B-strand mimetic foldamers rigidified through dipolar repulsion
B-strand mimetic foldamers rigidified through dipolar repulsion
Many therapeutically relevant protein–protein interactions contain hot-spot regions on secondary structural elements, which contribute disproportionately to binding enthalpy. Mimicry of such ?-helical regions has met with considerable success, however the analogous approach for the ?-strand has received less attention. Presented herein is a foldamer for strand mimicry in which dipolar repulsion is a central determinant of conformation. Computation as well as solution- and solid-phase data are consistent with an ensemble weighted almost exclusively in favor of the desired conformation.
2649-2652
German, Elizabeth A.
03d53651-149f-49bb-95e0-4f67cdf7a452
Ross, Jonathan E.
90459779-9860-40a3-9ce7-4efb14ed15ec
Knipe, Peter C.
a75b6ed7-4d9b-45fc-aacc-49e9e0d0b266
Don, Michaela F.
01a73f9a-0eb7-437b-aaf1-3dde3d758fd0
Thompson, Sam
99b7e34e-fe24-401c-b7b0-64e56cbbbcb1
Hamilton, Andrew D.
048a6c75-91bf-4555-ab12-ce885eee65dd
23 February 2015
German, Elizabeth A.
03d53651-149f-49bb-95e0-4f67cdf7a452
Ross, Jonathan E.
90459779-9860-40a3-9ce7-4efb14ed15ec
Knipe, Peter C.
a75b6ed7-4d9b-45fc-aacc-49e9e0d0b266
Don, Michaela F.
01a73f9a-0eb7-437b-aaf1-3dde3d758fd0
Thompson, Sam
99b7e34e-fe24-401c-b7b0-64e56cbbbcb1
Hamilton, Andrew D.
048a6c75-91bf-4555-ab12-ce885eee65dd
German, Elizabeth A., Ross, Jonathan E., Knipe, Peter C., Don, Michaela F., Thompson, Sam and Hamilton, Andrew D.
(2015)
B-strand mimetic foldamers rigidified through dipolar repulsion.
Angewandte Chemie International Edition, 54 (9), .
(doi:10.1002/anie.201410290).
Abstract
Many therapeutically relevant protein–protein interactions contain hot-spot regions on secondary structural elements, which contribute disproportionately to binding enthalpy. Mimicry of such ?-helical regions has met with considerable success, however the analogous approach for the ?-strand has received less attention. Presented herein is a foldamer for strand mimicry in which dipolar repulsion is a central determinant of conformation. Computation as well as solution- and solid-phase data are consistent with an ensemble weighted almost exclusively in favor of the desired conformation.
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e-pub ahead of print date: 19 January 2015
Published date: 23 February 2015
Organisations:
Chemistry
Identifiers
Local EPrints ID: 403576
URI: http://eprints.soton.ac.uk/id/eprint/403576
ISSN: 1433-7851
PURE UUID: 331e6885-4af9-46da-97c1-3179bb038dab
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Date deposited: 07 Dec 2016 09:57
Last modified: 15 Mar 2024 03:54
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Contributors
Author:
Elizabeth A. German
Author:
Jonathan E. Ross
Author:
Peter C. Knipe
Author:
Michaela F. Don
Author:
Andrew D. Hamilton
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