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Structure of ristocetin A in complex with a bacterial cell-wall mimetic.

Abstract
Antimicrobial drug resistance is a serious public health problem and the development of new antibiotics has become an important priority. Ristocetin A is a class III glycopeptide antibiotic that is used in the diagnosis of von Willebrand disease and which has served as a lead compound for the development of new antimicrobial therapeutics. The 1.0 A resolution crystal structure of the complex between ristocetin A and a bacterial cell-wall peptide has been determined. As is observed for most other glycopeptide antibiotics, it is shown that ristocetin A forms a back-to-back dimer containing concave binding pockets that recognize the cell-wall peptide. A comparison of the structure of ristocetin A with those of class I glycopeptide antibiotics such as vancomycin and balhimycin identifies differences in the details of dimerization and ligand binding. The structure of the ligand-binding site reveals a likely explanation for ristocetin A's unique anticooperativity between dimerization and ligand binding.
AuthorsVirginie Nahoum, Sherri Spector, Patrick J Loll
JournalActa crystallographica. Section D, Biological crystallography (Acta Crystallogr D Biol Crystallogr) Vol. 65 Issue Pt 8 Pg. 832-8 (Aug 2009) ISSN: 1399-0047 [Electronic] United States
PMID19622867 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, U.S. Gov't, Non-P.H.S.)
Chemical References
  • Anti-Bacterial Agents
  • Ligands
  • Ristocetin
  • balhimycin
  • ristocetin A
  • Vancomycin
Topics
  • Anti-Bacterial Agents (chemistry, metabolism, therapeutic use)
  • Biomimetics (trends)
  • Cell Wall (chemistry)
  • Crystallization
  • Dimerization
  • Drug Design
  • Humans
  • Ligands
  • Methicillin Resistance
  • Methicillin-Resistant Staphylococcus aureus
  • Protein Binding
  • Protein Conformation
  • Ristocetin (chemistry, metabolism, therapeutic use)
  • Staphylococcal Infections (drug therapy)
  • Vancomycin (analogs & derivatives, chemistry, metabolism, therapeutic use)
  • X-Rays

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