-quadruplexes (G4). Their formation in vivo has been associated to a range of biological functions and therefore they have been identified as potential drug targets. Consequently, a broad range of small molecules have been developed to target G4s. Amongst those are metal complexes with Schiff base ligands. Herein, we report the functionalisation of one of these well-established G4 DNA binders (based on a square planar platinum(II)-salphen complex) with two different radiolabelled complexes. An 111In-conjugate was successfully used to assess its in vivo distribution in a mouse tumour model using single-photon emission computed tomography (SPECT) imaging. These studies highlighted the accumulation of this Pt-salphen-111In conjugate in the tumour.
AU  - Lo,R
AU  - Majid,A
AU  - Fruhwirth,GO
AU  - Vilar,R
DO  - 10.1016/j.bmc.2022.117097
EP  - 9
PY  - 2022///
SN  - 0968-0896
SP  - 1
TI  - Radiolabelling Pt-based quadruplex DNA binders via click chemistry.
T2  - Bioorganic and Medicinal Chemistry
UR  - http://dx.doi.org/10.1016/j.bmc.2022.117097
UR  - https://www.ncbi.nlm.nih.gov/pubmed/36417789
UR  - https://www.sciencedirect.com/science/article/pii/S0968089622004904?via%3Dihub
UR  - http://hdl.handle.net/10044/1/100881
VL  - 76
ER  - 

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