title: G protein-coupled receptors as oncogenic signals in glioma: emerging therapeutic avenues.
abstract: Gliomas are the most common malignant intracranial tumors. Newly developed targeted therapies for these cancers aim to inhibit oncogenic signals, many of which emanate from receptor tyrosine kinases, including the epidermal growth factor receptor (EGFR) and the vascular endothelial growth factor receptor (VEGFR). Unfortunately, the first-generation treatments targeting these oncogenic signals provide little survival benefit in both mouse xenograft models and human patients. The search for new treatment options has uncovered several G protein-coupled receptor (GPCR) candidates and generated a growing interest in this class of proteins as alternative therapeutic targets for the treatment of various cancers, including glioblastoma multiforme (GBM). GPCRs constitute a large family of membrane receptors that influence oncogenic pathways through canonical and non-canonical signaling. Accordingly, evidence indicates that GPCRs display a unique ability to crosstalk with receptor tyrosine kinases, making them important molecular components controlling tumorigenesis. This review summarizes the current research on GPCR functionality in gliomas and explores the potential of modulating these receptors to treat this devastating disease.
authors.affiliation: Department of Pharmacology, University of Washington, 1959 NE Pacific Street, BB1538, Health Sciences Building, Seattle, WA 98195, United States. Electronic address: aecherry@uw.edu.
authors.forename: A E
authors.initials: AE
authors.lastname: Cherry
authors.affiliation: Department of Pharmacology, University of Washington, 1959 NE Pacific Street, BB1538, Health Sciences Building, Seattle, WA 98195, United States; Department of Psychiatry & Behavioral Sciences, University of Washington, 1959 NE Pacific Street, BB1538, Health Sciences Building, Seattle, WA 98195, United States. Electronic address: nstella@uw.edu.
authors.forename: N
authors.initials: N
authors.lastname: Stella
mesh_terms: D000818:Animals; D001932:Brain Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D005909:Glioblastoma / Q000188:drug therapy / Q000378:metabolism*; D006801:Humans; D051379:Mice; D051381:Rats; D020794:Receptor Protein-Tyrosine Kinases / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D043562:Receptors, G-Protein-Coupled; D020794:Receptor Protein-Tyrosine Kinases
keywords: G protein-coupled receptor; astrocytoma; glioblastoma multiforme; receptor tyrosine kinase