Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo alpha(v)beta(3) integrin related tumor imaging

The association of the alpha(v)beta(3) integrin with tumor metastasis and tumor related angiogenesis has been suggested. Therefore, by imaging the alpha(v)6(3) receptor with PET. information concerning the tumor status could be obtained. Cyclic peptides including the RGD sequence. Were radiolabeled by direct electrophilic fluorination with [F-18]AcOF. In tumor-bearing mice, the labeled peptides accumulated at the tumor with a high tumor to blood ratio. These findings suggest that an assessment of tumor characteristics may be obtained by using these F-18-labeled peptides. (C) 2002 Elsevier Science Inc. All rights reserved.