Radiolabelling Pt-based quadruplex DNA binders via click chemistry.
File(s)1-s2.0-S0968089622004904-main.pdf (2.37 MB)
Published version
Author(s)
Lo, Rainbow
Majid, Aatikah
Fruhwirth, Gilbert O
Vilar, Ramon
Type
Journal Article
Abstract
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.
Date Issued
2022-11-13
Date Acceptance
2022-11-08
Citation
Bioorganic and Medicinal Chemistry, 2022, 76, pp.1-9
ISSN
0968-0896
Publisher
Elsevier
Start Page
1
End Page
9
Journal / Book Title
Bioorganic and Medicinal Chemistry
Volume
76
Copyright Statement
© 2022 The Author(s). Published by Elsevier Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/)
License URL
Identifier
https://www.ncbi.nlm.nih.gov/pubmed/36417789
PII: S0968-0896(22)00490-4
Subjects
0304 Medicinal and Biomolecular Chemistry
0305 Organic Chemistry
1115 Pharmacology and Pharmaceutical Sciences
Medicinal & Biomolecular Chemistry
Publication Status
Published
Coverage Spatial
England
Date Publish Online
2022-11-13