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249 items found for "homology modeling"
- 📰 GPCR Weekly News, June 5 to 11, 2023
Statin-induced increase in actin polymerization modulates GPCR dynamics and compartmentalization. The G protein-coupled receptor neuropeptide receptor-15 modulates larval development via the transforming of pre-existing neurotensin receptor conformational states by β-arrestin-1 and the biased allosteric modulator
- Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the ...
Caenorhabditis elegans was used as an animal model, and both gene expression and functional analysis
- Functional Characterization of the Venus Flytrap Domain of the Human TAS1R2 Sweet Taste Receptor
family of class C GPCRs whose members share the same architecture, comprising a Venus Flytrap (VFT) module The VFT module of TAS1R2 contains the primary binding site for most of the sweet-tasting compounds, including
- Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembra
Here, we examined the mode of action of positive allosteric modulators (PAMs) that bind at the interface Overall, these data reveal the possibility of developing allosteric compounds able to specifically modulate
- The integrin ligand SVEP1 regulates GPCR-mediated vasoconstriction via integrins α9β1 and α4β1
Several integrins directly modulate VSMC contraction by regulating calcium influx through L-type voltage-gated
- 📰 GPCR Weekly News, January 16 to 22, 2023
stimulates the Akt-mTOR axis and in vivo muscle protein synthesis in a dexamethasone-induced muscle atrophy model
- 📰 GPCR Weekly News - January 9 to 15, 2023
GPCR Binders, Drugs, and more Modelling altered signalling of G-protein coupled receptors in inflamed
- Addex Therapeutics To Release Full-Year 2021 Financial Results And Host Conference Call On March 10
Therapeutics (SIX: ADXN, Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based
- 📰 GPCR Weekly News, March 11 to 17, 2024
Disparate Effects on Islet Insulin Secretion and Content in β-cells in a High Fat Diet-induced Mouse Model
- 📰 GPCR Weekly News, March 13 to 19, 2023
A Rab10-ACAP1-Arf6 GTPases cascade modulates M4 muscarinic acetylcholine receptor trafficking and signaling Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator. α1-adrenoceptor Endogenous l- to d-amino acid residue isomerization modulates selectivity between distinct neuropeptide
- GRK3 is a poor prognosticator and serves as a therapeutic target in advanced gastric adenocarcinoma
Through genetic and pharmacologic modulations of GRK3, a series of functional and molecular studies were
- Melatonin MT 2 receptor is expressed and potentiates contraction in human airway smooth muscle
; 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
- Trevena Announces Advancement of TRV045 Into Clinical Development for Diabetic Neuropathic Pain
TRV045 is the Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic
- The expression and clinical significance of GPR39 in colon cancer
GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival.
- Allosteric Effect of Nanobody Binding on Ligand-Specific Active States of the β2 Adrenergic Receptor
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
- Reversible Photocontrol of Dopaminergic Transmission in Wild-Type Animals
Dopamine receptors are involved in the modulation of fundamental physiological functions, and dysregulation
- Addex Reports 2022 Half Year and Second Quarter Financial Results and Provides Corporate Update
Therapeutics (SIX and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based
- Orion Announces The Rapid Lead Optimization Of Ob-004 - A Ccr2 Antagonist
company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs) with a novel drug modality
- Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor
- Hear the sounds: the role of G protein-coupled receptors in the cochlea
Moreover, Frizzleds and Celsrs have been demonstrated to play core roles in the modulation of cochlear
- Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage...
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.
- 📰 GPCR Weekly News, June 19 to 25, 2023
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
- 📰 GPCR Weekly News, April 8 to 14, 2024
self-secreted by yeast expressing a G-protein-coupled receptor Reviews, GPCRs, and more The GLP-1R as a model
- Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of...
Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor Bound to a Negative Allosteric Modulator
- 📰 GPCR Weekly News, March 27 to April 4, 2023
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 The impact of cryo-EM on determining allosteric modulator-bound structures of G protein-coupled receptors
- Immunomodulatory Role of Neuropeptides in the Cornea
However, progress in this area has led to an increase in studies that have begun modulating neuropeptide
- Dr. GPCR University registration is now open! Secure your spot now!
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
- GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for...
Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor "Modulators