What question did this study set out to answer?

The aim is to develop selective inhibitors for bacterial thymidylate synthase to improve drug effectiveness against infectious diseases.

April 27, 2026Open Access

Structure-based design of inhibitors specific for bacterial thymidylate synthase

View Full Paper

Ask AI

Bookmark

Authors

Randomized trial demonstrates selective inhibition of bacterial thymidylate synthase, suggesting potential for drug development.

The aim is to develop selective inhibitors for bacterial thymidylate synthase to improve drug effectiveness against infectious diseases.
Designed inhibitors based on the structure of thymidylate synthase from Lactobacillus casei.
Synthesized and tested inhibitors for selectivity against human thymidylate synthase.
Utilized X-ray crystallography to analyze inhibitor binding orientations and site-directed mutagenesis to explore binding configurations.
Initial inhibitors showed up to 40-fold selectivity for bacterial over human enzyme activity.
Second-round compounds inhibited the bacterial enzyme at sub-micromolar concentrations with selectivities of 100-1000-fold or greater.
X-ray crystal structures indicate that inhibitors bind to thymidylate synthase in distinct orientations.

STOUT et al. (1999) studied this question.

View Full Paper

Ask AI

Bookmark