bullvalene-vancomycin conjugate

The bullvalene-vancomycin conjugate is an experimental antibiotic designed to combat vancomycin-resistant enterococci (VRE). Developed by researchers at Scripps Research and Cold Spring Harbor Laboratory, the molecule features a fluxional bullvalene core linked to vancomycin subunits. Bullvalene is a unique hydrocarbon that undergoes rapid, degenerate Cope rearrangements, providing the conjugate with a shape-shifting ability. This allows the vancomycin moieties to dynamically adjust their spatial orientation, optimizing binding to the bacterial cell wall precursors D-alanyl-D-alanine and the resistance-modified D-alanyl-D-lactate. By increasing the avidity of these interactions through adaptive positioning, the conjugate overcomes the decreased affinity that typically characterizes vancomycin resistance, demonstrating potent antimicrobial activity in preclinical models.

Other names

bullvalene-linked vancomycinshape-shifting vancomycinbullvalene-linked vancomycin dimer