Structure guided design of biotin protein ligase inhibitors for antibiotic discovery.

@article{Paparella2014StructureGD,
  title={Structure guided design of biotin protein ligase inhibitors for antibiotic discovery.},
  author={Ashleigh S. Paparella and Tatiana P. Soares da Costa and Min Y Yap and William Tieu and Matthew C. J. Wilce and Grant W Booker and Andrew D. Abell and Steven W Polyak},
  journal={Current topics in medicinal chemistry},
  year={2014},
  volume={14 1},
  pages={
          4-20
        }
}
Biotin protein ligase (BPL) represents a promising target for the discovery of new antibacterial chemotherapeutics. Here we review the central role of BPL for the survival and virulence of clinically important Staphylococcus aureus in support of this claim. X-ray crystallography structures of BPLs in complex with ligands and small molecule inhibitors provide new insights into the mechanism of protein biotinylation, and a template for structure guided approaches to the design of inhibitors for… CONTINUE READING

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