Selective and potent proteomimetic inhibitors of intracellular protein–protein interactions
File(s)
Author(s)
Type
Journal Article
Abstract
Inhibition of protein–protein interactions (PPIs) represents a major challenge in chemical biology and drug discovery. α-Helix mediated PPIs may be amenable to modulation using generic chemotypes, termed “proteomimetics”, which can be assembled in a modular manner to reproduce the vectoral presentation of key side chains found on a helical motif from one partner within the PPI. In this work, it is demonstrated that by using a library of N-alkylated aromatic oligoamide helix mimetics, potent helix mimetics which reproduce their biophysical binding selectivity in a cellular context can be identified.
Date Issued
2015-02-04
Date Acceptance
2015-02-04
Citation
Angewandte Chemie - International Edition, 2015, 54 (10), pp.2960-2965
ISSN
1433-7851
Publisher
Wiley
Start Page
2960
End Page
2965
Journal / Book Title
Angewandte Chemie - International Edition
Volume
54
Issue
10
Copyright Statement
© 2015 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
License URL
Identifier
https://onlinelibrary.wiley.com/doi/full/10.1002/anie.201410810
Subjects
Science & Technology
Physical Sciences
Chemistry, Multidisciplinary
Chemistry
apoptosis
foldamers
helical structures
peptidomimetics
protein-protein interactions
ALPHA-HELIX MIMETICS
MDM2 INHIBITOR
P53
ACTIVATION
AUTOPHAGY
APOPTOSIS
PEPTIDE
CANCER
MCL-1
ANTAGONISTS
apoptosis
foldamers
helical structures
peptidomimetics
protein-protein interactions
Cell Line, Tumor
Humans
Molecular Mimicry
Proteins
Cell Line, Tumor
Humans
Proteins
Molecular Mimicry
Organic Chemistry
03 Chemical Sciences
Publication Status
Published
Date Publish Online
2015-02-04