Presence of receptors for bombesin/gastrin-releasing peptide and mRNA for three receptor subtypes in human prostate cancers

Sun, Baodong; Halmos, Gábor; Schally, Andrew V.; Wang, Xiaofei; Martínez, Miriam

doi:10.1002/(sici)1097-0045(20000301)42:4<295::aid-pros7>3.0.co;2-b

Cited by 157 publications

(80 citation statements)

References 33 publications

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“…Prostate tumours overexpress GRP receptors [11,14,[18][19][20][21]. In an autoradiographic study, Markwalder and Reubi found the GRP receptor to be expressed in high density on invasive prostate carcinomas and proliferative intraepithelial prostate lesions, mostly prostatic intraepithelial neoplasias, whereas normal prostate tissue and, in most cases, hyperplastic prostate tissue were GRP receptornegative [14].…”

supporting

confidence: 54%

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Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Visser

Bernard

Erion

et al. 2007

Eur J Nucl Med Mol Imaging

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Purpose It has been shown that some primary human tumours and their metastases, including prostate and breast tumours, overexpress gastrin-releasing peptide (GRP) (5-14)), was tested in vivo in biodistribution studies using rats bearing GRP receptor-expressing CA20948 tumours, and nude mice bearing human PC3 xenografts. Injection of 111In-labelled Cmp 3 in these animals showed high, receptor-mediated uptake in receptor-positive organs and tumours which could be visualised using planar gamma camera and microSPECT/CT imaging. Conclusion With their enhanced receptor affinity and their rapid receptor-mediated internalisation in vitro and in vivo, the new BN analogues, and especially Cmp 3, are promising candidates for use in diagnostic molecular imaging and targeted radionuclide therapy of GRP receptor-expressing cancers.

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supporting

confidence: 54%

“…BN receptors are expressed in high densities on several primary human tumours and their metastases, including prostate, breast, small cell lung and pancreatic cancers [9][10][11][12][13][14][15][16]. Prostate cancer is the most frequently diagnosed malignancy and the third leading cause of cancer mortality among men in the Western world [17].…”

mentioning

confidence: 99%

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Visser

Bernard

Erion

et al. 2007

Eur J Nucl Med Mol Imaging

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“…More than 50% of SCLC and NSCLC cell lines express elevated levels of GRP or GRPR (Sorenson et al, 1982;Alexander et al, 1988;Siegfried et al, 1998;). Sun et al reported that approximately 60% of primary prostate cancer cells express GRPR (Sun et al, 2000a). In vitro and in vivo ablation of the GRP/GRPR autocrine pathway using a GRP neutralizing antibody or bombesin analogs resulted in the inhibition of tumor growth in preclinical models of SCLC, NSCLC and prostate cancer in addition to HNSCC (Kelley et al, 1997;Siegfried et al, 1999;Plonowski et al, 2000).…”

Section: Discussionmentioning

confidence: 99%

“…Overexpression of GRPR has been shown to promote proliferation in Balb/3T3 and Rat-1 fibroblasts (Lach et al, 1995;Feldman et al, 1996). Upregulation of GRP/GRPR, or BLP receptors and their ligands have been reported in various cancers including carcinomas of the lung (both small cell lung carcinoma and nonsmall cell lung carcinoma), prostate, colon, kidney, breast and ovary, as well as glioblastoma (Halmos et al, 1995;Sharif et al, 1997;Siegfried et al, 1999;Carroll et al, 2000;Pansky et al, 2000;Rounseville & Davis, 2000;Sun et al, 2000a, b). GRP/GRPR has been shown to contribute to lung carcinogenesis by autocrine growth stimulation.…”

Section: Introductionmentioning

confidence: 99%

Mitogenic effects of gastrin-releasing peptide in head and neck squamous cancer cells are mediated by activation of the epidermal growth factor receptor

et al. 2003

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Head and neck squamous cell carcinomas (HNSCC) are characterized by upregulation of the epidermal growth factor receptor (EGFR), where EGFR serves as a potential therapeutic target. We previously reported that a gastrin-releasing peptide/gastrin-releasing peptide receptor (GRP/GRPR) autocrine growth pathway is activated early in HNSCC carcinogenesis. In the present study, we examined the mechanism of EGFR activation by GRP/GRPR in HNSCC proliferation. In HNSCC cells that express elevated levels of both GRPR and EGFR, we found that GRP induced rapid phosphorylation of EGFR as well as p44/42-MAPK activation. Using several EGFR-specific tyrosine kinase inhibitors and cells derived from EGFR knockout mice, we demonstrated that GRPinduced p44/42-MAPK activation was dependent upon EGFR activation. Further investigation demonstrated that cleavage of transforming growth factor-alpha (TGF-a) by matrix metalloproteinases mediated GRP-induced MAPK activation. In addition, HNSCC proliferation stimulated by GRP was eliminated upon specific inhibition of EGFR or MEK, and GRP failed to stimulate proliferation in EGFR-deficient cells. These results imply that the mitogenic effects of GRP in HNSCC are mediated by extracellular release of TGF-a and require the activation of an EGFR-dependent MEK/MAPK-dependent pathway.

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“…These neuroendocrine cells express a variety of bioactive neuropeptides including GRP. A number of studies document the elevated expression of GRP receptors in prostate cancer specimens (Bartholdi et al, 1998;Markwalder and Reubi, 1999;Sun et al, 2000a) and on cultured prostatic cancer cell lines (Aprikian et al, 1996), supporting a paracrine role for GRP in prostate cancer progression.…”

Section: Bombesin-like Peptidesmentioning

confidence: 99%

Autocrine and paracrine signaling through neuropeptide receptors in human cancer

2001

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Autocrine and paracrine signaling leading to stimulation of tumor cell growth is a common theme in human cancers. In addition to polypeptide growth factors such as EGF family members which signal through receptor tyrosine kinases, accumulating evidence supports the autocrine and paracrine involvement of speci®c neuropeptides with de®ned physiologic actions as neurotransmitters and gut hormones in lung, gastric, colorectal, pancreatic and prostatic cancers. These neuropeptides, including gastrin-releasing peptide, neuromedin B, neurotensin, gastrin, cholecystokinin and arginine vasopressin bind seven transmembrane-spanning receptors that couple to heterotrimeric G proteins. Studies with human small cell lung cancer (SCLC) cells support a requirement for balanced signaling through G q and G 12/13 proteins leading to intracellular Ca 2+ mobilization, PKC activation and regulation of the ERK and JNK MAP kinase pathways. While speci®c neuropeptide antagonists o er promise for interrupting the single neuropeptide autocrine systems operating in pancreatic and prostatic cancers, SCLC is exempli®ed by multiple, redundant neuropeptide autocrine systems such that tumor growth cannot be inhibited with a single speci®c antagonist. However, a novel class of neuropeptide derivatives based on the substance P sequence have been de®ned that exhibit broad speci®city for neuropeptide receptors and induce apoptosis in SCLC by functioning as biased agonists that stimulate discordant signal transduction. Thus, interruption of autocrine and paracrine neuropeptide signaling with speci®c antagonists or broad-spectrum biased agonists o er promising new therapeutic approaches to the treatment of human cancers. Oncogene (2001) 20, 1563 ± 1569.

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Presence of receptors for bombesin/gastrin-releasing peptide and mRNA for three receptor subtypes in human prostate cancers

Cited by 157 publications

References 33 publications

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Mitogenic effects of gastrin-releasing peptide in head and neck squamous cancer cells are mediated by activation of the epidermal growth factor receptor

Autocrine and paracrine signaling through neuropeptide receptors in human cancer

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