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Results found for "GPCR Biology"
- 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
- Rescue of Cell Surface Expression and Signaling of Mutant Follicle-Stimulating Hormone Receptors
Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Pharmacological chaperones are cell-permeant small molecules that engage nascent mutant GPCRs in the These findings aid in advancing the understanding of the effects of genetic mutations on GPCR function
- HDX-MS-optimized approach to characterize nanobodies as tools for biochemical and structural ...
multiple immune signaling processes and is dependent on activation by Ras and G protein-coupled receptors (GPCRs that stimulated lipid kinase activity, block Ras activation, and specifically inhibited p101-mediated GPCR
- Target Residence Time: The Hidden Driver of In Vivo Efficacy
From restricted tissue diffusion to PK–PD dissociation, Kenakin equips you with the kinetic models and biological And when receptors are dense (like GPCRs on membranes), this rebinding hits the collisional limit , where
- 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
- Chronic itch: emerging treatments following new research concepts
However, many new targets, such as Mas-related GPCRs and unexpected new pathways need to be also explored
- Rhodopsin as a Molecular Target to Mitigate Retinitis Pigmentosa
These disorders are mainly related to the abnormalities in the rod G protein-coupled receptor (GPCR),
- 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
- 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
- Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas ...
and review Odorant receptors (ORs) account for about 60% of all human G protein-coupled receptors (GPCRs
- 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
- Purpose-Driven Opioid Research: Catherine Demery’s Academic Path
And GPCR pharmacology isn’t just an academic pursuit—it’s essential to understanding and responding to
- 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
- HBx induces hepatocellular carcinogenesis through ARRB1-mediated autophagy to drive the G 1/S cycle
dependent kinase inhibitor 1B; CQ: chloroquine; E2F1: E2F transcription factor 1; FBS: fetal bovine serum; GPCRs
- Pharmacology Isn't What You Think—It's So Much More
You’ll uncover: Why pharmacology is the glue between chemistry and biology How to interpret drug behavior
- 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
- What If the Most Important Part of Your Drug Isn’t What It Binds—But What It Does?
uncover why efficacy is the unsung hero of drug discovery and how its effects depend entirely on the biological
- The Five Traps of Ignoring Kinetics
But biology isn’t tidy.
- Understanding Orthosteric Binding: The Key to Drug Action
Often, a low EC50 indicates high potency, but this isn't always the case due to various biological factors
- TeachOpenCADD - A teaching platform for computer-aided drug design
as well as practical aspect of these topics, the platform addresses students and researchers with a biological






