Optimized Inhibitors of MDM2 via an Attempted Protein-Templated Reductive Amination.

ABSTRACT: Innovative and efficient hit-identification techniques are required to accelerate drug discovery. Protein-templated fragment ligations represent a promising strategy in early drug discovery, enabling the target to assemble and select its binders from a pool of building blocks. Development of new protein-templated reactions to access a larger structural diversity and expansion of the variety of targets to demonstrate the scope of the technique are of prime interest for medicinal chemists. Herein, we present our attempts to use a protein-templated reductive amination to target protein-protein interactions (PPIs), a challenging class of drug targets. We address a flexible pocket, which is difficult to achieve by structure-based drug design. After careful analysis we did not find one of the po

SUBMITTER: van der Vlag R 

PROVIDER: S-EPMC7064911 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature