Radiolabeled annexins
Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.
1. A modified annexin which is direct radiolabeled with a metal radionuclide, comprising a metal radionuclide complexed directly to a modified annexin, wherein the annexin is modified by the addition of a sulfhydryl group comprised of an N-terminal extension of the annexin, the N-terminal extension comprising a cysteine residue within ten amino acids of the N-terminus of the modified annexin.
2. The modified annexin of claim 1 , wherein the modification of the annexin comprises an amino acid extension at the N-terminus, said amino acid extension comprising a sequence X-Cys-X-X-X-X wherein X signifies an amino acid residue.
3. The modified annexin of claim 2 , wherein the N-terminal extension comprises a sequence Ala-Cys-Asp-His-Ser-Met.
4. The modified annexin of claim 2 , wherein the amino acid extension further comprises glycine.
5. The modified annexin of claim 2 , wherein the annexin is annexin V.
6. The modified annexin of any one of claims 1 - 4 and 5 , wherein the radionuclide is a diagnostic radionuclide.
7. The modified annexin of any one of claims 1 - 4 and 5 , wherein the radionuclide is Cu-64, Cu-67, Re-186, Re-188, Pd-100, Pd-109, Bi-212, Pb-212, Ga-67, Ga-68, Tc-99 m, Tc-94, Ru-95, Ru-105, Rh-99, Rh-105, In-111, Sm-153, Lu-177, Lu-170, Pt-189, Pt-193, Au-199 or Hg-197.
8. The modified annexin of claim 7 , wherein the radionuclide is Cu-64, Cu-67, Re-186, Re-188, Pd-100, Pd-109, Bi-212, Pb-212, Ga-67, Ga-68, Tc-99 m, Tc-94, Ru-95, Ru-105, Rh-99, Rh-105 or In-111.
9. The modified annexin of claim 8 , wherein the radionuclide is Tc-99 m.