a-helix mimetics: outwards and upwards
a-helix mimetics: outwards and upwards
?-Helices are common secondary structural elements forming key parts of the large, generally featureless interfacial regions of many therapeutically-relevant protein–protein interactions (PPIs). The rational design of helix mimetics is an appealing small-molecule strategy for the mediation of aberrant PPIs, however the first generation of scaffolds presented a relatively small number of residues on a single recognition surface. Increasingly, helices involved in PPIs are found to have more complex binding modes, utilizing two or three recognition surfaces, or binding with extended points of contact. To address these unmet needs the design and synthesis of new generations of multi-sided, extended, and supersecondary structures are underway.
717-724
Jayatunga, Madura K.P.
a30f1efb-bf44-4a9b-b8d0-4b34e7575313
Thompson, Sam
99b7e34e-fe24-401c-b7b0-64e56cbbbcb1
Hamilton, Andrew D.
048a6c75-91bf-4555-ab12-ce885eee65dd
1 February 2014
Jayatunga, Madura K.P.
a30f1efb-bf44-4a9b-b8d0-4b34e7575313
Thompson, Sam
99b7e34e-fe24-401c-b7b0-64e56cbbbcb1
Hamilton, Andrew D.
048a6c75-91bf-4555-ab12-ce885eee65dd
Jayatunga, Madura K.P., Thompson, Sam and Hamilton, Andrew D.
(2014)
a-helix mimetics: outwards and upwards.
Bioorganic & Medicinal Chemistry Letters, 24 (3), .
(doi:10.1016/j.bmcl.2013.12.003).
Abstract
?-Helices are common secondary structural elements forming key parts of the large, generally featureless interfacial regions of many therapeutically-relevant protein–protein interactions (PPIs). The rational design of helix mimetics is an appealing small-molecule strategy for the mediation of aberrant PPIs, however the first generation of scaffolds presented a relatively small number of residues on a single recognition surface. Increasingly, helices involved in PPIs are found to have more complex binding modes, utilizing two or three recognition surfaces, or binding with extended points of contact. To address these unmet needs the design and synthesis of new generations of multi-sided, extended, and supersecondary structures are underway.
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bmcl 2014 717.pdf
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Accepted/In Press date: 1 December 2013
e-pub ahead of print date: 8 December 2013
Published date: 1 February 2014
Organisations:
Chemistry
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Local EPrints ID: 403584
URI: http://eprints.soton.ac.uk/id/eprint/403584
ISSN: 0960-894X
PURE UUID: ef8af648-3e29-4a42-96c5-b2fff4fd667c
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Date deposited: 07 Dec 2016 10:20
Last modified: 15 Mar 2024 03:54
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Author:
Madura K.P. Jayatunga
Author:
Andrew D. Hamilton
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