Lee M, Jensen R T, Huang S C, Bepler G, Korman L, Moody T W
Department of Biochemistry and Molecular Biology, George Washington University School of Medicine and Health Sciences, Washington, DC 20037.
Peptides. 1990 Nov-Dec;11(6):1205-9. doi: 10.1016/0196-9781(90)90153-v.
Vasoactive intestinal polypeptide (VIP) receptors were characterized on non-small cell lung cancer (NSCLC) cells. 125I-VIP bound specifically to membranes derived from 6 NSCLC cell lines. Specific 125I-VIP was time dependent and a linear function of EPLC-65H membrane concentration. 125I-VIP bound with high (Kd = 0.2 nM) and moderate (Kd = 39 nM) affinity to two classes of sites. Pharmacology studies indicated that the order of peptide potency was VIP greater than rGHRH greater than PHI = helodermin greater than secretin greater than glucagon. Also VIP elevated the cAMP levels 10-fold using cell line ADLC-5M2. These data indicate that functional VIP receptors are present on NSCLC cells.
对非小细胞肺癌(NSCLC)细胞上的血管活性肠肽(VIP)受体进行了特性分析。125I-VIP特异性结合于源自6种NSCLC细胞系的细胞膜。特异性125I-VIP与时间相关,并且是EPLC-65H膜浓度的线性函数。125I-VIP以高亲和力(Kd = 0.2 nM)和中等亲和力(Kd = 39 nM)结合两类位点。药理学研究表明,肽的效力顺序为VIP大于rGHRH大于PHI = 海蟾蜍肽大于促胰液素大于胰高血糖素。此外,使用细胞系ADLC-5M2时,VIP使cAMP水平升高了10倍。这些数据表明NSCLC细胞上存在功能性VIP受体。