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Results found for "Druggable GPCR"
- Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild trauma
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- PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal...
MRGPRB2 receptor in mouse peritoneal mast cells "A novel mast cell-specific G-protein-coupled receptor (GPCR 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
- The expression and clinical significance of GPR39 in colon cancer
GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival. tumor-adjacent tissues by retrieving TCGA data and detected the expression of GPR39 in colon cancers with qPCR several other biomarkers including PPARG, EPCAM, and PD-L1 was investigated by re-analyzing TCGA data, qPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal...
Confers Cholesterol-Induced Thermal Stability to the Serotonin 1A Receptor "G protein-coupled receptors (GPCRs The serotonin1A receptor is a crucial neurotransmitter receptor in the GPCR family involved in a multitude envision that our results could have potential implications in structural biological advancements of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
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- Dynamic recognition of naloxone, morphine and endomorphin1 in the same pocket of µ-opioid receptors
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- 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..
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- Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
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- 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
- 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
- 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
- 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
- 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
- Chemical Drug Matter : Rethinking the Molecules We Choose to Develop In Drug Discovery
outcomes An understanding of new chemical sources beyond natural agonist analogs Awareness of how GPCR Allostery and Biased Signaling Change the Game The most profound change in GPCR drug discovery is our GPCRs are not simple on/off switches. Peptide GPCR therapies now address obesity, diabetes, cancer, neuroendocrine disorders, inflammatory GPCR innovation is accelerating.
- Location bias contributes to functionally selective responses of biased CXCR3 agonists
November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially Although GPCRs are primarily found at the plasma membrane, GPCRs can traffic to and signal from many subcellular signaling contributes to the biased signaling generated by three endogenous ligands of the GPCR observed at CXCR3, which has important implications for drugs targeting chemokine receptors and other GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Molecular basis for variations in the sensitivity of pathogenic rhodopsin variants to 9-cis-retinal
Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE
- G-protein-coupled receptors as therapeutic targets for glioblastoma
In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets.
- G protein-coupled receptor signaling: transducers and effectors
October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance dynamic structures, and physiological relevance in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins, GPCR kinases (GRKs), and β-arrestins. As new technologies are developed and applied to studying GPCR structure and their downstream effectors Read more at the source #DrGPCR #GPCR #IndustryNews
