Annexin derivatives with endogenous chelation sites

Details Annexin derivatives with endogenous chelation sites Annexin derivatives with endogenous chelation sites

C - Chemistry, Metallurgy

12

N

C12N 15/12 (2006.01) A61K 51/08 (2006.01) C07K 1/00 (2006.01) C07K 5/083 (2006.01) C07K 14/00 (2006.01) C07K 14/47 (2006.01) C07K 17/00 (2006.01) C12N 15/63 (2006.01)

Patent

CA 2377948

Modified annexins having an N-terminal chelation site comprising an amino acid extension are disclosed. The amino acid extension includes an amino acid sequence X1-Gly-X2, where X1 and X2 are selected from Gly and Cys, where at least one of X1 or X2 is Cys. Radionuclides are readily chelated by the modified annexins to provide radiolabeled annexins useful in imaging vascular thrombi and apoptosis <i>in vivo</i>.

L'invention concerne des annexines modifiées comportant un site de chélation N-terminal comprenant une extension acide aminé. Cette extension acide aminé comprend une séquence d'acides aminés X¿1?-Gly-X¿2?, où X¿1? et X¿2? sont choisis entre Gly et Cys, l'un au moins de X¿1? ou de X¿2? étant Cys. Les radionucléides sont rapidement chélatés par les annexines modifiées, ce qui permet d'obtenir des annexines radiomarquées utiles pour l'imagerie des thrombi vasculaires et de l'apoptose <i>in vivo</i>.

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