PMID: 9533649Apr 9, 1998Paper

(Arg15, Arg21) VIP: evaluation of biological activity and localization to breast cancer tumors

Peptides
T W MoodyW C Eckelman

Abstract

VIP analogs, which contain a single lysine amino acid, were synthesized and evaluated using breast cancer cells. (Arg15, Arg20) VIP, (Argl5, Arg21) VIP, and (Arg20, Arg21) VIP inhibited 125I-VIP binding to T47D cells with high affinity (IC50 values of 1.2, 1.0, and 0.8 nM, respectively). The VIP analogs elevated cAMP in T47D cells with ED50 values ranging from 0.1-1 nM. Because (Arg15, Arg21) VIP was the most potent at elevating cAMP, it was characterized further. (Arg15, Arg21) 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 (Arg15, Arg21) 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.

References

Jan 6, 1992·Biochimica Et Biophysica Acta·M HosoyaA Arimura
Nov 1, 1987·Peptides·M M ShafferT W Moody
Feb 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·D E Brenneman, L E Eiden
Jan 1, 1981·Journal of Supramolecular Structure and Cellular Biochemistry·T W MoodyC B Pert
Jan 1, 1981·Peptides·J ChristopheP Robberecht
Dec 1, 1994·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·L Lang, W C Eckelman
Apr 1, 1994·Trends in Pharmacological Sciences·T Harmar, E Lutz
May 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·T W MoodyI Gozes
Jul 1, 1993·Proceedings of the National Academy of Sciences of the United States of America·J R Pisegna, S A Wank

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Citations

Feb 11, 2003·Peptides·Terry W MoodyRobert T Jensen
Jul 29, 2000·Bioorganic & Medicinal Chemistry Letters·J L Sutcliffe-GouldenS S Bansal
Mar 14, 2001·Breast Cancer Research and Treatment·S DagarH Onyüksel
Jan 25, 2014·BioMed Research International·Dengfeng ChengHongcheng Shi
Dec 26, 2015·Current Opinion in Endocrinology, Diabetes, and Obesity·Terry W MoodyRobert T Jensen
Jul 13, 2004·Nuclear Medicine and Biology·E M JagodaW C Eckelman
Mar 21, 2006·Nuclear Medicine and Biology·Kjerstin Bruus-JensenHans-Jürgen Wester
Jul 16, 2005·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·M Olga García-FernándezJuan Carlos Prieto
Feb 26, 2016·Natural Product Reports·C L CharronL G Luyt
Aug 31, 2002·Journal of Molecular Recognition : JMR·Sarah BhargavaRudolf Volkmer-Engert
Aug 16, 2003·Endocrine Reviews·Jean Claude Reubi
May 11, 2019·Annals of the New York Academy of Sciences·Terry W Moody
Feb 1, 2014·International Journal of Oncology·Bo TangShi-Ming Yang
Feb 24, 2001·Annals of the New York Academy of Sciences·T W MoodyY Gozes
Feb 24, 2001·Annals of the New York Academy of Sciences·B MadsenJ Fahrenkrug
Jul 17, 2018·Frontiers in Endocrinology·Terry W MoodyRobert T Jensen
Nov 20, 2009·Bioconjugate Chemistry·Jessica BecaudBeate Koksch

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