8-Triazolylpurines: Towards Fluorescent Inhibitors of the MDM2/p53 Interaction.

ABSTRACT: Small molecule nonpeptidic mimics of α-helices are widely recognised as protein-protein interaction (PPIs) inhibitors. Protein-protein interactions mediate virtually all important regulatory pathways in a cell, and the ability to control and modulate PPIs is therefore of great significance to basic biology, where controlled disruption of protein networks is key to understanding network connectivity and function. We have designed and synthesised two series of 2,6,9-substituted 8-triazolylpurines as α-helix mimetics. The first series was designed based on low energy conformations but did not display any biological activity in a biochemical fluorescence polarisation assay targeting MDM2/p53. Although solution NMR conformation studies demonstrated that such molecules could mimic the topography

SUBMITTER: Pettersson M 

PROVIDER: S-EPMC4420247 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature