Research Focus

Vancomycin inhibits bacterial cell wall synthesis by binding to the D-ala-D-alanine end of the pentapeptide via five hydrogen bonds, thereby preventing cross-linking of the pentapeptides to form the normal bacterial peptidoglycan layer. VanX hydrolyzes almost all of D-ala-D-alanyl dipeptides of the pentapeptides so that vancomycin loses the targets. Clearly, to produce tight-binding inhibitor of VanX is an effective way to combat vancomycin resistance in bacteria. Towards this goal, we are implementing rational strategy to design, synthesize and evaluate inhibitors of the VanX, to investigate structure-activity relationship (SAR), which is used for guiding design of new drugs.