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Selective and Potent Proteomimetic Inhibitors of Intracellular Protein-Protein Interactions.

ABSTRACT: Inhibition of protein-protein interactions (PPIs) represents a major challenge in chemical biology and drug discovery. ?-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.

SUBMITTER: Barnard A 

PROVIDER: S-EPMC4737265 | biostudies-literature | 2015 Mar

REPOSITORIES: biostudies-literature

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Selective and Potent Proteomimetic Inhibitors of Intracellular Protein-Protein Interactions.

Barnard Anna A   Long Kérya K   Martin Heather L HL   Miles Jennifer A JA   Edwards Thomas A TA   Tomlinson Darren C DC   Macdonald Andrew A   Wilson Andrew J AJ  

Angewandte Chemie (Weinheim an der Bergstrasse, Germany) 20150130 10

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 heli  ...[more]

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