Bold R J, Kim H J, Ishizuka J, Townsend C M, Thompson J C
Department of Surgery, University of California, Davis-East Bay, Oakland 94602, USA.
Cancer Invest. 1998;16(1):12-7. doi: 10.3109/07357909809039748.
Bombesin (BBS) exhibits diverse biological functions including those of neurotransmitter, regulator of gastrointestinal hormone release, and mitogen. Gastrin-releasing peptide (GRP, the mammalian equivalent of BBS) is found in mucosal cells of the gastric fundus and antrum. We determined whether a human gastric cancer cell line (SIIA) expresses a functional GRP-receptor (GRP-R). BBS increased intracellular calcium ([Ca2+]i), and a specific GRP-R antagonist, ([D-Phe6, Des-Met14]-BBS (6-14)-ethylamide), blocked BBS-induced increase in [Ca2+]i. SIIA cells possess GRP-R mRNA by reverse transcriptase-PCR. Furthermore, these cells possess an 80-kDa cell surface protein that specifically binds BBS with two high-binding affinities (Kd1 = 0.6 nM, Kd2 = 6.7 nM). These findings indicate that SIIA cells possess a GRP-R that is capable of physiological signal transduction, though the cellular response remains unknown.
蛙皮素(BBS)具有多种生物学功能,包括作为神经递质、胃肠激素释放调节剂和促细胞分裂剂。胃泌素释放肽(GRP,BBS的哺乳动物等同物)存在于胃底和胃窦的黏膜细胞中。我们确定了一种人胃癌细胞系(SIIA)是否表达功能性胃泌素释放肽受体(GRP-R)。蛙皮素增加细胞内钙浓度([Ca2+]i),而一种特异性胃泌素释放肽受体拮抗剂([D-苯丙氨酸6,去甲蛋氨酸14]-蛙皮素(6-14)乙酰胺)可阻断蛙皮素诱导的[Ca2+]i增加。通过逆转录聚合酶链反应(RT-PCR)检测发现SIIA细胞含有胃泌素释放肽受体信使核糖核酸(GRP-R mRNA)。此外,这些细胞具有一种80 kDa的细胞表面蛋白,该蛋白以两种高结合亲和力(Kd1 = 0.6 nM,Kd2 = 6.7 nM)特异性结合蛙皮素。这些发现表明,SIIA细胞拥有一种能够进行生理信号转导的胃泌素释放肽受体,尽管细胞反应尚不清楚。