Inside Cover: Stapled Peptides with γ‐Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction (Angew. Chem. Int. Ed. 13/2016). Issue 13 (3rd March 2016)

• Record Type: Journal Article
• Authors: Speltz, Thomas E.; Fanning, Sean W.; Mayne, Christopher G.; Fowler, Colin; Tajkhorshid, Emad; Greene, Geoffrey L.; Moore, Terry W.
• Is Part Of: Angewandte Chemie international edition. Volume 55:Issue 13(2016)
• Page Start: 4104
• Page End: 4104
• Publication Date: 2016-03-03
• Subjects: amino acids -- conformational analysis -- peptides -- peptidomimetics -- receptors; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201601641
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract : Mimicking protein side chains with a functionalized hydrocarbon "staple" can affect the conformation and/or affinity for a protein target. In their Communication onpage 4252 ff., T. W. Moore and co‐workers address the structural implications of replacing leucine and isoleucine residues with γ‐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 α.