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Glucagon superfamily peptides exhbiting G protein coupled receptor activity

  • US 9,145,451 B2
  • Filed: 05/10/2011
  • Issued: 09/29/2015
  • Est. Priority Date: 05/13/2010
  • Status: Expired due to Fees
First Claim
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1. A compound comprising the structure Q-L-Y;

  • wherein Q is a glucagon superfamily peptide having agonist activity at the glucagon receptor, the GIP receptor, the GLP-1 receptor, or a combination thereof;

    Y is a G protein-coupled receptor (GPCR) ligand which activates a G protein-coupled receptor selected from an adrenergic receptor or a nicotinic acetylcholine receptor with an EC50 of about 1 μ

    M or less, and has a molecular weight of up to about 1000 daltons; and

    L is a linking group or a bond,wherein Q comprises an amino acid sequence at least 50% identical to native glucagon that retains the alpha-helix conformation of the amino acids corresponding to amino acids 12-29 of native glucagon (SEQ ID NO;

         1601) or an amino acid sequence at least 50% identical to native GLP-1 that retains the alpha-helix conformation of the amino acids corresponding to amino acids 12-29 of native GLP-1 (SEQ ID NO;

         1603);

    wherein L-Y is conjugated to Q at position 10, 20, 24, 30, 37, 38, 39, 40, 41, 32, or 43 of Q.

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