Luis J, Said S I
University of Illinois, Chicago.
Peptides. 1990 Nov-Dec;11(6):1239-44. doi: 10.1016/0196-9781(90)90158-2.
We investigated the molecular and pharmacologic characteristics of VIP receptors on two human SCLC cell lines: NCI-N592 and NCI-H345. With NCI-N592 cell, the order of potency of VIP-related peptides in inhibiting 125I-VIP binding and in stimulating cAMP production was typical of the human VIP receptor. By covalent cross-linking, a polypeptide of Mr 62,300 was obtained. Conversely, the behavior of NCI-H345 cell line was totally different: helodermin was the most potent peptide, VIP and PHI were equipotent, while hGRF and secretin were totally ineffective. These results suggest that NCI-N592 cells possess a typical VIP receptor while NCI-H345 cells possess a helodermin-preferring receptor, and that the natural target of helodermin might not be the VIP receptor.
我们研究了两种人小细胞肺癌(SCLC)细胞系NCI-N592和NCI-H345上血管活性肠肽(VIP)受体的分子和药理学特性。对于NCI-N592细胞,VIP相关肽在抑制125I-VIP结合和刺激环磷酸腺苷(cAMP)产生方面的效力顺序是典型的人VIP受体。通过共价交联,获得了一个分子量为62300的多肽。相反,NCI-H345细胞系的表现完全不同:胃泌素释放肽(helodermin)是最有效的肽,VIP和胰高血糖素样肽I(PHI)效力相当,而人促生长激素释放因子(hGRF)和促胰液素完全无效。这些结果表明,NCI-N592细胞具有典型的VIP受体,而NCI-H345细胞具有偏向胃泌素释放肽的受体,并且胃泌素释放肽的天然靶点可能不是VIP受体。