Potential therapeutic targeting of BKCa channels in glioblastoma treatment
Molecular Oncology, EarlyView.This review summarizes current insights into the role of BKCa and mitoBKCa channels in glioblastoma biology, their potential classification as oncochannels, and the emerging pharmacological strategies targeting these channels, emphasizing the translational challenges in developing BKCa‐directed therapies for glioblastoma treatment.
Kamila Maliszewska‐Olejniczak +4 more
wiley +1 more source
M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]
, 2017 Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity.
Alvarez-Curto, Elisa +2 more
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SLAS DiscoveryBioluminescence- and fluorescence-based resonance energy transfer assays have gained considerable attention in pharmacological research as high-throughput scalable tools applicable to drug discovery. To this end, G protein-coupled receptors represent the
Joanna J. Sajkowska +2 more
doaj +1 more source
Discovery of new G protein-coupled receptors for lipid mediators
Journal of Lipid Research, 2004 Successful sequencing of the human genome has opened a new era in the life sciences and has greatly accelerated biomedical research. Among various research endeavors benefiting from established genomic information, one of the most fruitful areas is the ...
Dong-Soon Im
doaj +1 more source
Exploiting metabolic adaptations to overcome dabrafenib treatment resistance in melanoma cells
Molecular Oncology, EarlyView.We show that dabrafenib‐resistant melanoma cells undergo mitochondrial remodeling, leading to elevated respiration and ROS production balanced by stronger antioxidant defenses. This altered redox state promotes survival despite mitochondrial damage but renders resistant cells highly vulnerable to ROS‐inducing compounds such as PEITC, highlighting redox
Silvia Eller +17 more
wiley +1 more source
Representation Learning for Class C G Protein-Coupled Receptors Classification
Molecules, 2018 G protein-coupled receptors (GPCRs) are integral cell membrane proteins of relevance for pharmacology. The complete tertiary structure including both extracellular and transmembrane domains has not been determined for any member of class C GPCRs.
Raúl Cruz-Barbosa +2 more
doaj +1 more source
Cell surface interactome analysis identifies TSPAN4 as a negative regulator of PD‐L1 in melanoma
Molecular Oncology, EarlyView.Using cell surface proximity biotinylation, we identified tetraspanin TSPAN4 within the PD‐L1 interactome of melanoma cells. TSPAN4 negatively regulates PD‐L1 expression and lateral mobility by limiting its interaction with CMTM6 and promoting PD‐L1 degradation.
Guus A. Franken +7 more
wiley +1 more source
LDAcoop: Integrating non‐linear population dynamics into the analysis of clonogenic growth in vitro
Molecular Oncology, EarlyView.Limiting dilution assays (LDAs) quantify clonogenic growth by seeding serial dilutions of cells and scoring wells for colony formation. The fraction of negative wells is plotted against cells seeded and analyzed using the non‐linear modeling of LDAcoop.
Nikko Brix +13 more
wiley +1 more source
G protein-coupled receptors: Role in metabolic disorders
Frontiers in Endocrinology, 2022 Luiz F. Barella, Shanu Jain, Sai P. Pydi
doaj +1 more source
Evidence that neuronal G-protein-gated inwardly rectifying K+ channels are activated by Gβγ subunits and function as heteromultimers [PDF]
, 1995 Guanine nucleotide-binding proteins (G proteins) activate K+ conductances in cardiac atrial cells to slow heart rate and in neurons to decrease excitability. cDNAs encoding three isoforms of a G-protein-coupled, inwardly rectifying K+ channel (GIRK) have
Davidson, Norman +2 more
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