Peptide tyrosinase inhibitors and uses thereof
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorBasil M. Hantash
Life of this patent
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Abstract
Disclosed are peptides, which inhibit the enzymatic activity of tyrosinase, as well as formulations and methods for their use in the reduction of skin pigmentation, and methods of administering the inhibitory peptides in a topical formulation. The peptides are characterized by sequences RADSRADC (SEQ ID NO: 2) and PLG-OH. Methods of skin treatment are also provided, the methods further including use of a peptide characterized by the amino acid sequence SFLLRN (SEQ ID NO: 1).
Claims37
A purified peptide having an IC 50 of tyrosinase of less than about 10 mM and selected from the group consisting of:
- tripeptide PLG-OH, a peptide consisting of RADSRADC (SEQ ID NO:2) and a peptide having a sequence essentially identical to said RADSRADC (SEQ ID NO:
- 2), having no more than one amino acid residue substituted with another amino acid residue.
A topical, oral, or injectable formulation comprising an amount of a tyrosinase inhibitor effective to lighten skin pigmentation selected from the group consisting of a peptide consisting of RADSRADC (SEQ ID NO:
- 2), the tripeptide PLG-OH, and a peptide having no more than 2 amino acid substitutions to said RADSRADC (SEQ ID NO:
- 2) according to replacement of an amino acid from column 1 with an amino acid from column 2:
- Column 1
- Column 2
- R
- K or L
- S
- T, A, L, M, I
- D
- N, V, A, L, M, I
- C
- V, A, L, M, I
- A
- G, V, A, L, M, I.
A dermatologically acceptable topical formulation comprising an effective amount of a skin whitening agent and tyrosinase inhibitor selected from the group consisting of a peptide consisting of RADSRADC (SEQ ID NO:
- 2), tripeptide PLG-OH, and a peptide having no more than 2 amino acid substitutions to said RADSRADC (SEQ ID NO:
- 2) according to replacement of an amino acid from column 1 with an amino acid from column 2:
- Column 1
- Column 2
- R
- K or L
- S
- T, A, L, M, I
- D
- N, V, A, L, M, I
- C
- V, A, L, M, I
- A
- G, V, A, L, M, I
- L
- I, V, A, M, I
- N
- D
- F
- R, W, Y.
A method for treatment of skin comprising topically administering to the skin a peptide consisting of RADSRADC (SEQ ID NO:
- 2), a peptide having no more than two amino acid substitutions to said RADSRADC (SEQ ID NO:
- 2), or the tripeptide PLG-OH, wherein said administering of the peptide inhibits tyrosinase sufficiently to lighten skin pigmentation.
A kit for carrying out a skin whitening procedure, comprising a purified peptide having an IC 50 of tyrosinase of less than about 10 mM and selected from the group consisting of:
- tripeptide PLG-OH, a peptide consisting of SEQ ID NO:
- 2, and a peptide having no more than 1 amino acid substitutions to said SEQ ID NO:
- 2;
- a dermatologically acceptable carrier;
- a secondary treatment product;
- and directions for use.
Dependencies are inferred from the claim text.