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Orthogonal functionalisation of ?-helix mimetics.

ABSTRACT: ?-Helix mediated protein-protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide ?-helix mimetics using 'click' chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors.

SUBMITTER: Barnard A

PROVIDER: S-EPMC4157654 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature

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Orthogonal functionalisation of α-helix mimetics.

Barnard Anna A Long Kérya K Yeo David J DJ Miles Jennifer A JA Azzarito Valeria V Burslem George M GM Prabhakaran Panchami P A Edwards Thomas T Wilson Andrew J AJ

Organic & biomolecular chemistry 20140901 35

α-Helix mediated protein-protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using 'click' chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors. ...[more]

PMID: 25065821

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