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Results found for "GPCR Drug Design"
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled receptors (GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- GPCR voltage dependence controls neuronal plasticity and behavior
G-protein coupled receptors (GPCRs) play a paramount role in diverse brain functions. Almost 20 years ago, GPCR activity was shown to be regulated by membrane potential in vitro, but whether the voltage dependence of GPCRs contributes to neuronal coding and behavioral output under physiological Here we show that muscarinic GPCR mediated neuronal potentiation in vivo is voltage dependent. crucial involvement of GPCR voltage dependence in neuronal plasticity and behavior.
- Enhanced membrane binding of oncogenic G protein αqQ209L confers resistance to inhibitor YM-254890
October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular They can also function independently of GPCR activation upon acquiring mutations that prevent GTPase YM-254890 (YM) can inhibit signaling by both GPCR-activated wild type αq and GPCR-independent αqQ209L GPCR-dependent signaling by PM-restricted wild type αq is strongly inhibited by YM, demonstrating that Read more at the source #DrGPCR #GPCR #IndustryNews
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- Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent...
We designed and synthetized peptides that interfered with integrin αIIb binding (pCIB and pCIBm) or mimicked Read more at the source #DrGPCR #GPCR #IndustryNews
- Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response
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- Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but...
Protein Interaction "The calcium-sensing receptor is a homodimeric class C G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify...
and mediate intracellular pathway bias "Within the intestine, the human G protein-coupled receptor (GPCR The pharmacological profiles and mechanistic insights of our study provide clues for the future design Read more at the source #DrGPCR #GPCR #IndustryNews
- GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome activation
in innate immune cells and intestinal inflammation, and suggest that GPR84 may serve as a potential drug Read more at the source #DrGPCR #GPCR #IndustryNews
- Endocannabinoid System in the Neuroendocrine Response to Lipopolysaccharide-induced Immune Challenge
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- Neuropeptide S Encodes Stimulus Salience in the Paraventricular Thalamus
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- To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from...
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- A Setmelanotide-like Effect at MC4R Is Achieved by MC4R Dimer Separation
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- All About Addgene: More Open and Reproducible Science with Materials Sharing
GPCR Virtual Cafe? Register today! Addgene's Dr. Joanne Kamens is our guest. research or you want to share your materials, this is the place to go. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe / #gpcr #drgpcr #virtualcafe #addgene
- Reversible Photocontrol of Dopaminergic Transmission in Wild-Type Animals
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- Viral G Protein-Coupled Receptors Encoded by β- and γ-Herpesviruses
acquired genes are transmembrane proteins and cytokines, such as viral G protein-coupled receptors (vGPCRs This review focuses on the vGPCRs encoded by the human β- and γ-herpesviruses. These include receptors from human cytomegalovirus, which encodes four vGPCRs: US27, US28, UL33, and We discuss ligand binding, signaling, and structures of the vGPCRs in light of robust differences from Read more at the source #DrGPCR #GPCR #IndustryNews
- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
cost-effective methodologies for screening compound libraries targeting the CBRs becomes key for identifying drugs Cannabinoids as Anticancer Drugs: Current Status of Preclinical Research. Design and Synthesis of Fluorescent Ligands for the Detection of Cannabinoid Type 2 Receptor (CB2R). HTRF: A Technology Tailored for Drug Discovery - A Review of Theoretical Aspects and Recent Applications Protein Engineering Design and Selection 2006 , 19 (7), 309–316. https://doi.org/10.1093/protein/gzl014
- Integrative model of the FSH receptor reveals the structural role of the flexible hinge region
receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs The models are expected to allow for testable hypotheses about signal transduction and drug development for GPHRs." Read more at the source #DrGPCR #GPCR #IndustryNews
- Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin...
epithelial-cell-derived antimicrobial peptides defensins activated orphan G-protein-coupled receptors (GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma via...
Methods Immunohistochemistry staining and RT–qPCR analyses were performed to detect the correlation of Western blot and RT–qPCR assays were carried out to measure the downstream factors of the interaction Read more at the source #DrGPCR #GPCR #IndustryNews
- Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water ...
Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early evolution of eukaryotic species, therefore, the genome-wide identification of GPCR genes can provide Here, we identified a total 216 full-length GPCR genes in the marine water flea Diaphanosoma celebensis In this study, these results may provide a better understanding on the evolution of GPCRs, and expand
- Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild trauma
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- The Impact of CB1 Receptor on Nuclear Receptors in Skeletal Muscle Cells
Quantitative real-time probe-based polymerase chain reaction (qRT-PCR) assays are deployed in order to This can be deduced from the qRT-PCR assays; triggering CB1 receptors amplifies both NR4A1 and NR4A3 Read more at the source #DrGPCR #GPCR #IndustryNews
- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
of DOI differed among sexes - brain and plasma concentrations of DOI were lower 30 and 60 min after drug Read more at the source #DrGPCR #GPCR #IndustryNews
- Dynamic recognition of naloxone, morphine and endomorphin1 in the same pocket of µ-opioid receptors
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- Actions of Parathyroid Hormone Ligand Analogues in Humanized PTH1R Knockin Mice
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- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
Introduction Cannabinoid receptors are GPCRs, and two main types exist, CB1R and CB2R. for CB1R in live cells and the PHERAstar FSX is the ideal microplate reader for characterizing the GPCR-ligand
- When Pain Becomes a Catalyst: How Personal Experience Redefined One Scientist’s Mission
. _________________ Keyword Cloud: GPCR research community , chronic pain , GPCR drug discovery , GPCR
- Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Structural dynamics of Smoothened (SMO) in ciliary membrane and its interaction with membrane lipids
September 2022 "The Smoothened receptor (SMO, a 7 pass transmembrane domain, Class F GPCR family protein Read more at the source #DrGPCR #GPCR #IndustryNews
