Compositions and methods for treating endometriosis
AssigneeEndoMet Biosciences, Inc.
InventorsTanya PETROSSIAN, Stephen FIACCO, Tristin ROSE, Amanda HARDY, Keerthi BODDUPALLY, Matthew WILLMORE
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Abstract
Provided herein are peptides that bind β-catenin, and compositions comprising said peptides. Peptides binding β-catenin prevent translocation to the nucleus and modulate the canonical Wnt pathway. Also provided herein are methods of using said peptides and compositions in the treatment of tissue-infiltrating conditions including endometriosis.
Claims52
A peptide comprising an amino acid sequence having the formula X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16, wherein:
- X1 is M or null;
- X2 is S, I, G, T, A, L, or null;
- X3 is R, K or null;
- X4 is a positively-charged amino acid, citrulline, Orn, D, E, 8-aminooctanoic acid, or an amino carboxylic acid with between 4 and 12 carbons;
- X5 is M, Norleucine, Orn, D, E, K, H, R, K, 8-aminooctanoic acid, an amino carboxylic acid with between 4 and 12 carbons or null;
- X6 is W, Y, F, or N-methyl A;
- X7 is F, I, L, Chg, Cha, or Tle;
- X8 is L, I, or A;
- X9 is L, I, or A;
- X10 is C, S, A, Abu, C(me), or S(Bzl);
- X11 is F, H, A, K, E, Chg, Cng, or Orn
- X12 is W, Y, A, or F;
- and
- X13 is G, GABA, or null.
A peptide comprising an amino acid sequence having the formula R-X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16, wherein:
- R is NH2, acetylation, stearic acid, palmitic acid, myristic acid, lauric acid, a C1-C8 hydrocarbon, a C1-C8 fatty acid, or null;
- X1 is M, G, beta alanine, norleucine, norvaline, or null;
- X2 is W, N-methyl W, R, Y, F, citrulline, or K,
- X3 is P, W, N-methyl-W, N-ethyl-W, N-methyl A, N-ethyl A, L, Pip, Aib, Y, or F;
- X4 is E, Q, N, or D;
- X5 is S, alpha methyl S, K, D, Orn, T, or E;
- X6 is I, Chg, H, or L;
- X7 is L or I;
- X8 is D, N, E, or Q;
- X9 is D, E, K, Q, or Orn;
- X10 is H or methyl-H;
- X11 is V, alpha methyl V, Chg, L I, or norvaline;
- X12 is Q, Aib, S, R, or N;
- X13 is R, K, citrulline, Orn, D, or E;
- X14 is V, I, L, or norvaline;
- X15 is W, Y, or F;
- and
- X16 is R, G, or null.
A pharmaceutical composition comprising:
- a β-catenin inhibitor;
- a peptide comprising binding specificity to β-catenin;
- a β-catenin inhibitor comprising a peptide;
- or
- a peptide comprising an amino acid sequence of any one of SEQ ID NO:
- 1-490;
- and
- a pharmaceutically acceptable carrier.
An intravaginal device comprising a peptide comprising an amino acid sequence of SEQ ID NO:
- 215 or 393 formulated to release peptide in a time-controlled manner,
- wherein the peptide binds β-catenin,
- wherein the peptide inhibits translocation of β-catenin to a nucleus of a cell,
- wherein the peptide does not decrease β-catenin binding E-cadherin in the membrane;
- and
- wherein the peptide reduces size or severity of endometriosis lesions or other symptoms associated with endometriosis in a subject in need thereof.
Dependencies are inferred from the claim text.