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Margarita Stampelou, Graham Ladds, and Antonios Kolocouris refine AlphaFold models using binding calculations

a clearly defined biological question and the careful selection of a physiologically relevant cell model

GPCRs play a central role in neuronal signaling and have been used to treat these diseases with varying membrane of cells, they have easier access to the receptors than those that need to get into the cells to modulate The activation of these pathways regulates pain modulation, memory consolidation, motor coordination

begins first-in-human trial of SEP-631 for CSU; Maxion’s KnotBody® platform; a new angle on RGS protein modulation Must-read publications:  From on stabilizing RGS2 via modulating its degradation (versus direct inhibition

Through genetic and pharmacologic modulations of GRK3, a series of functional and molecular studies were

suggest that class B1 GPCRs can form both homodimers and heterodimers, which may play a crucial role in modulating also opens new avenues for developing therapeutic agents that target specific receptor dimer states to modulate

self-secreted by yeast expressing a G-protein-coupled receptor Reviews, GPCRs, and more The GLP-1R as a model

TRV045 is the Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic

; whether they regulate intracellular cyclic AMP (cAMP) and calcium concentrations ([Ca2+]i), which modulate These findings suggest that the melatonin MT2 receptor is expressed in ASM, and modulates airway smooth

Expression Ligand bias at the muscarinic acetylcholine receptor family: opportunities and challenges Modulating Industry News Confo Therapeutics Announces EUR 60M Series B Financing to Advance a Pipeline of Novel GPCR-Modulating

GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival.

Thal , et al., for their groundbreaking work on Positive allosteric modulation of a GPCR ternary complex promotes pressure overload-induced heart failure GPCR Activation and Signaling Positive allosteric modulation

Dopamine receptors are involved in the modulation of fundamental physiological functions, and dysregulation

🎉 Conformational coupling between extracellular and transmembrane domains modulates holo-adhesion GPCR Structural Biologist Adhesion GPCRs Conformational coupling between extracellular and transmembrane domains modulates pathways segregates the orexigenic activity from the control of whole-body glucose metabolism by AGRP Neurons agonists using virtual screening, molecular docking and dynamics simulation studies GPCRs in Neuroscience Neuronal sea cucumber Apostichopus japonicus: Ultrastructure and transcriptional profile Adult single-nucleus neuronal

Networks within Disease-Associated GαS Variants Characterized by an Integrative Biophysical Approach Redox-modulated mechanism of the proton-sensing GPR68 receptor Astrocytic GPCR signaling in the anterior cingulate cortex modulates

PTK7 is a positive allosteric modulator of GPR133 signaling in glioblastoma. Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y4 Receptor Positive Allosteric Modulator

Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor

Therapeutics (SIX and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based

Negative allosteric modulation of the glucagon receptor by RAMP2. Regulator of G-Protein Signalling 4 (RGS4) negatively modulates nociceptin/orphanin FQ opioid receptor more Predicting allosteric sites using fast conformational sampling as guided by coarse-grained normal modes Neuronal activity-induced, equilibrative nucleoside transporter-dependent, somatodendritic adenosine The impact of cryo-EM on determining allosteric modulator-bound structures of G protein-coupled receptors

Nanobody binding stabilizes G-protein-coupled receptors (GPCR) in a fully active state and modulates transmission mechanisms between the Nb80-binding site and the extracellular domains in conformations modulated

converted by hair cells in the cochlea into electrical signals, which are transmitted by spiral ganglion neurons Moreover, Frizzleds and Celsrs have been demonstrated to play core roles in the modulation of cochlear

Simulations show how two ligands differently activate class A GPCR NMBR, with allosteric communication hubs modulating

Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor Bound to a Negative Allosteric Modulator

company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs) with a novel drug modality

However, progress in this area has led to an increase in studies that have begun modulating neuropeptide

Rho-Kinase 2 Signaling to Manage Motoneuron Excitability Intrinsic membrane excitability (IME) sets up neuronal neuromodulators, acting through G-protein-coupled receptors (GPCRs), fine-tune motoneuron (MN) IME by modulating However, intracellular partners linking GPCRs to TASK1 modulation are not yet well-known.

Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor "Modulators

Must-read publications:  New insights on RGS protein modulation, GRK2-biased β₂AR signaling, and the If you’re not there, you’re missing out on the next wave of allosteric modulators, biased ligands, and

the intracellular loops of G protein-coupled receptors (GPCRs) that act in an allosteric manner to modulate

roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R activation in gut IELs to modulation