Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties

Ruthenium(II) polypyridyl complexes (RPCs) that emit from metal-to-ligand charge transfer (MLCT) states have been developed as DNA probes and are being examined as potential anticancer agents. Here, we report that MLCT-emissive RPCs that bind DNA undergo Förster resonance energy transfer (FRET) with...

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Main Authors: Elgar, Christopher E., Yusoh, Nur Aininie, Tiley, Paul R., Kolozsvári, Natália, Bennett, Laura G., Gamble, Amelia, Péan, Emmanuel V., Davies, Matthew L., Staples, Christopher J., Ahmad, Haslina, Gill, Martin R.
Format: Article
Language:English
Published: American Chemical Society 2023
Online Access:http://psasir.upm.edu.my/id/eprint/103125/
http://psasir.upm.edu.my/id/eprint/103125/1/103125.pdf
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author Elgar, Christopher E.
Yusoh, Nur Aininie
Tiley, Paul R.
Kolozsvári, Natália
Bennett, Laura G.
Gamble, Amelia
Péan, Emmanuel V.
Davies, Matthew L.
Staples, Christopher J.
Ahmad, Haslina
Gill, Martin R.
author_facet Elgar, Christopher E.
Yusoh, Nur Aininie
Tiley, Paul R.
Kolozsvári, Natália
Bennett, Laura G.
Gamble, Amelia
Péan, Emmanuel V.
Davies, Matthew L.
Staples, Christopher J.
Ahmad, Haslina
Gill, Martin R.
author_sort Elgar, Christopher E.
building UPM Institutional Repository
collection Online Access
description Ruthenium(II) polypyridyl complexes (RPCs) that emit from metal-to-ligand charge transfer (MLCT) states have been developed as DNA probes and are being examined as potential anticancer agents. Here, we report that MLCT-emissive RPCs that bind DNA undergo Förster resonance energy transfer (FRET) with Cy5.5-labeled DNA, forming mega-Stokes shift FRET pairs. Based on this discovery, we developed a simple and rapid FRET binding assay to examine DNA-binding interactions of RPCs with diverse photophysical properties, including non-“light switch” complexes [Ru(dppz)2(5,5′dmb)]2+ and [Ru(PIP)2(5,5′dmb)]2+ (dppz = dipyridophenazine, 5,5′dmb = 5,5′-dimethyl-2,2′-bipyridine, PIP = 2-phenyl-imidazo[4,5-f][1,10]phenanthroline). Binding affinities toward duplex, G-quadruplex, three-way junction, and mismatch DNA were determined, and derived FRET donor-acceptor proximities provide information on potential binding sites. Molecules characterized by this method demonstrate encouraging anticancer properties, including synergy with the PARP inhibitor Olaparib, and mechanistic studies indicate that [Ru(PIP)2(5,5′dmb)]2+ acts to block DNA replication fork progression.
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spelling upm-1031252025-04-21T04:27:10Z http://psasir.upm.edu.my/id/eprint/103125/ Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties Elgar, Christopher E. Yusoh, Nur Aininie Tiley, Paul R. Kolozsvári, Natália Bennett, Laura G. Gamble, Amelia Péan, Emmanuel V. Davies, Matthew L. Staples, Christopher J. Ahmad, Haslina Gill, Martin R. Ruthenium(II) polypyridyl complexes (RPCs) that emit from metal-to-ligand charge transfer (MLCT) states have been developed as DNA probes and are being examined as potential anticancer agents. Here, we report that MLCT-emissive RPCs that bind DNA undergo Förster resonance energy transfer (FRET) with Cy5.5-labeled DNA, forming mega-Stokes shift FRET pairs. Based on this discovery, we developed a simple and rapid FRET binding assay to examine DNA-binding interactions of RPCs with diverse photophysical properties, including non-“light switch” complexes [Ru(dppz)2(5,5′dmb)]2+ and [Ru(PIP)2(5,5′dmb)]2+ (dppz = dipyridophenazine, 5,5′dmb = 5,5′-dimethyl-2,2′-bipyridine, PIP = 2-phenyl-imidazo[4,5-f][1,10]phenanthroline). Binding affinities toward duplex, G-quadruplex, three-way junction, and mismatch DNA were determined, and derived FRET donor-acceptor proximities provide information on potential binding sites. Molecules characterized by this method demonstrate encouraging anticancer properties, including synergy with the PARP inhibitor Olaparib, and mechanistic studies indicate that [Ru(PIP)2(5,5′dmb)]2+ acts to block DNA replication fork progression. American Chemical Society 2023 Article PeerReviewed text en cc_by_4 http://psasir.upm.edu.my/id/eprint/103125/1/103125.pdf Elgar, Christopher E. and Yusoh, Nur Aininie and Tiley, Paul R. and Kolozsvári, Natália and Bennett, Laura G. and Gamble, Amelia and Péan, Emmanuel V. and Davies, Matthew L. and Staples, Christopher J. and Ahmad, Haslina and Gill, Martin R. (2023) Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties. Journal of the American Chemical Society, 145 (2). pp. 1236-1246. ISSN 0002-7863; eISSN: 1520-5126 https://pubs.acs.org/doi/10.1021/jacs.2c11111 10.1021/jacs.2c11111
spellingShingle Elgar, Christopher E.
Yusoh, Nur Aininie
Tiley, Paul R.
Kolozsvári, Natália
Bennett, Laura G.
Gamble, Amelia
Péan, Emmanuel V.
Davies, Matthew L.
Staples, Christopher J.
Ahmad, Haslina
Gill, Martin R.
Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties
title Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties
title_full Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties
title_fullStr Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties
title_full_unstemmed Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties
title_short Ruthenium(II) Polypyridyl Complexes as FRET donors: structure- and sequence-selective DNA-binding and anticancer properties
title_sort ruthenium(ii) polypyridyl complexes as fret donors: structure- and sequence-selective dna-binding and anticancer properties
url http://psasir.upm.edu.my/id/eprint/103125/
http://psasir.upm.edu.my/id/eprint/103125/
http://psasir.upm.edu.my/id/eprint/103125/
http://psasir.upm.edu.my/id/eprint/103125/1/103125.pdf