Patent Number: 6,169,074

Title: Peptide inhibitors of neurotransmitter secretion by neuronal cells

Abstract: The invention consists of peptides which inhibit the secretion of neurotransmitters from synaptic vesicles. The peptides of the invention are believed to mimic the activity of neurotoxins produced by Clostridium botulinum and tetani (including botulinum serotypes A, B, C, D, E, F and G). Structurally, the peptides are comprised of amino acid fragments from the substrate binding domains selected from three proteins which bind to form a receptor for docking of synaptic vesicles to the plasma membranes of neuronal cells; i.e., SNAP-25, VAMP-2 and syntaxin. Certain of the inventive peptides exhibit strong inhibitory activity; e.g., 50% or greater decline in neurotransmitter release is obtained at even nanomolar concentrations. The peptides are suited for use as substitutes for Clostridium neurotoxins in clinical applications and in compounds for targeted delivery of drugs into neural cells.

Inventors: Montal; Mauricio (La Jolla, CA), Canaves; Jaume M. (San Diego, CA), Ferrer-Monteil; Antonio V. (Alicante, ES)

Assignee: The Regents of the University of California

International Classification: C07K 14/195 (20060101); C07K 14/33 (20060101); A61K 38/00 (20060101); C07K 007/08 (); C07K 014/435 (); A61K 038/10 (); A61K 038/17 ()

Expiration Date: 01/02/2018