The Discovery of MMP7 Inhibitors Exploiting a Novel Selectivity Trigger

Trigger happy! High-throughput screening was used to identify selective MMP7 inhibitors. Subsequent analysis by X-ray crystallography revealed the underlying features for the selectivity trigger, unique to MMP7. In addition, further structural studies increased the understanding of the plasticity of the MMP7 active site. Finally, a single round of chemistry resulted in compounds with improved potency and retained selectivity.