(Stearyl, Norleucine(17))VIP hybrid antagonizes VIP receptors on non-small cell lung cancer cells

被引：34

作者：

Moody, TW

Leyton, J

Coelho, T

Jakowlew, S

Takahashi, K

Jameison, F

Koh, M

Fridkin, M

Gozes, I

Knight, M

机构：

[1] PEPTIDE TECHNOL, GAITHERSBURG, MD 20877 USA

[2] UNIV MARYLAND, SCH MED, DEPT OPHTHALMOL, BALTIMORE, MD 21201 USA

[3] WEIZMANN INST SCI, DEPT ORGAN CHEM, IL-76100 REHOVOT, ISRAEL

[4] SACKLER SCH MED, DEPT CLIN BIOCHEM, TEL AVIV, ISRAEL

来源：

LIFE SCIENCES | 1997年 / 61卷 / 17期

关键词：

VIP receptor antagonists; non-small cell lung cancer; cAMP; (S; N); VIPhybrid; cell proliferation;

D O I：

10.1016/S0024-3205(97)00771-6

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

The effects of VIP receptor antagonists were investigated using non-small cell lung cancer (NSCLC) cells. By Northern blot and RT-PCR, VIP, receptors were detected on NSCLC cell line NCI-H1299. VIPhybrid,(N-Stearyl-Norleucine(17)) VIPhybrid ((SN)VIPhybrid) and PTC4495 inhibited I-125-VIP binding to NCI-H1299 cells with IC50 values of 500, 30 and 5000 nM respectively. (SN)VIPhybrid (1 mu M) had no effect on basal cAMP but strongly inhibited the increase in cAMP caused by 10 nM VIP. The order of peptide potency to inhibit cAMP was (SN)VIPhybrid > VIPhybrid > PTC4495. (SN)VIPhybrid was more potent than VIPhybrid at inhibiting NCI-H1299 colony formation. Also, (SN)VIPhybrid was more potent than VIPhybrid at inhibiting NCI-H1299 xenograft formation in nude mice. These data suggest that (SN)VIPhybrid antagonizes VIP, receptors on NSCLC cells.

引用

页码：1657 / 1666

页数：10

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