ArticleThe Biochemical journal2006
Galphaq binds to p110alpha/p85alpha phosphoinositide 3-kinase and displaces Ras.
Article in The Biochemical journal, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 38 citations in OpenAlex.
- Mechanistic Insights into the Anticancer Potential of Methoxyflavones Analogs: A Review.Molecules (Basel, Switzerland) · 2025Review
- Neuroprotection against beta-amyloid toxicity by the novel estrogen receptor modulator STX requires convergent signaling pathways.Frontiers in molecular neuroscience · 2025Article
- Going Rogue: Mechanisms, Regulation, and Roles of Mutationally Activated GMolecular pharmacology · 2024Review
- Targeting PI3K/Akt signal transduction for cancer therapy.Signal transduction and targeted therapy · 2021Review
- Calcium-containing scaffolds induce bone regeneration by regulating mesenchymal stem cell differentiation and migration.Stem cell research & therapy · 2017Article
- Activation of Gαq in Cardiomyocytes Increases Vps34 Activity and Stimulates Autophagy.Journal of cardiovascular pharmacology · 2017Article
- Control of cardiac repolarization by phosphoinositide 3-kinase signaling to ion channels.Circulation research · 2015Review
- PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting.Nature reviews. Cancer · 2015Review
- Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11.Frontiers in cardiovascular medicine · 2015Review
- G protein-coupled receptors and the regulation of autophagy.Trends in endocrinology and metabolism: TEM · 2014Review
- The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells.Molecular cancer therapeutics · 2014Article
- Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner.Clinical cancer research : an official journal of the American Association for Cancer Research · 2012Article
- Genetic and molecular characterization of uveal melanoma cell lines.Pigment cell & melanoma research · 2012Article
- The interferon-gamma-induced murine guanylate-binding protein-2 inhibits rac activation during cell spreading on fibronectin and after platelet-derived growth factor treatment: role for phosphatidylinositol 3-kinase.Molecular biology of the cell · 2010Article
- The emerging mechanisms of isoform-specific PI3K signalling.Nature reviews. Molecular cell biology · 2010Review
- Phosphoinositide 3-kinase mediated signaling in lobster olfactory receptor neurons.Journal of neurochemistry · 2010Article
- The effect of membrane domains on the G protein-phospholipase Cbeta signaling pathway.Critical reviews in biochemistry and molecular biology · 2010Review
- Gq-coupled purinergic receptors inhibit insulin-like growth factor-I/phosphoinositide 3-kinase pathway-dependent keratinocyte migration.Molecular biology of the cell · 2010Article
- Galphaq binds two effectors separately in cells: evidence for predetermined signaling pathways.Biophysical journal · 2008Article
- Signaling and cross-talk by C5a and UDP in macrophages selectively use PLCbeta3 to regulate intracellular free calcium.The Journal of biological chemistry · 2008Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Several studies have reported that activation of G(q)-coupled receptors inhibits PI3K (phosphoinositide 3-kinase) signalling. In the present study, we used purified proteins to demonstrate that Galpha(q) directly inhibits p110alpha/p85alpha PI3K in a GTP-dependent manner. Activated Galpha(q) binds to the p110alpha/p85alpha PI3K with an apparent affinity that is seven times stronger than that for Galpha(q).GDP as measured by fluorescence spectroscopy. In contrast, Galpha(q) did not bind to the p110gamma PI3K. Fluorescence spectroscopy experiments also showed that Galpha(q) competes with Ras, a PI3K activator, for binding to p110alpha/p85alpha. Interestingly, co-precipitation studies using deletion mutants showed that Galpha(q) binds to the p85-binding domain of p110alpha and not to the Ras-binding domain. Expression of constitutively active Galpha(q)Q209L in cells inhibited Ras activation of the PI3K/Akt pathway but had no effect on Ras/Raf/MEK [MAPK (mitogen-activated protein kinase)/ERK (extracellular-signal-regulated kinase) kinase] signalling. These results suggest that activation of G(q)-coupled receptors leads to increased binding of Galpha(q).GTP to some isoforms of PI3K, which might explain why these receptors inhibit this signalling pathway in certain cell types.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.