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Solid phase synthesis of anthraquinone peptides and their evaluation as topoisomerase I inhibitors

Solid phase synthesis of anthraquinone peptides and their evaluation as topoisomerase I inhibitors
Solid phase synthesis of anthraquinone peptides and their evaluation as topoisomerase I inhibitors
Anthraquinone peptide derivatives have previously been shown to inhibit the enzyme topoisomerase I (topo I), a pharmaceutical target for the prevention of malignant carcinomas. A highly efficient procedure for the attachment of the anthraquinone moiety to the N-terminus of a peptide on a solid support is reported. This methodology provides a convenient method for the synthesis of labelled peptides, with potential applications for chemotherapy, DNA detection and protein purification. As the synthetic strategy utilizes the solid phase, it should also be amenable to the generation of combinatorial libraries. The utility of the method by synthesizing a pool of peptides and assaying for topo I inhibition is demonstrated.
anthraquinone peptide derivatives, topoisomerase I inhibitors
1075-2617
417-423
Giles, Gregory I.
0e3c10cd-6d8c-4f95-8fd8-45259415226d
Sharma, Ram P.
aef51420-fc90-49d8-b04c-142214c2961a
Giles, Gregory I.
0e3c10cd-6d8c-4f95-8fd8-45259415226d
Sharma, Ram P.
aef51420-fc90-49d8-b04c-142214c2961a

Giles, Gregory I. and Sharma, Ram P. (2005) Solid phase synthesis of anthraquinone peptides and their evaluation as topoisomerase I inhibitors. Journal of Peptide Science, 11 (7), 417-423. (doi:10.1002/psc.635).

Record type: Article

Abstract

Anthraquinone peptide derivatives have previously been shown to inhibit the enzyme topoisomerase I (topo I), a pharmaceutical target for the prevention of malignant carcinomas. A highly efficient procedure for the attachment of the anthraquinone moiety to the N-terminus of a peptide on a solid support is reported. This methodology provides a convenient method for the synthesis of labelled peptides, with potential applications for chemotherapy, DNA detection and protein purification. As the synthetic strategy utilizes the solid phase, it should also be amenable to the generation of combinatorial libraries. The utility of the method by synthesizing a pool of peptides and assaying for topo I inhibition is demonstrated.

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More information

Published date: 2005
Keywords: anthraquinone peptide derivatives, topoisomerase I inhibitors

Identifiers

Local EPrints ID: 25075
URI: https://eprints.soton.ac.uk/id/eprint/25075
ISSN: 1075-2617
PURE UUID: a07222cf-b823-4f97-a750-18f8f5eba195

Catalogue record

Date deposited: 05 Apr 2006
Last modified: 17 Jul 2017 16:12

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