Identifying Oxacillinase-48 Carbapenemase Inhibitors Using DNA-Encoded Chemical Libraries

DNA-encoded chemical libraries.

The discovery and development of novel drugs for the multitude of targets originating from functional genomic research is a challenging task. While antibodies can nowadays be raised against virtually any given target using phage-display methodologies, a similar "selection/amplification" approach for the facile discovery of low-molecular weight compounds capable of specific binding to protein ta...

Discovery of small molecule inhibitors of protein-protein interactions using DNA- encoded chemical libraries

Discovery of small molecule inhibitors of protein-protein interactions (PPIs) has been limited due to technological hurdles. Here we present the discovery of small molecule (MW< 500 Da) inhibitors of PPIs with IC50 in the μM range from a 2 million compound DNA-encoded chemical library. The screening of the library was performed using a recently developed homogenous binding assay. This format av...

Novel selection methods for DNA-encoded chemical libraries.

Driven by the need for new compounds to serve as biological probes and leads for therapeutic development and the growing accessibility of DNA technologies including high-throughput sequencing, many academic and industrial groups have begun to use DNA-encoded chemical libraries as a source of bioactive small molecules. In this review, we describe the technologies that have enabled the selection ...

Carbapenem-hydrolyzing Oxacillinase-48 and Oxacillinase-181 in Canada, 2011

Euclidean shape-encoded combinatorial chemical libraries.

A method for the encoding of split/mix combinatorial chemical libraries based on Euclidean shapes is described. The shapes are fashioned from a polymeric matrix designed to swell in common organic solvents while retaining their unique forms, and exhibit good mechanical strength. The lightly crosslinked gel-type polymer was processed into an array of Euclidean forms that serve as encoding elemen...