Abstract
Moody, T. W., J. Leyton, E. Unsworth, C. John, L. Lang and W. C. Eckelman. (Arg 15, Arg 21) VIP: Evaluation of biological activity and localization to breast cancer tumors. Peptides 19(3) 585–592, 1998.—VIP analogs, which contain a single lysine amino acid, were synthesized and evaluated using breast cancer cells. (Arg 15, Arg 20) VIP, (Arg 15, Arg 21) VIP, and (Arg 20, Arg 21) VIP inhibited 125I-VIP binding to T47D cells with high affinity (IC 50 values of 1.2, 1.0, and 0.8 nM, respectively). The VIP analogs elevated cAMP in T47D cells with ED 50 values ranging from 0.1–1 nM. Because (Arg 15, Arg 21) VIP was the most potent at elevating cAMP, it was characterized further. (Arg 15, Arg 21) VIP transiently increased c-fos gene expression in breast cancer cells. N-Succinimidyl-4- 18F (fluoromethly) benzoate was prepared in one chemical step from N-succinimidyl-4-(4-nitrobenzenesulfonyl)oxomethyl)benzoate by adding 18F in acetone at room temperature. This prosthetic group was then reacted with (Arg 15, Arg 21) VIP ((RR) VIP). ( 18F-RR) VIP bound with high affinity to T47D cells and was rapidly internalized. ( 18F-RR) VIP was injected intravenously into nude mice bearing breast cancer xenografts and after 4 h, the density of ( 18F-RR) VIP was elevated in the tumors relative to normal organs. These data suggest that VIP receptors may be used to localize breast cancer tumors.
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