Woll P J, Coy D H, Rozengurt E
Growth Regulation Laboratory, Imperial Cancer Research Fund, London, U.K.
Biochem Biophys Res Commun. 1988 Aug 30;155(1):359-65. doi: 10.1016/s0006-291x(88)81093-3.
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.
假肽[Leu13-psi(CH2NH)Leu14]蛙皮素以竞争性和可逆的方式阻断蛙皮素刺激的瑞士3T3细胞有丝分裂，但对其他促细胞分裂剂无此作用。它抑制蛙皮素样肽引起的细胞内Ca2+动员和蛋白激酶C的激活。如对[125I]胃泌素释放肽（GRP）结合的抑制以及Mr 75 - 85,000受体相关蛋白交联的减少所示，它作用于受体水平。因此，[Leu13-psi(CH2NH)Leu14]蛙皮素是瑞士3T3细胞中的一种特异性蛙皮素受体拮抗剂，可阻断蛙皮素样肽的长期生长促进作用。
