Rgd-containing cyclic peptides
AssigneeThe Regents of the University of California
InventorsKit S. Lam, Yan Wang, Wenwu Xiao
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Abstract
The present invention is drawn to cyclic RGD peptides linked via a disulfide bond, where the terminal cysteines are preferably in the D configuration. These peptides target αvβ3 integrin on tumor cells and neovasculatures and function as targeting agents for tumor diagnostic imaging and therapy. Compared with the commonly used RGD ligands, compounds of the present invention have improved targeting efficacy and lower nonspecific binding to normal organs. Moreover, the compounds of the present invention can be functionalized to conjugate imaging payload without decreasing binding strength.
Claims26
A compound of formula I:
- X1-X2-X3-X4-X5-X6-X7-X8 (I)
- wherein
- X1, X2, X6, X7 and X8 are each independently an amino acid, wherein at least one of X1, X2, X6, X7 and X8 is a D-amino acid;
- X3 is a basic amino acid;
- X4 is Gly;
- and
- X5 is an acidic amino acid;
- wherein the compounds of formula I are peptides cyclized via a disulfide or a diselenium bond between amino acids X1 and X8.
Dependencies are inferred from the claim text.