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血管活性肠肽与非小细胞肺癌细胞高亲和力结合并提高环磷酸腺苷水平。

Vasoactive intestinal polypeptide binds with high affinity to non-small cell lung cancer cells and elevates cyclic AMP levels.

作者信息

Lee M, Jensen R T, Huang S C, Bepler G, Korman L, Moody T W

机构信息

Department of Biochemistry and Molecular Biology, George Washington University School of Medicine and Health Sciences, Washington, DC 20037.

出版信息

Peptides. 1990 Nov-Dec;11(6):1205-9. doi: 10.1016/0196-9781(90)90153-v.

Abstract

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.

摘要

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。

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