Orthogonal functionalisation of α-helix mimetics.

ABSTRACT: 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.

SUBMITTER: Barnard A 

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

REPOSITORIES: biostudies-literature