abstract |
The present invention includes non-RGD cyclic peptides that inhibit the function of the integrin receptor, alpha v beta 3. The inventive peptides are between five to about thirty amino acids in length and include the sequence (SEQ ID NO:8), Arg-Cys-Asp-Gly-Xi where Xi is any amino acid, and a five-membered cyclic portion. These non-RGD peptides display surprisingly potent antagonist activity despite the lack of the consensus binding sequence Arg-Gly-Asp, and present opportunities for selective targeting to the alpha v beta 3 receptor. Pharmaceutical compositions and methods of use are also disclosed. The therapeutic uses for the inventive peptides include treating diseases involving alpha v beta 3 receptors such as cancer, osteoporosis, restenosis, and angiogenic-based diseases. |