ArticleProceedings of the National Academy of Sciences of the United States of America2007
Growth inhibition of non-small-cell lung carcinoma by BN/GRP antagonist is linked with suppression of K-Ras, COX-2, and pAkt.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 28 citations in OpenAlex.
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- Anti-proliferative, pro-apoptotic and anti-invasive effect of EC/EV system in human osteosarcoma.Oncotarget · 2017Article
- Role of cyclooxygenase-2 in gastric cancer development and progression.World journal of gastroenterology · 2013Review
- Shrinkage of experimental benign prostatic hyperplasia and reduction of prostatic cell volume by a gastrin-releasing peptide antagonist.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Combination of gastrin-releasing peptide antagonist with cytotoxic agents produces synergistic inhibition of growth of human experimental colon cancers.Cell cycle (Georgetown, Tex.) · 2012Article
- Gastrin-releasing peptide receptors in the central nervous system: role in brain function and as a drug target.Frontiers in endocrinology · 2012Article
- Increased expression of 14-3-3β promotes tumor progression and predicts extrahepatic metastasis and worse survival in hepatocellular carcinoma.The American journal of pathology · 2011Article
- Regulation of bombesin-stimulated cyclooxygenase-2 expression in prostate cancer cells.BMC molecular biology · 2011Article
- Anticancer activity of Noscapine, an opioid alkaloid in combination with Cisplatin in human non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands) · 2011Article
- Bombesin receptor-mediated imaging and cytotoxicity: review and current status.Current drug delivery · 2011Review
- Gastrin-releasing peptide links stressor to cancer progression.Journal of cancer research and clinical oncology · 2010Review
- Regression of murine lung tumors by the let-7 microRNA.Oncogene · 2010Article
- [Small cell lung cancer: pathology and molecular pathology].Der Pathologe · 2009Article
- Expression of GRP and its receptor is associated with improved survival in patients with colon cancer.Clinical & experimental metastasis · 2009Article
- Design, synthesis, and biological evaluation of an antagonist-bombesin analogue as targeting vector.Bioconjugate chemistry · 2008Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bombesin (BN) or gastrin-releasing peptide (GRP) can stimulate the growth of neoplasms such as breast cancer and small-cell lung carcinoma (SCLC). Antagonists of BN/GRP have been shown to inhibit these cancers. We evaluated whether antagonists of BN/GRP can suppress the growth of human non-SCLC (NSCLC) xenografted into nude mice. The effect of the administration of BN/GRP antagonist RC-3940-II on the growth of H460 and A549 NSCLC cell lines orthotopically xenografted into the intrapulmonary interstitium was examined. Protein levels of K-Ras, COX-2, Akt/pAkt, WT p53, Erk1/2, and lung resistance-related protein (LRP) in tumors were analyzed by Western blot analaysis, and receptors for BN/GRP were investigated by radioligand-binding studies. The effect of RC-3940-II on the proliferation of H460 and A549 cells in vitro was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assays. High-affinity receptors for BN/GRP were found on tumors. Treatment with RC-3940-II significantly (P < 0.001) inhibited growth of H460 and A549 NSCLC xenografts by 30-50% and led to an improved performance status, compared with controls. In H460 NSCLC, the antitumor effect was associated with a significant (P < 0.001) reduction in protein levels of K-Ras, COX-2, pAkt, and pERK1/2 and with a major augmentation in the expression of WT p53, compared with controls. In A549 NSCLC, pAkt and LRP were significantly down-regulated. Our findings demonstrate the efficacy of BN/GRP antagonist RC-3940-II for the treatment of NSCLC. The suppression of K-Ras, COX-2, pAkt, and LRP, as well as the up-regulation of WT p53 might contribute to the antitumor action of BN/GRP antagonists.
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