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Results found for "GPCR research community"
- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
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- Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84
August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR
- Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone...
glucose-dependent insulinotropic polypeptide (GIP) which exert their functions through G protein-coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Hypoxia: New..
Stem-Like Cells under Hypoxia: New Insights into MRP3 Transporter Function "Glioblastoma is the most common Transcript and protein levels were determined by RT-qPCR and Western blot, respectively. Read more at the source #DrGPCR #GPCR #IndustryNews
- Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated
Finally, inhibition of Gq-GPCR coupling in mice enhanced the antinociceptive effects of morphine. that would allow for lower dose utilization of opioid analgesics. " Read more at the source #DrGPCR #GPCR
- Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell...
Methods: Immunohistochemistry, western blot and quantitative real-time PCR techniques were used to analyze Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- 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
- Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response
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- Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of...
)-a major family of GPCRs-play critical roles in the regulation of tissue development and cancer progression The orphan receptor GPR97, activated by glucocorticoid stress hormones, is a prototypical aGPCR. Furthermore, the community network analysis suggests that the palmitoylation of Go not only allosterically of the Go protein, and offers guidance for future drug design of aGPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews
- Pharmacological Properties and Function of PxOctβ3 Octopamine Receptor in Plutella xylostella (L.)
showed that the receptor is a member of the Octβ3 protein family, and an analysis using quantitative PCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
Although some GPCRs constitutively internalize through clathrin-coated pits independently of phosphorylation In this study, it is revealed that CCR2 scavenging role was largely independent of the classical GPCR Check the original article at https://pubmed.ncbi.nlm.nih.gov/36719944/ #GPCR #DrGPCR#Ecosystem
- Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent...
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- Endocannabinoid System in the Neuroendocrine Response to Lipopolysaccharide-induced Immune Challenge
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- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
GPCRs are not suitable for antibody use due to steric hindrance and reverse binding, thus, other strategies This modification is small enough to not affect GPCR expression or activity.[21–23] The Tag-lite® binding It has been applied to different GPCR binding assays, such as CXCR4, opioid receptors, CCK1 and CCK2. Cannabinoids as Anticancer Drugs: Current Status of Preclinical Research. Nucleic Acids Research 2021 , 49 (12), e72–e72. https://doi.org/10.1093/nar/gkab237 . (20) Degorce
- 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
increasing numbers of people with excess body weight, the MC4R has become a target of interest in the search Read more at the source #DrGPCR #GPCR #IndustryNews
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- 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
- 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 Read more at the source #DrGPCR #GPCR #IndustryNews
- Therapeutic validation of an orphan G protein‐coupled receptor
Historically, ligands for GPCRs have been identified before their receptor counterparts. Orphan GPCRs have been shown to play key roles in various physiological functions, such as sensory perception Therefore, matching a ligand to an orphan GPCRs, the process of de-orphanizing, is of great importance GPR84 is a Gi‐coupled class A GPCR mainly expressed in immune cells and microglia in the brain (Wojciechowicz #GPCR #DrGPCR#Ecosystem
- 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
- 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
- Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild trauma
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- Pharmacophore-guided Virtual Screening to Identify New β 3 -adrenergic Receptor Agonists
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- Actions of Parathyroid Hormone Ligand Analogues in Humanized PTH1R Knockin Mice
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- Dynamic recognition of naloxone, morphine and endomorphin1 in the same pocket of µ-opioid receptors
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