(STEARYL, NORLEUCINE(17))VIP HYBRID ANTAGONIZES VIP RECEPTORS ON NONSMALL CELL LUNG-CANCER CELLS

Authors
MOODY TW LEYTON J COELHO T JAKOWLEW S TAKAHASHI K JAMEISON F KOH M FRIDKIN M GOZES I KNIGHT M
Citation
Tw. Moody et al., (STEARYL, NORLEUCINE(17))VIP HYBRID ANTAGONIZES VIP RECEPTORS ON NONSMALL CELL LUNG-CANCER CELLS, Life sciences, 61(17), 1997, pp. 1657-1666
Citations number
27
Categorie Soggetti
Biology,"Medicine, Research & Experimental","Pharmacology & Pharmacy
Journal title
Life sciences → ACNP
ISSN journal
00243205
Volume
61
Issue
17
Year of publication
1997
Pages
1657 - 1666
Database
ISI
SICI code
0024-3205(1997)61:17<1657:(NHAVR>2.0.ZU;2-9
Abstract
The effects of VIP receptor antagonists were investigated using non-sm all cell lung cancer (NSCLC) cells. By Northern blot and RT-PCR, VIP, receptors were detected on NSCLC cell line NCI-H1299. VIPhybrid,(N-Ste aryl-Norleucine(17)) VIPhybrid ((SN)VIPhybrid) and PTC4495 inhibited I -125-VIP binding to NCI-H1299 cells with IC50 values of 500, 30 and 50 00 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. Th ese data suggest that (SN)VIPhybrid antagonizes VIP, receptors on NSCL C cells.