Fluorescein-labelled peptides
AssigneeGe Healthcare Limited
InventorsAlan Cuthbertson, Bard Indrevoll, Magne Solbakken
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Abstract
The invention relates to new peptide-based compounds and their use in diagnostic optical imaging. More specifically the invention relates to the use of such peptide-based compounds as targeting vectors that bind to receptors associated with angiogenesis. The compounds are labeled with fluorescein and may be used as contrast agents in optical imaging in diagnosis of angiogenesis-related diseases.
Claims10
A compound comprising a peptidic vector and at least one fluorescein dye, wherein the peptidic vector and the fluorescein dye are coupled, and wherein said peptidic vector is defined by formula I:
- Ra—C(═O)—X1—X2—X3-G-D-X4—X5—X6—X7 (I)
- wherein Formula I comprises two cyclising bridges, and wherein
- Ra represents —(CH2)n— or —(CH2)n—C6H4— forming a bridge to one of X2, X4 or X6, wherein
- n represents a positive integer from 1 to 10, and
- X1 represents a bond or 1, 2, 3, 4 or 5 amino acid residues, wherein one amino acid residue is optionally functionalised with a spacer moiety, or said amino acid residue possesses a functional side-chain chosen from an acid or amine group,
- X2 is an amino acid residue forming a cyclising bridge to one of Ra, X4 or X6;
- X3 represents arginine or N-methylarginine,
- G represents glycine,
- D represents aspartic acid,
- X4 is an amino acid residue forming a cyclising bridge to one of Ra, X2 or X6;
- X5 represents a hydrophobic amino acid, and
- X6 represents an amino acid residue forming a cyclising bridge to either Ra, X2 or X4, and
- X7 represents a spacer or biomodifier moiety or is absent, wherein said biomodifier comprises a monodisperse polyethylene glycol (PEG) building block comprising 1 to 10 units of said building block;
- and,
- wherein at least one of the fluorescein dye is linked to one or more of the groups X1, X6, or X7 optionally via a spacer group.
Dependencies are inferred from the claim text.