Therapeutic use and Perspectives of Synthetic Peptides in Oncology

Prevost, Grégoire; Mormont, C.; Gunning, Martyn; Thomas, François

doi:10.3109/02841869309083914

Cited by 16 publications

(6 citation statements)

References 52 publications

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“…The biological effect of a given GPCR agonist is tentatively inhibited by a corresponding selective antagonist targeting the receptor (20)(21)(22)(23). However, the therapeutic effect of this strategy should appear limited because tumor growth is simultaneously driven by several GPCR agonists.…”

Section: Introductionmentioning

confidence: 99%

Anticancer Activity of BIM-46174, a New Inhibitor of the Heterotrimeric Gα/Gβγ Protein Complex

et al. 2006

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A large number of hormones and local agonists activating guanine-binding protein-coupled receptors (GPCR) play a major role in cancer progression. Here, we characterize the new imidazo-pyrazine derivative BIM-46174, which acts as a selective inhibitor of heterotrimeric G-protein complex. BIM-46174 prevents the heterotrimeric G-protein signaling linked to several GPCRs mediating (a) cyclic AMP generation (GAs), (b) calcium release (GAq), and (c) cancer cell invasion by Wnt-2 frizzled receptors and high-affinity neurotensin receptors (GAo/i and GAq). BIM-46174 inhibits the growth of a large panel of human cancer cell lines, including anticancer drug-resistant cells. Exposure of cancer cells to BIM-46174 leads to caspase-3-dependent apoptosis and poly(ADP-ribose) polymerase cleavage. National Cancer Institute COMPARE analysis for BIM-46174 supports its novel pharmacologic profile compared with 12,000 anticancer agents. The growth rate of human tumor xenografts in athymic mice is significantly reduced after administration of BIM-46174 combined with either cisplatin, farnesyltransferase inhibitor, or topoisomerase inhibitors. Our data validate the feasibility of targeting heterotrimeric G-protein functions downstream the GPCRs to improve anticancer chemotherapy. (Cancer Res 2006; 66(18): 9227-34)

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Section: Introductionmentioning

confidence: 99%

Anticancer Activity of BIM-46174, a New Inhibitor of the Heterotrimeric Gα/Gβγ Protein Complex

et al. 2006

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“…Generally, small neuropeptides, such as somatostatin (SST) and gastrin releasing peptide (GRP)/bombesin (BN) analogues, labelled with g -and/or b --emitting radionuclides are investigated for their ability to bind to receptors which are overexpressed in a variety of malignant tumours [14][15][16]. The affinity of the designed chelator-peptide construct to these receptors may vary depending on the metal incorporated into the complex [17].…”

Section: Introductionmentioning

confidence: 99%

Comparison of receptor affinity of natSc-DOTA-TATE versus natGa-DOTA-TATE

Koumarianou¹,

Pawlak²,

Korsak³

et al. 2011

Nucl Med Rev Cent East Eur.

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“…Prostatic carcinomas with neuroendocrine differentiation are potentially amenable to innovative therapeutic approaches, including immunotherapy (treatment with interferon, antibodies to growth promoting peptides/ neuropeptides, or antibodies to receptors for these peptides/neuropeptides), endocrine therapy (antagonist analogues to peptide/neuropeptide growth factors and/or agonist analogues to secretion and growth inhibiting peptides/neuropeptides), and specialized chemotherapy using agents more specifically targeted at and effective against neuroendocrine differentiation. 75,76 In my last review of neuroendocrine differentiation in prostate cancer,' the use of bombesin/gastrin-releasing peptide antagonist analogues and monoclonal antibodies to bombesin was reviewed. These approaches were used in vitro and in vivo against experimental small cell carcinoma model systems with encouraging results to the point that clinical trials were initiated in humans with small cell carcinoma of the lung using monoclonal antibody to bombesin.…”

Section: Potential New Therapeutic Approaches Directed Toward Neuroenmentioning

confidence: 99%

Neuroendocrine differentiation in prostatic carcinoma. Recent findings and new concepts

Sant'Agnese¹

1995

Cancer

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Neuroendocrine cells of the prostate are intraepithelial regulatory cells that probably modulate both growth and differentiation as well as the exocrine secretory process. These cells form a component of the more generalized multiorgan regulatory system known as the amine precursor uptake and decarboxylation (APUD), or dispersed neuroendocrine system. The prostatic neuroendocrine cells contain serotonin and a variety of regulatory neuroendocrine peptides. Neuroendocrine differentiation in prostatic carcinoma is manifested as the relatively rare small cell carcinoma and the much more common, if not ubiquitous, focal neuroendocrine differentiation in conventional prostatic carcinoma. Neuroendocrine differentiation may have diagnostic, prognostic, and therapeutic implications. Recent findings include the expression of parathyroid hormone‐related protein, the cnromogranin peptide family, epidermal growth factor receptor, and c‐erbB‐2 immunoreactivity by prostatic neuroendocrine cells. Immunoreactive androgen receptor is not expressed by benign or malignant prostatic neuroendocrine cells. Non‐neuroendocrine proliferation foci and bcl‐2 immunoreactive cells appear to cluster around neuroendocrine cells in prostatic carcinoma. These findings, along with additional clinical and experimental evidence, suggest that neuroendocrine cells may play a role as an independent prognostic factor in prostate cancer, particularly those that are resistant to hormonal therapy. The therapeutic implications of prostatic neuroendocrine differentiation are discussed as are potential lines of investigation. Cancer 1995;75:1850–9.

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Therapeutic use and Perspectives of Synthetic Peptides in Oncology

Cited by 16 publications

References 52 publications

Anticancer Activity of BIM-46174, a New Inhibitor of the Heterotrimeric Gα/Gβγ Protein Complex

Anticancer Activity of BIM-46174, a New Inhibitor of the Heterotrimeric Gα/Gβγ Protein Complex

Comparison of receptor affinity of natSc-DOTA-TATE versus natGa-DOTA-TATE

Neuroendocrine differentiation in prostatic carcinoma. Recent findings and new concepts

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