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a-helix mimetics: outwards and upwards

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.
0960-894X
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
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), 717-724. (doi:10.1016/j.bmcl.2013.12.003).

Record type: Article

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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Accepted/In Press date: 1 December 2013
e-pub ahead of print date: 8 December 2013
Published date: 1 February 2014
Organisations: Chemistry

Identifiers

Local EPrints ID: 403584
URI: http://eprints.soton.ac.uk/id/eprint/403584
ISSN: 0960-894X
PURE UUID: ef8af648-3e29-4a42-96c5-b2fff4fd667c
ORCID for Sam Thompson: ORCID iD orcid.org/0000-0001-6267-5693

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Date deposited: 07 Dec 2016 10:20
Last modified: 03 Dec 2019 01:32

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Contributors

Author: Madura K.P. Jayatunga
Author: Sam Thompson ORCID iD
Author: Andrew D. Hamilton

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