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Novel series of DNA triple helix-binding ligands

Novel series of DNA triple helix-binding ligands
Novel series of DNA triple helix-binding ligands

We have examined the effect of a series of substituted imidazothioxanthones on the stability of an intermolecular DNA triple helix by DNase I footprinting. We find that several of these compounds promote the formation of a complex between T5C5 and the target site A6G6·C6T6, suggesting that they bind specifically to triplex DNA. The only inactive derivative lacked a protonatable function in the side chain, suggesting that this is an essential feature for triplex stabilization. These compounds, which are amongst the first triplex-binding ligands which possess an uncharged chromophore, are selective for the T·AT rather than the C+·GC triplet.

0006-291X
717-720
Fox, Keith R.
9da5debc-4e45-473e-ab8c-550d1104659f
Thurston, David E.
9e2a56ac-259f-4977-a087-9d97c9003fbb
Jenkins, Terence C.
87f02eac-6560-4f66-92fa-c87a7d55d558
Varvaresou, Athanasia
12607b1d-7d8f-4b43-973d-304c0eefe05f
Tsotinis, Andrew
aa014052-342c-42ae-8674-e2a9006f6f25
Siatra-Papastaikoudi, Theodora
1e980f59-3ac0-49eb-894e-bc28ea4638f7
Fox, Keith R.
9da5debc-4e45-473e-ab8c-550d1104659f
Thurston, David E.
9e2a56ac-259f-4977-a087-9d97c9003fbb
Jenkins, Terence C.
87f02eac-6560-4f66-92fa-c87a7d55d558
Varvaresou, Athanasia
12607b1d-7d8f-4b43-973d-304c0eefe05f
Tsotinis, Andrew
aa014052-342c-42ae-8674-e2a9006f6f25
Siatra-Papastaikoudi, Theodora
1e980f59-3ac0-49eb-894e-bc28ea4638f7

Fox, Keith R., Thurston, David E., Jenkins, Terence C., Varvaresou, Athanasia, Tsotinis, Andrew and Siatra-Papastaikoudi, Theodora (1996) Novel series of DNA triple helix-binding ligands. Biochemical and Biophysical Research Communications, 224 (3), 717-720. (doi:10.1006/bbrc.1996.1089).

Record type: Article

Abstract

We have examined the effect of a series of substituted imidazothioxanthones on the stability of an intermolecular DNA triple helix by DNase I footprinting. We find that several of these compounds promote the formation of a complex between T5C5 and the target site A6G6·C6T6, suggesting that they bind specifically to triplex DNA. The only inactive derivative lacked a protonatable function in the side chain, suggesting that this is an essential feature for triplex stabilization. These compounds, which are amongst the first triplex-binding ligands which possess an uncharged chromophore, are selective for the T·AT rather than the C+·GC triplet.

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More information

Published date: 25 July 1996
Additional Information: Funding Information: This work was supported by grants from the Cancer Research Campaign and the Medical Research Council (KRF).

Identifiers

Local EPrints ID: 476347
URI: http://eprints.soton.ac.uk/id/eprint/476347
ISSN: 0006-291X
PURE UUID: 8d620865-a78b-471c-a22a-68bbf3939b7b
ORCID for Keith R. Fox: ORCID iD orcid.org/0000-0002-2925-7315

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Date deposited: 19 Apr 2023 16:46
Last modified: 18 Mar 2024 02:32

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Contributors

Author: Keith R. Fox ORCID iD
Author: David E. Thurston
Author: Terence C. Jenkins
Author: Athanasia Varvaresou
Author: Andrew Tsotinis
Author: Theodora Siatra-Papastaikoudi

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