Peptide conjugates and methods of use
AssigneeThe Scripps Research Institute
InventorsWeijun Shen, Elsa Pflimlin, Sam Lear, Zaid Amso, Peter G. Schultz
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Abstract
Peptide conjugates comprising a peptide selected from a peptide that modulates the PYY receptor, a peptide that modulates both the GLP-1 receptor and the GCG receptor, a peptide that modulates both the GLP-1 receptor and the GIP receptor, and a peptide that modulates the GLP-1 receptor; and a staple attached to the peptide at a first amino acid and a second amino acid are disclosed herein. Also provided are peptide conjugates comprising prolactin-releasing peptide. The peptide conjugates may be used for treating conditions such as obesity. Further provided are stapled prolactin-releasing peptide.
Claims5
A peptide conjugate comprising:
- a) a peptide comprising SEQ ID NO:
- 6, or an amino acid sequence having one amino acid addition, deletion, or substitution relative to the sequence from SEQ ID NO:
- 6;
- and
- b) a staple attached to the peptide at a first amino acid and a second amino acid, wherein the first amino acid and second amino acid is independently cysteine or homocysteine, wherein the first amino acid has a position i in the peptide and the second amino acid has a position i+7 in the peptide, wherein the staple is:
- wherein
- each L1 is independently -alkylene-O—, —O-alkylene-, —C(═O)NH—, —NHC(=0)-, -alkylene-C(=0)NH—, —alkylene-NHC(=0)-, or —(CR1R2)—, wherein each R1 and R2 is independently hydrogen, C1-6 alkyl, or —COOH, and v is 2-20;
- s1 is 1-15;
- and
- Y is COOH.
Dependencies are inferred from the claim text.