Methods for the creation of cyclic peptide libraries for use in lead discovery
Methods for the creation of cyclic peptide libraries for use in lead discovery
The identification of initial hits is a crucial stage in the drug discovery process. Although many projects adopt high-throughput screening of small-molecule libraries at this stage, there is significant potential for screening libraries of macromolecules created using chemical biology approaches. Not only can the production of the library be directly interfaced with a cell-based assay, but these libraries also require significantly fewer resources to generate and maintain. In this context, cyclic peptides are increasingly viewed as ideal scaffolds and have proven capability against challenging targets such as protein-protein interactions. Here we discuss a range of methods used for the creation of cyclic peptide libraries and detail examples of their successful implementation.
cyclic peptide, high-throughput screening, protein-protein interactions, review
563-567
Foster, Andrew
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Ingram, James
2d63d67f-3ce9-4429-b679-2408170f6d54
Leitch, Eilidh
a6cfc162-80d3-40b8-8d63-6e50ac71a160
Lennard, Katherine
1ddd5215-8af1-4654-ac6e-f6ff308403da
Osher, Eliot
bcaf2f72-05de-41b2-aa0d-995f4c66d8f0
Tavassoli, Ali
d561cf8f-2669-46b5-b6e1-2016c85d63b2
June 2015
Foster, Andrew
e12c139f-cb45-4bed-ae80-821e9b540f3d
Ingram, James
2d63d67f-3ce9-4429-b679-2408170f6d54
Leitch, Eilidh
a6cfc162-80d3-40b8-8d63-6e50ac71a160
Lennard, Katherine
1ddd5215-8af1-4654-ac6e-f6ff308403da
Osher, Eliot
bcaf2f72-05de-41b2-aa0d-995f4c66d8f0
Tavassoli, Ali
d561cf8f-2669-46b5-b6e1-2016c85d63b2
Foster, Andrew, Ingram, James, Leitch, Eilidh, Lennard, Katherine, Osher, Eliot and Tavassoli, Ali
(2015)
Methods for the creation of cyclic peptide libraries for use in lead discovery.
Journal of Biomolecular Screening, 20 (5), .
(doi:10.1177/1087057114566803).
(PMID:25586497)
Abstract
The identification of initial hits is a crucial stage in the drug discovery process. Although many projects adopt high-throughput screening of small-molecule libraries at this stage, there is significant potential for screening libraries of macromolecules created using chemical biology approaches. Not only can the production of the library be directly interfaced with a cell-based assay, but these libraries also require significantly fewer resources to generate and maintain. In this context, cyclic peptides are increasingly viewed as ideal scaffolds and have proven capability against challenging targets such as protein-protein interactions. Here we discuss a range of methods used for the creation of cyclic peptide libraries and detail examples of their successful implementation.
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Accepted/In Press date: 11 December 2014
e-pub ahead of print date: 19 May 2015
Published date: June 2015
Keywords:
cyclic peptide, high-throughput screening, protein-protein interactions, review
Identifiers
Local EPrints ID: 389333
URI: http://eprints.soton.ac.uk/id/eprint/389333
ISSN: 1087-0571
PURE UUID: 0eea101d-8be7-4adc-84c1-26a759eeaaa5
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Date deposited: 04 Mar 2016 11:56
Last modified: 15 Mar 2024 03:26
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Contributors
Author:
Andrew Foster
Author:
James Ingram
Author:
Eilidh Leitch
Author:
Katherine Lennard
Author:
Eliot Osher
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