Abstract
G-protein-coupled receptors (GPCRs) are increasingly being considered as possible therapeutic targets in cancers. Activation of GPCR on tumors can have prominent growth effects, and GPCRs are frequently over-/ectopically expressed on tumors and thus can be used for targeted therapy. CNS/neural tumors are receiving increasing attention using this approach. Gliomas are the most frequent primary malignant brain/CNS tumor with glioblastoma having a 10-year survival <1%; neuroblastomas are the most common extracranial solid tumor in children with long-term survival<40%, and medulloblastomas are less common, but one subgroup has a 5-year survival <60%. Thus, there is an increased need for more effective treatments of these tumors. The Bombesin-receptor family (BnRs) is one of the GPCRs that are most frequently over/ectopically expressed by common tumors and is receiving particular attention as a possible therapeutic target in several tumors, particularly in prostate, breast, and lung cancer. We review in this paper evidence suggesting why a similar approach in some CNS/neural tumors (gliomas, neuroblastomas, medulloblastomas) should also be considered.
Highlights
G-protein-coupled receptors (GPCRs) are increasingly being considered as possible therapeutic targets in cancer [1,2,3]
Gliomas: Bn/bombesin receptor (BnR) Related to Prognosis, Treatment In studies with experimental gliomas, the treatment with Gastrinreleasing peptide receptor (GRPR) antagonists increased the survival time by inhibiting the growth of xenografts of human glioblastomas cell lines (U-87G,U373MG) in nude mice [159, 160]
In contrast to the growth inhibitory effect of higher concentrations of cetuximab in the medulloblastoma cell line DAOY, neither the addition of neuromedin B (NMB) nor the Neuromedin B receptor (NMBR) antagonist BIM-23127 had an effect on the cell line’s growth or viability when present alone [215]. These results suggested that NMBR activation alone does not affect DAOY medulloblastoma cell line’s viability, but instead could potentiate the growth inhibitory effect of EGFR blockade due to the addition of cetuximab [213]
Summary
G-protein-coupled receptors (GPCRs) are increasingly being considered as possible therapeutic targets in cancer [1,2,3]. One study [153] investigated the mRNA expression levels of each of the human BnRs (GRPR, NMBR, BRS-3) in recurrent gliomas in nine patients.
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