Search Results
584 items found for "GPCR therapeutics"
- G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial ...
vasoconstrictors, resulting in enhanced signalling through their cognate G protein-coupled receptors (GPCR Prolonged vasoconstrictor GPCR signalling increases arterial contraction and stimulates signalling pathways GPCR signalling through phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt) promotes VSMC proliferation In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs
- In Vitro and In Silico Characterization of Kurarinone as a Dopamine D 1A Receptor Antagonist and ...
Alterations in the expression and/or activity of brain G-protein-coupled receptors (GPCRs) such as dopamine Since studies have indicated that flavonoids can target brain GPCRs and provide neuroprotection via inhibition Functional GPCR assays unfolded the compound's antagonist behavior on D1R (IC50 42.1 ± 0.35 μM) and agonist
- Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage...
Several neurotransmitters and neuromodulators, acting through G-protein-coupled receptors (GPCRs), fine-tune However, intracellular partners linking GPCRs to TASK1 modulation are not yet well-known. We hypothesized that isoform 2 of rho-kinase (ROCK2), acting as downstream GPCRs, mediates adjustment Furthermore, ROCK activity assays were performed to evaluate the ability of various physiological GPCR
- Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs
Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest typically have a protonated amino group that contributes to receptor binding, and the functioning of GPCRs
- 4GPCRnet - International Symposium
SEPTEMBER 26-29, 2022 (Leipzig, Germany) 4GPCRnet meeting bringing together four of the biggest GPCR Four of the biggest European networks on GPCR research (COST Actions Adher’n Rise and ERNEST plus DFG-funded
- Chemogenetic stimulation of the G i pathway in astrocytes suppresses neuroinflammation
Engineered G protein-coupled receptors (GPCRs) are commonly used in chemogenetics as designer receptors Although several GPCRs have been studied in astrocytes using a chemogenetic approach, the functional
- Melatonin MT 2 receptor is expressed and potentiates contraction in human airway smooth muscle
Numerous physiological effects of melatonin are mediated via its specific G protein-coupled receptors (GPCRs human and guinea pig airway smooth muscle and cultured human airway smooth muscle (HASM) cells by RT-PCR
- Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall ...
target for control of the fall webworm Hyphantria cunea Background: Insect G protein-coupled receptors (GPCRs HLGR2 is a typical GPCR and shows high structural and sequence similarity with other insect LGR2 proteins
- A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent ...
The D1 receptor (D1R) is a Gαs/olf-coupled GPCR which activates a cAMP/PKA/DARPP-32 signalling cascade Finally, we report that JQ1 treatment downregulated expression of many GPCRs and also impaired ERK1/2
- Targeted Activation of G-Protein Coupled Receptor-Mediated Ca 2+ Signaling Drives Enhanced Cartilage
This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement cartilage-like matrix production, and it established hM3Dq as a powerful tool for elucidating the role of GPCR-mediated
- 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 Altogether, our results provide insights into the effect of intracellular binding partners on the GPCR
- HBx induces hepatocellular carcinogenesis through ARRB1-mediated autophagy to drive the G 1/S cycle
modulating autophagy and the CDKN1B-CDK2-CCNE1-E2F1 axis and indicate that ARRB1 may be a potential therapeutic dependent kinase inhibitor 1B; CQ: chloroquine; E2F1: E2F transcription factor 1; FBS: fetal bovine serum; GPCRs
- Prostaglandin signaling in ciliogenesis and development
Many G-protein-coupled receptors (GPCRs) including EP4 are localized in cilia for modulating cAMP signaling
- Engineered synaptic tools reveal localized cAMP signaling in synapse assembly
Given that postsynaptic latrophilin adhesion-GPCRs drive synapse formation and produce cAMP, we suggest
- Disentangling bias between G q, GRK2, and arrestin3 recruitment to the M 3 muscarinic acetylcholine
G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular
- On-cell nuclear magnetic resonance spectroscopy to probe cell surface interactions
characterize ligand interactions with cell surface membrane proteins such as G-protein coupled receptors (GPCRs
- Free-Energy Simulations Support a Lipophilic Binding Route for Melatonin Receptors
"The effects of the neurohormone melatonin are mediated by the activation of the GPCRs MT1 and MT2 in
- Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion ...
their functional activities are achieved by binding to the cell surface G protein-coupled receptors (GPCRs
- Deficiency of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in ...
is a key protein that mediates desensitization and internalization of G protein-coupled receptors (GPCRs
- Synaptic integration of subquantal neurotransmission by co-localized G protein coupled receptors in
Colocalization of different actions of GPCRs provide synaptic integration within presynaptic terminals
- Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial ...
Exendin-4, and possibly through G protein-coupled receptors (GPCRs), increases levels of cAMP and upregulates
- New role of β-arrestins in MOR signaling
Opioid receptors belong to class A of G protein-coupled receptors or GPCRs and signaled mainly through
- Twist Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID-19...
Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID-19 and Other Antibody Therapeutics
- Canonical chemokine receptors as scavenging “decoys”
The scavenging function of CKRs should be considered when evaluating the safety and therapeutic efficacy