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US 2012/0122803 A1Published application
Alpha-conotoxin mii analogs
AssigneeUniversity of Utah Research Foundation
InventorJ. Michael McIntosh
Life of this patent
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Abstract
The invention relates to novel conopeptides and/or novel uses of conopeptides. The conopeptides of the invention are analogs of α-Conotoxin MII that are selective for α6-containing nAChRs as described herein.
Claims4
An isolated conopeptide selected from the group consisting of:
- (SEQ ID NO:
- 15)
- (a) Gly-Cys-Cys-Ser-Asn-Pro-Val-Cys-His-Leu-Ala-
- His-Ser-Asn-Ala-Cys;
- (b) a derivative of (a) having α6-containing nicotinic acetylcholine receptor binding activity, wherein the derivative is a peptide in which the Pro residue is substituted with hydroxy-Pro or O-glycosylated hydroxy-Pro;
- one or both of the Ser residues is or are substituted with O-glycosylated Ser, Thr, O-glycosylated Thr or a synthetic hydroxylated amino acid;
- one or both of the Asn residues is or are substituted with N-glycosylated Asn;
- the Cys residues are in D or L configuration;
- one or more of the Cys residues is or are substituted with homocysteine in the D or L configuration;
- one or more pairs of Cys residues is or are replaced pairwise with a Ser/(Glu or Asp) combination or a Lys/(Glu or Asp) combination, wherein the synthetic hydroxylated amino acid is selected from the group consisting of 4-hydroxymethyl-Phe 4-hydroxyphenyl-Gly, 2,6-dimethyl-Tyr and 5-amino-Tyr;
- (c) a physiologically acceptable salt of (a) or (b).
8 more elements
Dependencies are inferred from the claim text.