Inside Cover: Stapled Peptides with [gamma]-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction

Mimicking protein side chains with a functionalized hydrocarbon "staple" can affect the conformation and/or affinity for a protein target. In their Communication on page4252ff., T.W. Moore and co-workers address the structural implications of replacing leucine and isoleucine residues with...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2016-03, Vol.55 (13), p.4104
Main Authors: Speltz, Thomas E, Fanning, Sean W, Mayne, Christopher G, Fowler, Colin, Tajkhorshid, Emad, Greene, Geoffrey L, Moore, Terry W
Format: Article
Language:English
Subjects:
Estrogens
Hydrocarbons
Online Access:Get full text
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Summary:Mimicking protein side chains with a functionalized hydrocarbon "staple" can affect the conformation and/or affinity for a protein target. In their Communication on page4252ff., T.W. Moore and co-workers address the structural implications of replacing leucine and isoleucine residues with [gamma]-methyl-substituted stapling amino acids. X-ray crystal structures and molecular dynamics simulations provide a molecular understanding of the conformations of stapled peptides bound to estrogen receptor[alpha].
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201601641