[Leu13-psi(CH2NH)Leu14]bombesin is a specific bombesin receptor antagonist in Swiss 3T3 cells.
The pseudopeptide [Leu13-psi(CH2NH)Leu14]bombesin blocks bombesin-stimulated mitogenesis in Swiss 3T3 cells in a competitive and reversible manner, but not that of other mitogens. It inhibits the mobilization of intracellular Ca2+ and activation of protein kinase C by bombesin-like peptides. It acts at receptor level, as shown by inhibition of [125I]GRP binding and reduction in cross-linking of the Mr 75-85,000 receptor-associated protein. Thus [Leu13-psi(CH2NH)Leu14]bombesin is a specific bombesin receptor antagonist in Swiss 3T3 cells which blocks long-term growth promoting effects of bombesin-like peptides.
Woll
P J
PJ
Growth Regulation Laboratory, Imperial Cancer Research Fund, London, U.K.
Coy
D H
DH
Rozengurt
E
E
D000818:Animals; D001839:Bombesin / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology*; D002460:Cell Line; D003432:Cross-Linking Reagents; D005347:Fibroblasts / Q000187:drug effects* / Q000378:metabolism; D019886:Gastrin-Releasing Peptide; D051379:Mice; D008934:Mitogens / Q000378:metabolism / Q000494:pharmacology*; D010455:Peptides / Q000494:pharmacology; D018004:Receptors, Bombesin; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors*; D014667:Vasopressins / Q000378:metabolism
D003432:Cross-Linking Reagents; D008934:Mitogens; D010455:Peptides; D018004:Receptors, Bombesin; D017981:Receptors, Neurotransmitter; D014667:Vasopressins; D019886:Gastrin-Releasing Peptide; D001839:Bombesin