Ed T. Buurman

TL;DR: A mechanistic PD model that includes drug-target kinetic parameters, including the on- and off-rates for the formation and breakdown of the drug- target complex is described and used to predict dose response curves for inhibitors of the LpxC enzyme from Pseudomonas aeruginosa in an animal model of infection.

TL;DR: Substrate binding sites in Kdp, a P-type ATPase of Escherichia coli, were identified by the isolation and characterization of mutants with reduced affinity for K+, its cation substrate, suggesting that KdpA has 10 membrane-spanning segments and forms two separate and distinct sites where K+ is bound.

TL;DR: A novel class of substituted adenosine analogs was discovered by target-based high-throughput screening (HTS), and these compounds were optimized to render them more effective and selective inhibitors of LigA, validating LgA as a target for antibacterial therapy.

TL;DR: Modifications described herein led to compounds that possessed antibacterial activity, which was shown to occur through inhibition of GlmU, a bifunctional essential enzyme involved in bacterial cell wall synthesis.