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US 2025/0026787 A1Published application
Peptides and methods for reducing skin pigmentation
AssigneeGlo Pharma, Inc.
InventorRobert A. LOVE
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to novel peptide antagonists that inhibit binding of melanocyte stimulating hormone to the melanocortin 1 receptor. The peptide antagonists of the disclosure are useful in cosmetic compositions that prevent or reduce the appearance of skin discoloration caused by pigmentation. The disclosure further relates to cosmetic compositions comprising a peptide antagonist of the disclosure, and methods for their use for preventing or reducing the appearance of skin discoloration in a subject in need thereof.
Claims25
A melanocortin 1 receptor (MC1R) peptide antagonist comprising an amino acid sequence:
- Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9
- wherein:
- Xaa1 is absent or selected from:
- Cys, Met, Sec, Ser, Thr, D-Cys, D-Met, D-Sec, D-Ser, D-Thr, Ala, Gly, Val, Leu, Ile, D-Ala, D-Gly, D-Val, D-Leu, D-Ile, Phe, Trp, Tyr, D-Phe, D-Trp, D-Tyr, Asn, Asp, Gln, Glu, D-Asn, D-Asp, D-Gln, D-Glu, and a derivative of Cys, Met, Sec, Ser, Thr, D-Cys, D-Met, D-Sec, D-Ser, D-Thr, Ala, Gly, Val, Leu, Ile, D-Ala, D-Gly, D-Val, D-Leu, D-Ile, Phe, Trp, Tyr, D-Phe, D-Trp, D-Tyr, Asn, Asp, Gln, Glu, D-Asn, D-Asp, D-Gln, or D-Glu;
- Xaa2 is selected from:
- Pro, D-Pro, Ala, Gly, Val, Leu, Ile, D-Ala, D-Gly, D-Val, D-Leu, D-Ile, and a derivative of Pro, D-Pro, Ala, Gly, Val, Leu, Ile, D-Ala, D-Gly, D-Val, D-Leu, or D-Ile;
- Xaa3 is selected from:
- Phe, Trp, Tyr, D-Phe, D-Trp, D-Tyr, and a derivative of Phe, Trp, Tyr, D-Phe, D-Trp, or D-Tyr;
- Xaa4 is selected from:
- Arg, His, Lys, D-Arg, D-His, D-Lys, and a derivative of Arg, His, Lys, D-Arg, D-His, or D-Lys;
- Xaa5 is selected from:
- Phe, Trp, Tyr, D-Phe, D-Trp, D-Tyr, and a derivative of Phe, Trp, Tyr, D-Phe, D-Trp, or D-Tyr;
- Xaa6 is selected from:
- Phe, Trp, Tyr, D-Phe, D-Trp, D-Tyr, and a derivative of Phe, Trp, Tyr, D-Phe, D-Trp, or D-Tyr;
- Xaa7 is selected from:
- Arg, His, Lys, D-Arg, D-His, D-Lys, and a derivative of Arg, His, Lys, D-Arg, D-His, or D-Lys,
- Xaa8 is selected from:
- Pro, D-Pro, and a derivative of Pro or D-Pro;
- Xaa9 is selected from:
- Ala, Gly, Val, Leu, Ile, D-Ala, D-Gly, D-Val, D-Leu, D-Ile, and a derivative of Ala, Gly, Val, Leu, Ile, D-Ala, D-Gly, D-Val, D-Leu, or D-Ile;
- wherein when Xaa1 is Met, Xaa2 is not Pro;
- the N-terminus is optionally modified;
- and
- the C-terminus is optionally modified.
21 more elements
A melanocortin 1 receptor (MC1R) peptide antagonist comprising an amino acid sequence:
- Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-Xaa17-Xaa18-Xaa19-Xaa20-Xaa21-Xaa22-Xaa23-Xaa24-Xaa25-Xaa26
- wherein:
- Xaa1 is absent or Xaa1 and Xaa19 form a linkage Xaa1-Xaa19;
- Xaa2 is absent or selected from:
- Ala, Gly, Val, Leu, Ile, and a derivative of Ala, Gly, Val, Leu, or Ile;
- Xaa3 is absent or selected from:
- Asn, Asp, Gln, Glu, and a derivative of Asn, Asp, Gln, or Glu;
- Xaa4 is absent or selected from:
- Pro and a derivative of Pro;
- Xaa5 is absent or Xaa5 and Xaa26 form a linkage Xaa5-Xaa26;
- Xaa6 is absent or selected from:
- Ala, Gly, Val, Leu, Ile, and a derivative of Ala, Gly, Val, Leu, or Ile;
- Xaa7 is absent or selected from:
- Cys, Met, Sec, Ser, Thr, and a derivative of Cys, Met, Sec, Ser, or Thr;
- Xaa8 is absent or selected from:
- Ala, Gly, Val, Leu, Ile, Arg, His, Lys, Asn, Asp, Gln, Glu, and a derivative of Ala, Gly, Val, Leu, Ile, Arg, His, Lys, Asn, Asp, Gln, or Glu, and/or Xaa8 and Xaa19 form a linkage Xaa8-Xaa19;
- Xaa9 is absent or selected from:
- Phe, Trp, Tyr, Asn, Asp, Gln, Glu, and a derivative of Phe, Trp, Tyr, Asn, Asp, Gln, or Glu;
- Xaa10 and Xaa17 form a linkage Xaa10-Xaa17;
- Xaa11 is selected from:
- Arg, His, Lys, and a derivative of Arg, His, or Lys;
- Xaa12 is selected from:
- Phe, Trp, Tyr, and a derivative of Phe, Trp, or Tyr;
- Xaa13 is selected from:
- Phe, Trp, Tyr, and a derivative of Phe, Trp, or Tyr;
- Xaa14 is selected from:
- Arg, His, Lys, and a derivative of Arg, His, or Lys;
- Xaa15 is selected from:
- Cys, Met, Sec, Ser, Thr, and a derivative of Cys, Met, Sec, Ser, Thr;
- Xaa16 is selected from:
- Ala, Gly, Val, Leu, Ile, and a derivative of Ala, Gly, Val, Leu, or Ile;
- Xaa18 is absent or selected from:
- Phe, Trp, Tyr, Cys, Met, Sec, Ser, Thr, and a derivative of Phe, Trp, Tyr, Cys, Met, Sec, Ser, or Thr;
- Xaa19 is absent or selected from:
- Ala, Gly, Val, Leu, Ile, Arg, His, Lys, Asn, Asp, Gln, Glu, and a derivative of Ala, Gly, Val, Leu, Ile, Arg, His, Lys, Asn, Asp, Gln, or Glu, and/or Xaa8 and Xaa19 form a linkage Xaa8-Xaa19, or Xaa1 and Xaa19 form a linkage Xaa1-Xaa19;
- Xaa20 is absent or selected from:
- Arg, His, Lys, and a derivative of Arg, His, or Lys;
- Xaa21 is absent or selected from:
- Ala, Gly, Val, Leu, Ile, and a derivative of Ala, Gly, Val, Leu, or Ile;
- Xaa22 is absent or selected from:
- Ala, Gly, Val, Leu, Ile, and a derivative of Ala, Gly, Val, Leu, or Ile;
- Xaa23 is absent or selected from:
- Cys, Met, Sec, Ser, Thr, and a derivative of Cys, Met, Sec, Ser, Thr;
- Xaa24 is absent or selected from:
- Ala, Gly, Val, Leu, Ile, and a derivative of Ala, Gly, Val, Leu, or Ile;
- Xaa25 is absent or selected from:
- Asn, Asp, Gln, Glu, and a derivative of Asn, Asp, Gln, or Glu;
- Xaa26 is absent or Xaa5 and Xaa26 form a linkage Xaa5-Xaa26;
- the N-terminus is optionally modified;
- and
- the C-terminus is optionally modified.
48 more elements
A melanocortin 1 receptor peptide antagonist comprising an amino acid sequence set forth as any of SEQ ID NOS:
- 4-90.
Dependencies are inferred from the claim text.