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Comparison of Four 64Cu-Labeled Somatostatin Analogues in Vitro and in a Tumor-Bearing Rat Model: Evaluation of New Derivatives for Positron
 

Summary: Articles
Comparison of Four 64Cu-Labeled Somatostatin Analogues in Vitro and in a
Tumor-Bearing Rat Model: Evaluation of New Derivatives for Positron
Emission Tomography Imaging and Targeted Radiotherapy|
Jason S. Lewis, Michael R. Lewis, Ananth Srinivasan, Michelle A. Schmidt, Jian Wang, and
Carolyn J. Anderson*,
Mallinckrodt Institute of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard,
Campus Box 8225, St. Louis, Missouri 63110, and Mallinckrodt, Inc., 675 McDonnell Boulevard, Hazelwood, Missouri 63042
Received October 27, 1998
Previous studies have shown that modification of the somatostatin analogue octreotide (OC),
by substitution of tyrosine for phenylalanine at position 3 and of a C-terminal carboxylic acid
for an alcohol, to give Tyr3-octreotate (Y3-TATE) improved uptake of the peptide in somatostatin
receptor-positive tissues. To determine which substitution best accounts for increased target
tissue uptake, the peptides containing single modifications, Tyr3
-octreotide (Y3-OC) and
octreotate (TATE), were synthesized. These peptides were conjugated to the macrocyclic
chelating agent 1,4,8,11-tetraazacyclotetradecane-N,N,N,N-tetraacetic acid (TETA) and
radiolabeled with 64Cu(II). The in vitro receptor binding, in vitro tumor cell uptake, and in
vivo distribution properties of 64
Cu-labeled TETA-Y3-OC and TETA-TATE were compared to

  

Source: Anderson, Carolyn J. - Department of Molecular Biology and Pharmacology, Washington University in St. Louis

 

Collections: Biology and Medicine