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September 2022 High GPER expression in triple-negative breast cancer is linked to pro-metastatic pathways According to the cutoff value, 26.4% (95/360) of patients showed high GPER expression and significant In quantitative comparison, GPER abundance is correlated with the high-risk subtype of TNBC. Furthermore, univariate analysis confirmed that GPER was a significant prognostic factor for DMFS in Read more at the source #DrGPCR #GPCR #IndustryNews

Innovative Approaches in GPCR Drug Discovery: Designing Precise Solutions for GPCR Challenges. GPCR Podcast: Leadership, Impact, and GPCR Signaling with Dr. From cAMP to femtomolar ligands, she unpacks a career at the edge of precision signaling. GPCR evolved from a grassroots effort to a global force in GPCR science—one rooted in connection, sustainability The pace of GPCR innovation is accelerating.

Ligands exert their action via the interactions in the ligand binding pocket. We hypothesized that there is a common set of receptor interactions made by ligands of diverse structures We demonstrate with the application of ML methods that it is possible to identify the key interactions to be important in GPCR activation. Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational However, how these states impact GPCRs biological function and therapeutic targeting remains incompletely quantitative analysis revealed agonist-like properties of gp120s. " Read more at the source #DrGPCR #GPCR

exploring the relationship between the actual psychedelic effects and those manifestations of therapeutic interest Read more at the source #DrGPCR #GPCR #IndustryNews

Register today: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, Read more at the source #DrGPCR #GPCR #IndustryNews

Canonical chemokine receptors – scavenging “decoys” Chemokine receptors coordinate cell migration upon interaction Although some GPCRs constitutively internalize through clathrin-coated pits independently of phosphorylation CCR2 vs CCR1 scavenging signatures CCR1 is constitutively phosphorylated, constitutively interacts with 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

session, you’ll gain: ✅Clarity on Definitions:  What truly distinguishes orthosteric from allosteric interactions Allosteric Interactions Still Matter Orthosteric and allosteric interactions have been in pharmacology Recognizing how your ligand interacts with the receptor lets you predict safety margins, dose–response GPCR members save  50%+  (check your Weekly News code). If your team is still treating orthosteric and allosteric interactions as interchangeable, you’re leaving

ERK1/2), signal transducer and activator of transcription 3 (STAT3), cyclic adenosine monophosphate (cAMP ), Ras homolog family member A (RhoA), exchange protein activated by cAMP (Epac), and transient receptor Read more at the source #DrGPCR #GPCR #IndustryNews

Understanding receptor-ligand interaction is key in drug discovery and biomedical research. ligands labeled with radioactive isotopes which can be used in binding assays to quantify other ligands’ interaction in the pharmacophore and its optimization ensure access to the binding site with minimal unspecific interactions Quantitative cell binding studies : Radioligands have superior precision when accounting for ligand-receptor interactions GPCR-radioligand binding assays.

G protein-coupled receptor 3 (GPR3) belongs to the class A rhodopsin-type GPCR family and is highly expressed to constitutively activate the Gαs protein without a ligand, which elevates the basal intracellular cAMP Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The Smoothened receptor (SMO, a 7 pass transmembrane domain, Class F GPCR family protein We are able to identify the interaction of membrane cholesterols with definite sites and domains within We show that cholesterol interactions with the transmembrane domain TMD, unlike those with the cysteine-rich We have also reported the interaction of phosphatidylinositol 4-phosphate with the intracellular region Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling signaling produce discrete and separable effects and provide proof of concept for the development of safer GPCR-targeting Read more at the source #DrGPCR #GPCR #IndustryNews

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

Dear GPCR Community, Before diving into this week's news, prepare for an incredible learning journey! GPCR Event Spotlight    11th Adhesion GPCR Workshop    Location:  Mexico City Dates:  October 23-25, 2024 Join us  to connect with peers and explore cutting-edge adhesion GPCR biology.  Let’s dive into the   Classified GPCR News  from August 12th to 18th, 2024 Adhesion GPCRs Heterogeneity screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November

AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP Their functionality in terms of cAMP production via Gαs protein coupling was decreased compared to the Read more at the source #DrGPCR #GPCR #IndustryNews

In one example, to study a G protein coupled receptor (GPCR), we used one antagonist as probe and multiple Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway of hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors (GPCR ) to modulate cAMP levels. Read more at the source #DrGPCR #GPCR #IndustryNews

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.

Read more at the source #DrGPCR #GPCR #IndustryNews

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. potentially prove effective also in diseases associated with inflammation of the lower gut there is emerging interest pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR

glucose-dependent insulinotropic polypeptide (GIP) which exert their functions through G protein-coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

Transcript and protein levels were determined by RT-qPCR and Western blot, respectively. Read more at the source #DrGPCR #GPCR #IndustryNews

Discover our comprehensive coverage of GPCRs, We welcome GPCR paper suggestions! GPCR Podcast featuring Dr. Neil Grimsey and Dr. Katarzyna Marcinkiewicz. in Neuroscience Targeting sensory neuron GPCRs for peripheral neuropathic pain GPCRs in Oncology and Insights into GPCR Function Fully activated structure of the sterol-bound Smoothened GPCR-Gi protein GPCR Ecosystem

09, 2022 | | SNOWBIRD RESORT, UTAH, UNITED STATES The superfamily of G protein-coupled receptors (GPCRs mechanisms of GPCR function has revealed new paradigms with increasingly complex models of receptor Spatial-temporal signaling of GPCRs and physiological functions; 2. GPCRs as environmental sensors; 3. New approaches to GPCR drug discovery.

function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR OR51E1 and OR51E2, initially assumed to be GPCRs only expressed in prostate tissue, play a role in prostate from the scientific community to target this class of GPCRs. expression of ORs is generally more technically challenging compared with expression of nonolfactory GPCRs Check the original article at https://pubmed.ncbi.nlm.nih.gov/35999088/ #GPCR #DrGPCR#Ecosystem

Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but Not G Protein Interaction "The calcium-sensing receptor is a homodimeric class C G protein-coupled receptor (GPCR) that senses However, the nature of interactions between VFT units and HH bundles, and the impacts of heterozygous Read more at the source #DrGPCR #GPCR #IndustryNews

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