Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold.

ABSTRACT: Mimicry of two faces of an α-helix might yield more potent and more selective inhibitors of aberrant, helix-mediated protein-protein interactions (PPI). Herein, we demonstrate that a 2,6,9-tri-substituted purine is capable of disrupting the Mcl-1-Bak-BH3 PPI through effective mimicry of key residues on opposing faces of the Bak-BH3 α-helix.

SUBMITTER: Lanning ME 

PROVIDER: S-EPMC4528301 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature