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Results found for "Druggable GPCR"
- 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 A central question of GPCR drug discovery is to understand what determines the agonism or antagonism ligands made interactions with W2866.48×48 and Y3167.43×42, both residues considered to be important in GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism, microbiota..
Read more at the source #DrGPCR #GPCR #IndustryNews
- Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
Read more at the source #DrGPCR #GPCR #IndustryNews
- Endogenous ligand recognition and structural transition of a human PTH receptor
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- PAR-Induced Harnessing of EZH2 to β-Catenin: Implications for Colorectal Cancer
September 2022 "G-protein-coupled receptors (GPCRs) are involved in a wide array of physiological and In addition, the molecular mechanisms underlying GPCR-induced post-translational signaling regulation Read more at the source #DrGPCR #GPCR #IndustryNews
- Endocannabinoid System in the Neuroendocrine Response to Lipopolysaccharide-induced Immune Challenge
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- GPR108 is required for gambogic acid inhibiting NF-κB signaling in cancer
September 2022 "GPCRs are the most potential targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer drug is not fully investigated. Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...
Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled (GPCR Here, we show that a combination of insulin and the GPCR agonist neurotensin induced rapid activation Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- 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
- 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 However, little is known about the mechanism for GP coupling and activation for class C GPCRs. This mechanism provides fresh insights into the mechanistic details of class C GPCRs activation expected Read more at the source #DrGPCR #GPCR #IndustryNews
- GRK3 is a poor prognosticator and serves as a therapeutic target in advanced gastric adenocarcinoma
September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the GPCR-kinase 3 (GRK3) is critical for GPCR signaling. Read more at the source #DrGPCR #GPCR #IndustryNews
- Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Inflammation..
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- Neuropeptide S Encodes Stimulus Salience in the Paraventricular Thalamus
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- Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent ROCK...
In addition, as an intermediary of G protein-coupled receptor (GPCR) signaling, the functions of ROCK Read more at the source #DrGPCR #GPCR #IndustryNews
- Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs)...
Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling 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
- To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Novel Driver Strength Index highlights important cancer genes in TCGA PanCanAtlas patients
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- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
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- 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
- 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
- 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
- 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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- Irreversible Drugs, Real Control: Design for Durable Target Engagement
Molecular innovation This Week’s GPCR Intelligence: The next edge in discovery isn’t louder exposure—it Breakthroughs this week: nanomedicines targeting PAR2 for sustained analgesia; Emerging Voices in GPCR GPCR Premium: Sneak Peek Industry insights: Confo VLAIO grant; Skye CB1 Ph2 miss; Chugai CT-388 in-license Upcoming events: Membrane-mimetic screening; GPCR Forum 2025; GPCR-TDD Summit Europe. GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need
- Biphasic activation of β-arrestin 1 upon interaction with a GPCR revealed by methyl-TROSY NMR
β-arrestins (βarrs) play multifaceted roles in the function of G protein-coupled receptors (GPCRs). βarrs typically interact with phosphorylated C-terminal tail (C tail) and transmembrane core (TM core) of GPCRs changes for βarr activation upon the C tail- and TM core-mediated interactions with a prototypical GPCR This plasticity of βarr conformation in complex with GPCRs engaged in different binding modes may explain
- GBCRdb for beginners
Join us for a fantastic introduction to GPCRdb with Dr. David Gloriam and Dr. Albert Kooistra. Register today: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe
- Orion and Peptilogics are pursuing AI-driven drug discovery to explore new functional chemical ...
and precision-engineer therapeutics with enhanced potency and tailored signaling against an undrugged GPCR #ai #drugdiscovery #gpcr" Read more at the source #DrGPCR #GPCR #IndustryNews
