Crystals of LuxP and complexes thereof

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S462000

Reexamination Certificate

active

10227400

ABSTRACT:
A crystal comprising LuxP is obtained, and a binding site for autoinducer-2 (AI-2) identified. The X-ray crystallographic data for LuxP and a LuxP-AI-2 complex is determined and used in a drug discovery method. Pharmaceutical compositions comprising ligands identified by such drug discovery methods are used to treat bacterial infections.

REFERENCES:
patent: 2003/0022932 (2003-01-01), Surette et al.
patent: W/O 0032152 (2000-06-01), None
Xin Chen, Stephan Schauder, Noelle Potier, Alain Van Dorsselaer, Istvan Pelczer, Bonnie L. Bassler, & Frederick M. Hughson, Structural identification of a bacterial quorum-sensing signal containing boron, Nature, 415:545-549 (Jan. 31, 2002).
Chen & Zhi, Ligand-Protein Inverse Docking and Its Potential Use in the Computer Search of Protein Targets of a Small Molecule, Proteins: Structure, Function, and Genetics, 43:217-226 (2001).
Chen, Xin et al., “Structural identification of a bacterial quorum-sensing signal containing boron,” Nature, vol. 415, pp. 545-549 (2002).
Klaus Benner, Peter Klufers, “A combined x-ray and NMR study of borate esters of furanoidic cis-1, 2-diols,” Institute for Organic Chemistry University, Germany, Feb. 14, 2000.
Ron van den Berg, Joop A. Peters and Herman van Bekkum, “The structure and (local) stability constants of borate esters of mono- and di-saccharides as studied by 11B and 13C NMR spectroscopy,” Laboratory of Organic Chemistry and Catalysts, Delft University of Technology, Netherlands, Jun. 29, 1993.
Database Caplus, DN 121:247611. Bassler et al. Multiple signalling systems controlling expression of luminescence inVibrio harveyi: sequence and function of genes encoding a second sensory pathway. Molecular Microbiology, 1994, vol. 13, No. 2, pp. 273-286.
Database Biosis, AN 2002:233419. Lo et al. Analysis of a quorum sensing system n Mannheimia (Pasteurella) haemolytica A1 and related pasteurellaceae species. Abstracts of the General Meeting of the American Society for Microbiology, (2001) vol. 101, pp. 741-742. Meeting Info: 101stGeneral Meeting of the American Society for Microbiology, Orlando, FL, May 20-24, 2001.
International Preliminary Examination Report dated Dec. 23, 2003.
Crystal Screen User Guide, Hampton Research, 1991.

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