AH6809 antagonizes non-small cell lung cancer prostaglandin receptors

被引:15
作者
Casibang, M [1 ]
Moody, TW [1 ]
机构
[1] NCI, Cell & Canc Biol Dept, Med Branch, Rockville, MD 20850 USA
关键词
PGE(2); receptor binding; NSCLC; AH6809; proliferation;
D O I
10.1016/S0169-5002(01)00476-7
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
The effects of prostaglandin (PG)E-2 on lung cancer cells were investigated. H-3-PGE, bound with high affinity to membranes derived from small cell lung cancer (SCLC) and non-SCLC (NSCI-C) cell lines. Using NSCLC NCI-H1299 membranes, specific H-3-PGE, binding to NCI-H1299 membranes was inhibited with moderate affinity by PGE(2), PGE(1), PGF(2alpha) and 6-isopropoxy-9-xanthone-2-carboxylic acid (AH6809) but not PGD(2), LTB4 or 5-HETE. By RT-PCR, EP2 receptor PCR products were detected in extracts derived from lung cancer cells. PGE(2) caused cAMP elevation in a concentration-dependent manner using NCI-H1299 cells and the increase in cAMP caused by PGE(2) was antaconized by AH6809. PGE(2) had no effect on cytosolic Ca2+ but PGE(2) caused increased c-fos mRNA in NCI-H1299 cells. AH6809 inhibited the proliferation of NCI-H1299 cells using MTT and clonogenic assays. These results indicate that functional PG receptors are present on NSCLC cells which are antagonized by AH6809. Published by Elsevier Science Ireland Ltd.
引用
收藏
页码:33 / 42
页数:10
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