Insulin and IGF-1 receptor agonists and antagonists
First Claim
1. An insulin-like growth factor receptor antagonist comprising the Formula 2 sequence, X6X7X8X9X10X11X12X13, such that X6 and X7 are aromatic amino acids, X8, X9, X11, and X12 are any amino acid, and X10 and X13 are leucine, wherein the antagonist further comprises two or more cysteines which are separated by at least 3 amino acids, with the proviso that the antagonist is not insulin, insulin-like growth factor, an anti-insulin receptor antibody, an anti-insulin-like growth factor receptor antibody, or fragments thereof.
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Abstract
Peptide sequences capable of binding to insulin and/or insulin-like growth factor receptors with either agonist or antagonist activity and identified from various peptide libraries are disclosed. This invention also identifies at least two different binding sites, which are present on insulin and insulin-like growth factor receptors, and which selectively bind the peptides of this invention. As agonists, the peptides of this invention may be useful for development as therapeutics to supplement or replace endogenous peptide hormones. The antagonist peptides may also be developed as therapeutics.
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Citations
5 Claims
- 1. An insulin-like growth factor receptor antagonist comprising the Formula 2 sequence, X6X7X8X9X10X11X12X13, such that X6 and X7 are aromatic amino acids, X8, X9, X11, and X12 are any amino acid, and X10 and X13 are leucine, wherein the antagonist further comprises two or more cysteines which are separated by at least 3 amino acids, with the proviso that the antagonist is not insulin, insulin-like growth factor, an anti-insulin receptor antibody, an anti-insulin-like growth factor receptor antibody, or fragments thereof.
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4. A method of decreasing insulin-like growth factor receptor activity in insulin-like growth factor-responsive mammalian cells comprising:
- contacting the cells with an insulin-like growth factor receptor antagonist in an amount sufficient to decrease the activity of the insulin-like growth factor receptor, wherein i) the antagonist comprises the Formula 2 sequence,
X6X7X8X9X10X11X12X13, such that X6 and X7 are aromatic amino acids, X8, X9, X11, and X12 are any amino acid, and X10 and X13 are leucine;
ii) the antagonist further comprises two or more cysteines which are separated by at least 3 amino acids; and
iii) with the proviso that the antagonist is not insulin, insulin-like growth factor, an anti-insulin receptor antibody, an anti-insulin-like growth factor receptor antibody, or fragments thereof. - View Dependent Claims (5)
- contacting the cells with an insulin-like growth factor receptor antagonist in an amount sufficient to decrease the activity of the insulin-like growth factor receptor, wherein i) the antagonist comprises the Formula 2 sequence,
Specification