Previns as specific inhibitors and therapeutic agents for...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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Details

C514S015800, C530S300000, C435S007100, C435S320100, C536S023500, C424S239100

Reexamination Certificate

active

09979101

ABSTRACT:
The compounds of the invention are generally described by the formula (1): B1Z*2B3Z*4X*5Q6F7X8X9X10X11, (2): B1X2X3X4X5Q6F7X8X9X10X11, or (3): B1X2B3X4Z5Q6F7Z8X9X10X11and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum B and tetanus toxins.

REFERENCES:
patent: 99 37664 (1999-07-01), None
Garcia, Gregory E. et al., “Botulinum B toxin activity is inhibited by Buforin I.”FASEB Journal,Apr. 24, 1998, p. A1472, vol. 12, No. 8., Meeting of the American Society for Biochemistry and Molecular Biology, Washington D.C., US.
Park, C.B. et al., “A Novel Antimicrobial Peptide From Bufo Buto Gargarizans”,Biochemical and Biophysical Research Communications,1996, pp. 408-413, vol. 218, Academic Press Inc. Orlando, FL, US.
Norinder, U et al., “Quantitative Structure-Activity Relationship Study of Some Substance P-Related Peptides. A Multivariate Approach Using PLS and Variable Selection”,Journal of Peptide Research,Feb. 1, 1997, pp. 155-162, vol. 49, No. 2, Munksgaard International Publishers, Copenhagen, Denmark.
Niedzwiecki, Lisa et al., “Substrate Specificity Of The Human Matrix Metalloproteinase Stromelysin And The Development Of Continuous Fluorometric Assays”,BIOCHEMISTRY,1992.
Boksa, Patricia et al., “Characterization Of Substance P And Somatostatin Receptors On Adrenal Chromaffin Cells Using Structural Analogs”,Chemical Abstracts Service, Columbus, Ohio, US.

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