Glycogen synthase kinase-3 inhibitors
AssigneeTel Aviv University Future Technology Development L.P.
InventorHagit Eldar-Finkelman
Life of this patent
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Abstract
Novel conjugates that are capable of inhibiting GSK-3 activity, a process of producing same, pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions are disclosed. Methods of treating affective disorders using GSK-3 inhibitors are further disclosed.
Claims95
A conjugate comprising:
- (a) a polypeptide having the amino acid sequence:
- [Yn . . . Y1]ZX1X2X3S(p)[W1 . . . Wm]
- wherein,
- m equals 1 or 2;
- n is an integer from 1 to 50;
- S(p) is a phosphorylated serine residue or a phosphorylated threonine residue;
- Z is any amino acid residue excepting serine residue or threonine residue;
- and
- X1, X2, X3, Y1-Yn and W1-Wm are each independently any amino acid residue;
- and
- (b) at least one hydrophobic moiety being attached to said polypeptide,
- the conjugate being capable of inhibiting an activity of glycogen synthase kinase-3 (GSK-3), wherein the hydrophobic moiety provides the conjugate with better (i) membrane permeability and/or (b) interaction with the hydrophobic patch of the GSK-3.
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A method of treating an affective disorder, the method comprising administering to a subject in need thereof a therapeutically effective amount of at least one compound that is capable of specifically inhibiting an activity of GSK-3.
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A method of up-regulating a β-catenin level in a hippocampus of a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of at least one compound that is capable of specifically inhibiting an activity of GSK-3.
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Dependencies are inferred from the claim text.