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.
717-720
Fox, Keith R.
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Thurston, David E.
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Jenkins, Terence C.
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Varvaresou, Athanasia
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Tsotinis, Andrew
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Siatra-Papastaikoudi, Theodora
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25 July 1996
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), .
(doi:10.1006/bbrc.1996.1089).
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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Published date: 25 July 1996
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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
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Date deposited: 19 Apr 2023 16:46
Last modified: 18 Mar 2024 02:32
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Contributors
Author:
David E. Thurston
Author:
Terence C. Jenkins
Author:
Athanasia Varvaresou
Author:
Andrew Tsotinis
Author:
Theodora Siatra-Papastaikoudi
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