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584 items found for "GPCR therapeutics"
- Addex and Indivior Extend GABAB Positive Allosteric Modulator Research Collaboration for...
Modulator Research Collaboration for Substance Use Disorders "Geneva, Switzerland, August 15, 2022 - Addex Therapeutics compounds for Charcot-Marie-Tooth type 1A neuropathy (CMT1A) and pain. " Read more at the source #DrGPCR #GPCR
- High hedgehog signaling is transduced by a multikinase-dependent switch controlling the...
signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR smoothened "The oncogenic G-protein-coupled receptor (GPCR) Smoothened (SMO) is a key transducer of of HH to the apico-basal distribution of SMO and provide a novel mechanism for the regulation of a GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- OMass Therapeutics's founder, Carol Robinson, has been awarded the prestigious Louis-Jeantet ...
December 2021 OMass Therapeutics's founder, Carol Robinson, has been awarded the prestigious Louis-Jeantet #DrugDiscovery #MassSpec #Award #massspectrometry" Read more at the source #DrGPCR #GPCR #IndustryNews
- Interacting binding insights and conformational consequences of the differential activity of...
Notably, while CBD is able to antagonize some GPCRs in the endocannabinoid system, it also seems to activate we investigate the interacting determinants of CBD in two closely related endocannabinoid-activated GPCRs the CBD ligand in the GPR55 receptor elicit conformational changes associated with antagonist-bound GPCRs way for understanding the CBD pharmacology at a molecular level and aid in harnessing its potential therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews
- Functional modulation of PTH1R activation and signaling by RAMP2
ubiquitously expressed membrane proteins that associate with different G protein–coupled receptors (GPCRs ), including the parathyroid hormone 1 receptor (PTH1R), a class B GPCR and an important modulator of These data uncover a critical role of RAMPs in the activation and signaling of a GPCR that may provide a new venue for highly specific modulation of GPCR function and advanced drug design." Read more at the source #DrGPCR #GPCR #IndustryNews
- Cholesterol-Dependent Dynamics of the Serotonin 1A Receptor Utilizing Single Particle Tracking....
September 2022 "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes that regulate Serotonin1A receptors are important members of the GPCR family and are implicated in neuropsychiatric To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking results bring out the interdependence of cholesterol and actin cytoskeleton in regulating diffusion of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C...
are involved in mGlu5a receptor internalization "The internalization of G protein-coupled receptors (GPCRs Additionally, using the Gαq/11 inhibitor YM-254890, GPCR kinase 2 and 3 (GRK2 and GRK3) KO cells, and Our PKC KO cell lines expand the repertoire of KO HEK293A cell lines available to research GPCR pharmacology Read more at the source #DrGPCR #GPCR #IndustryNews
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
"Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors (GPCRs targeting the intracellular allosteric binding site (IABS) of the CC chemokine receptor 2 (CCR2), a class A GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders with ...
Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders with Tim Dyer Addex Therapeutics "Tim Dyer is the Co-Founder and CEO of Addex Therapeutics, which is focusing on the pharmacology known Read more at the source #DrGPCR #GPCR #IndustryNews
- Production of human A2AAR in lipid nanodiscs for 19F-NMR and single-molecule fluorescence...
describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Function and structure of bradykinin receptor 2 for drug discovery
October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that Read more at the source #DrGPCR #GPCR #IndustryNews
- Specific Functions of Melanocortin 3 Receptor (MC3R)
October 2022 "Melanocortin 3 receptor (MC3R) is a G-protein coupled receptor (GPCR) that is defined Read more at the source #DrGPCR #GPCR #IndustryNews
- MSX-122: Is an effective small molecule CXCR4 antagonist in cancer therapy?
C-X-C motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural Read more at the source #DrGPCR #GPCR #IndustryNews
- Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1
September 2022 "Given the promising clinical value of allosteric modulators of G protein-coupled-receptors (GPCRs ), mechanistic understanding of how these modulators alter GPCR function is of significance. Read more at the source #DrGPCR #GPCR #IndustryNews
- Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its...
ligands "The CX3C chemokine receptor 1 (CX3CR1), a member of the class A of G Protein-Coupled Receptors (GPCR patterns that characterize a functional state to contribute to the understanding of the complexity of the GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin recept
pentan-3-yl)-1-cyclopentyl-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamide hydrochloride) of this GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to...
Pathways "Adhesion G protein-coupled receptor A1 (ADGRA1) belongs to the G protein-coupled receptor (GPCR regulating the PI3K/AKT/GSK-3β and MEK/ERK pathways in amygdalae of male mice, implicating a potential, therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews
- GPR15 expressed in T lymphocytes from RA patients is involved in leukocyte chemotaxis to the...
GPR15 is a G protein-coupled receptor (GPCR) located on chromosome 3 and has similarity in its sequence The expression of GPR15 and c10orf99/gpr15l mRNA was analyzed by RT-qPCR. Our results suggest that GPR15/GPR15L have a pathogenic role in RA and their antagonizing could be a therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews
- 4GPCRnet, September 26-29, 2022. Leipzig, Germany
August 2022 "WELCOME 4GPCRnet meeting bringing together four of the biggest GPCR networks in Europe for Four of the biggest European networks on GPCR research (COST Actions Adher’n Rise and ERNEST plus DFG-funded Read more at the source #DrGPCR #GPCR #IndustryNews
- C5aR2 receptor: The genomic twin of the flamboyant C5aR1
The C5aR1 is a classical G-protein-coupled receptor (GPCR), whereas C5aR2 is a nonclassical GPCR that Read more at the source #DrGPCR #GPCR #IndustryNews
- Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior...
A major pan-receptor focus has been to identify GPCR-selective ligands that have bias in G protein-dependent Read more at the source #DrGPCR #GPCR #IndustryNews
- ADGRL3 genomic variation implicated in neurogenesis and ADHD links functional effects to the...
harbored in the ADGLR3-hormone receptor domain (HRM, a common extracellular domain of the secretin-like GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Helix 8 in chemotactic receptors of the complement system
crystal structures of inactive C5aR1 in terms of an inverted orientation of helix H8, unobserved in other GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Orion Shares New Data on its Latest Best-in-Class Drug Candidate
10, 2022 — Orion Biotechnology Canada Ltd, a drug discovery and development company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs), today announced that it will be presenting important Vice-President Drug Discovery, will present Orion’s novel technology for targeting undrugged peptidergic GPCRs discovery platform, one of the fastest drug discovery solutions in the industry for targeting peptidergic GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism or sy
hypoglycemia, we first checked expression of counterregulatory hormone G-protein coupled receptors (GPCRs regulators and downstream enzymes catalyzing glycogen metabolism, gluconeogenesis and lipolysis by qPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
indicated that the mechanism of KXS in treating depression was involved in the biological process of GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and...
STING-YAP signaling by both a small-molecule STING agonist, SR-717, and a G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand...
Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts Read more at the source #DrGPCR #GPCR #IndustryNews