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424 items found for "A3 adenosine receptor"
- GPCR kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by...
September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization evidence that distal carboxyl-terminal tail (C-tail), but not proximal, phosphorylation of the chemokine receptor We demonstrate by pharmacologic inhibition of GRK2/3-mediated phosphorylation of the chemokine receptor
- GPCR voltage dependence controls neuronal plasticity and behavior
G-protein coupled receptors (GPCRs) play a paramount role in diverse brain functions. This voltage dependent potentiation is abolished in mutant animals expressing a voltage independent receptor Depolarization alone, without a muscarinic agonist, results in a nicotinic ionotropic receptor potentiation that is mediated by muscarinic receptor voltage dependency. Finally, muscarinic receptor voltage independence causes a strong behavioral effect of increased odor
- Ode to GPCRs
to nicotinic acetylcholine receptors and muscarinic acetylcholine receptors.[18] The 1971 Nobel Prize receptor 1 (hTAAR1). These odorant receptors (ORs) now account for about 60% of all identified human GPCRs. Regulation of nuclear factor κB activation by G-protein-coupled receptors. Non-traditional roles of G protein-coupled receptors in basic cell biology.
- In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
2022 In vitro assays for the functional characterization of (psychedelic) substances at the serotonin receptor induce alterations in mood, perception, and thought, and have the activation of serotonin (5-HT) 2A receptors arachidonic acid release), assays to monitor β-arrestin recruitment or signaling, and assays to monitor receptor
- Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembra
G protein-coupled receptors (GPCRs) are among the most promising drug targets. They often form homo- and heterodimers with allosteric cross-talk between receptor entities, which contributes modulators (PAMs) that bind at the interface of the transmembrane domains of the heterodimeric GABAB receptor core of the GABAB2 transmembrane domain, which also controls the constitutive activity of the GABAB receptor region corresponds to the sodium ion binding site in class A GPCRs that controls the basal state of the receptors
- Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling
August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases, differences in the orientation of individual residues and/or their interactions not easily detectable in the receptor-transducer
- Combined docking and machine learning identify key molecular determinants of ligand pharmacological
September 2022 "G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases We hypothesized that there is a common set of receptor interactions made by ligands of diverse structures β2AR structures, generating ca 75 000 docking poses and predicted all atomic interactions between the receptor
- Neurotransmitters: Potential Targets in Glioblastoma
By targeting the receptors synaptically or non-synaptically, neurotransmitters activate multiple signaling Significantly, many ligands acting on neurotransmitter receptors have shown great potential for inhibiting
- GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...
basolateral membrane and regulates epithelial apicobasal polarity "The adhesion family of G protein-coupled receptors These receptors are expressed widely and involved in various functions including development, angiogenesis appears to occur at an atypical GPCR proteolysis site within the GAIN domain during an early stage of receptor
- PH-Binding Motif in PAR4 Oncogene: From Molecular Mechanism to Drug Design
October 2022 "While the role of G-protein-coupled receptors (GPCR) in cancer is acknowledged, their underlying Protease-activated receptors (PAR), a subgroup of GPCRs, form a family of four members (PAR1-4) centrally AYPGKF peptide ligand activation of PAR4 induces EGF receptor (EGFR) Tyr-phosphorylation, effectively
- 📰 GPCR Weekly News, August 21 to 27, 2023
Hébert and their colleagues research on 'G Protein-Biased Agonists for Intracellular Angiotensin Receptors GPCR Activation and Signaling G Protein-Biased Agonists for Intracellular Angiotensin Receptors Promote Myofibroblasts β-arrestin-dependent and -independent endosomal G protein activation by the vasopressin type 2 receptor with Nonobstructive Azoospermia GPCRs in Neuroscience Molecular insights into orphan G protein-coupled receptors
- Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling
November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies inhibitory GAIN domain and the dipping of the cleaved stalk peptide into the ligand-binding pocket of receptors
- Reversible Photocontrol of Dopaminergic Transmission in Wild-Type Animals
Dopamine receptors are involved in the modulation of fundamental physiological functions, and dysregulation We demonstrate that azodopa activates D1-like receptors in vitro in a light-dependent manner.
- Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR..
binding mechanisms of a middle-sized flexible molecule, bosentan, to a GPCR protein, human endothelin receptor GA-mD-VcMD is a generalized ensemble method that produces a free-energy landscape of the ligand-receptor Last, in the pocket, ligand–receptor attractive native contacts are formed.
- Chemerin Forms: Their Generation and Activity
Chemerin can signal via two G protein-coupled receptors, chem1 and chem2, as well as be bound to a third non-signaling receptor, CCRL2.
- Exploring pharmacological inhibition of G q/11 as an analgesic strategy
One potential solution is to develop analgesics that act at targets other than opioid receptors. Previous research showed that activation of Gq/11 proteins by G-protein coupled receptors has pro-nociceptive
- Isoform-and ligand-specific modulation of adhesion GPCR ADGRL3/Latrophilin3 by a synthetic binder
September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular Modulating a single function of a specific aGPCR isoform while affecting no other function and no other receptor
- Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent ROCK...
The purpose of this study was to evaluate the role of dual transactivation of EGF and TGF-β receptors In addition, as an intermediary of G protein-coupled receptor (GPCR) signaling, the functions of ROCK Moreover, ET-1-increased protein expression of PAI-1 was decreased in the presence of bosentan (ET receptor
- Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist...
upstream of the agonistic peptide sequence, an event necessary for NTF displacement and subsequent receptor phenocopies the pulmonary phenotype of GPR116 knock-out mice, demonstrating that tethered agonist-mediated receptor
- Multifunctional role of GPCR signaling in epithelial tube formation
Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified
- G protein coupling and activation of the metabotropic GABAB heterodimer
September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor
- 📰 GPCR Weekly News, July 10 to 16, 2023
GPCRs in Oncology and Immunology Ovarian cancer G protein-coupled receptor 1 (OGR1) deficiency exacerbates β2AR Using Native Mass Spectrometry. psnGPCRdb: The Structure-network Database of G Protein Coupled Receptors Reviews, GPCRs, and more Optical approaches for investigating neuromodulation and G Protein-Coupled Receptor
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
identified for their contribution to GPCR desensitization to agonist-mediated activation, followed by receptor recruitment, activation, and scaffolding of numerous cytoplasmic signaling complexes and assist in G-protein receptor
- Phosphorylation of RGS regulates MAP kinase localization and promotes completion of cytokinesis
September 2022 "Yeast use the G-protein–coupled receptor signaling pathway to detect and track the mating The G-protein–coupled receptor pathway is inhibited by the regulator of G-protein signaling (RGS) Sst2
- 📰 GPCR Weekly News, June 12 to 18, 2023
A unique melanocortin-4-receptor signaling profile for obesity-associated constitutively active variants GPCRs in Neuroscience Orphan receptor GPR88 as a potential therapeutic target for CNS disorders - an Stimulation of ectopically expressed muscarinic receptors induces IFN-γ but suppresses IL-2 production
- 📰 GPCR Weekly News, August 7 to 13, 2023
GPCR Activation and Signaling Tail engagement of arrestin at the glucagon receptor Gα protein signaling bias at 5-HT1A receptor GPCRs in Cardiology, Endocrinology, and Taste Gβγ-SNAP25 exocytotic brake removal adipocyte browning, and protects against diet-induced obesity GPCRs in Neuroscience The neuropeptide receptor
- Lipid Modulation of a Class B GPCR: Elucidating the Modulatory Role of PI(4,5)P 2 Lipids
(PI(4,5)P2) lipids have been shown to stabilize an active conformation of class A G-protein coupled receptors previous molecular dynamics (MD) simulation studies have shown PI(4,5)P2 interacting with the Glucagon receptor
- Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
Glutamate exerts its effect through ionotropic and metabotropic glutamate receptors (mGluRs). mGluR2 drug targets for the treatment of many neurological conditions and several compounds targeting these receptors