PMID: 8971929Jan 1, 1996Paper

BW 1023U90: a new GRP receptor antagonist for small-cell lung cancer cells

Peptides
T W MoodyJ J Leban

Abstract

Gastrin-releasing peptide (GRP) receptor antagonists were synthesized and their ability to interact with small-cell lung cancer (SCLC) cells determined. [125I] BW1023U90, bound with high affinity (Kd = 2 nM) to a single class of sites (Bmax = 55 fmol/mg protein) using SCLC cell line NCI-H345. [125I] BW1023U90 binding was time dependent and reversible even at 37 degrees C as the ligand was minimally internalized. Specific [125I] BW1023U90 binding was inhibited with high affinity by GRP as well as bombesin (BB) but not neuromedin B (NMB). BW1023U90 inhibited the ability of BB to elevate cytosolic Ca2+ and increase the growth of SCLC cells. A BW1023U90 analogue, BW2258U89 (10 micrograms/day, SC) slowed SCLC xenograft format on in nude mice and [125I] BW 1023U90 localized to SCLC tumors 1 h after injection into nude mice. BW2258U89 (4% by weight) was placed in microspheres and slowly released over a 3-week period in nude mice bearing SCLC xenografts. The microspheres containing BW2258U89 strongly inhibited SCLC growth in vivo. A radioimmunoassay was developed for the GRP receptor antagonists and the rabbit antiserum cross-reacted totally with BW2258U89 or BW1023U90. BW2258U89 immunoreactivity (5 nM) was detected in the plasma of nu...Continue Reading

References

Nov 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·T W MoodyM R Brown
Sep 12, 1979·Biochemical and Biophysical Research Communications·T J McDonaldV Mutt
Jan 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·J F BatteyR I Feldman
Mar 1, 1990·Proceedings of the National Academy of Sciences of the United States of America·P A BunnE Braunschweiger
Aug 31, 1987·Biochemical and Biophysical Research Communications·T W MoodyG Fiskum
Mar 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·P J Woll, E Rozengurt
Nov 15, 1988·Biochemical and Biophysical Research Communications·J B TrepelE A Sausville
Dec 1, 1981·The Journal of Clinical Endocrinology and Metabolism·S M WoodS R Bloom
Mar 1, 1993·Proceedings of the National Academy of Sciences of the United States of America·J J LebanJ D McDermed

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Citations

May 7, 1998·European Journal of Pharmacology·T K PradhanR T Jensen
Jul 6, 2000·Peptides·M Casibang, T W Moody
Sep 14, 2000·Neuropeptides·C MarquezT W Moody
Mar 14, 2007·Annals of Oncology : Official Journal of the European Society for Medical Oncology·D B CornelioG Schwartsmann
Apr 15, 2010·European Journal of Pharmacology·Terry W MoodyRobert T Jensen

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