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- 📰 GPCR Weekly News, January 29 to February 4, 2024
Check out our GPCR coverage for this week. plasma membrane, featured on the cover of Nature Chemical Biology Julia Kinsolving; Dr. GPCR Symposia Our upcoming symposium on March 15th is about GPCR activation and signaling. Biology NEW Research Scientist Post-Doc position Lead Researcher Senior Researcher in Structural Biology GPCR Ecosystem
- Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with ...
February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous The company's co-founder, GPCR pioneer and Nobel laureate Robert Lefkowitz, M.D., has 50 years of experience Read more at the source #DrGPCR #GPCR #IndustryNews
- Dynamic GPCR activation revealed through time-resolved Cryo-EM
Human cells express over 800 G-protein-coupled receptors (GPCRs) to facilitate communication with the Capturing the dynamics of GPCR activation has always been a challenge because G protein activation in With this high-resolution, dynamic view of GPCR activation, scientists can better tackle diseases by Beyond GPCRs, the methods and insights from this study can be applied to other fast, transient biological Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).
- 📰 GPCR Weekly News, August 21 to 27, 2023
Hi there GPCR minds! Join us for a deep dive into the world of GPCRs. This week's highlights: Dr. in the GPCR field. GPCR Symposium on 'GPCRs as Therapeutic Modalities'. Jobs NEW Researcher / Senior Researcher in Structural Biology NEW Research Specialist NEW Science Research GPCR Ecosystem
- What's Going On with GPCRs?! Find Out in This Week's Update! ⦿ Nov 4 - 10, 2024
GPCR University 🎥 Access to the recorded classes of GPCR Courses and talks from Symposia 💲 Discounted GPCR courses GPCR Forum Initiate a vibrant conversation or seek assistance GPCR Events to keep you Centessa Initiates Phase 2 Trial with ORX750, a Novel Orexin Receptor 2 (OX2R) Agonist AI, Synthetic Biology Jobs Scientist I Cell Biology - Tectonic Therapeutic NEW Senior Principal Scientist, Medicinal Chemistry Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist
- Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors
October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new As a result, there is an ongoing need to develop novel approaches to monitor and to modulate GPCR activation nanobodies have been adopted to elucidate the structure, pharmacology, and signaling of cardiovascular GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair
release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR
2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR will gain unique and valuable access to the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR targets and advance the development of new gastrointestinal therapeutics entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR drug discovery programs in the area of gastrointestinal diseases. " Read more at the source #DrGPCR #GPCR
- Phosphorylation of RGS regulates MAP kinase localization and promotes completion of cytokinesis
Read more at the source #DrGPCR #GPCR #IndustryNews
- Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System
are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors (GPCRs ) that act in an allosteric manner to modulate the activity of GPCRs. the past 2 decades, pepducins have progressed initially from pharmacologic tools used to manipulate GPCR To date, pepducins designed from numerous GPCRs have been studied for their impact on pathologic conditions Read more at the source #DrGPCR #GPCR #IndustryNews
- 📰 GPCR Weekly News, August 7 to 13, 2023
Hello GPCR enthusiasts! Check out the latest advancements in GPCR studies. Save the date! GPCR Symposium on 'GPCRs as Therapeutic Modalities'. Want to share your project in a casual way? GPCR Newsletter! , and more Tri-part NanoLuc as a new split technology with potential applications in chemical biology GPCR Ecosystem
- The integrin ligand SVEP1 regulates GPCR-mediated vasoconstriction via integrins α9β1 and α4β1
Read more at the source #DrGPCR #GPCR #IndustryNews
- 📰 GPCR Weekly News, August 14 to 20, 2023
the fascinating world of GPCRs. GPCR Symposium on 'GPCRs as Therapeutic Modalities'. GPCR Newsletter! Remember to check out the weekly Classified GPCR News from August 14 to 20, 2023 Adhesion GPCRs Amelioration GPCR Ecosystem
- Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent..
transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs activation by glucagon within 5 min and transit via EEA1-marked endosomes shown previously to be sites of GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Molecular basis for ligand modulation of the cannabinoid CB 1 receptor
August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). " Read more at the source #DrGPCR #GPCR
- 📰 GPCR Weekly News, July 10 to 16, 2023
Welcome, GPCR enthusiasts! This week's GPCR papers feature a publication by Dr. Robert J Lefkowitz. GPCR Symposium on Structural and Molecular Insights on GPCR Activation! GPCR Newsletter for updates! Hijacking of GPCRs and RTKs by pathogens. GPCR Ecosystem
- 📰 GPCR Weekly News, July 3 to 9, 2023
Hello GPCR enthusiasts! We're here to share the latest GPCR news with you. Congratulations to Dr. GPCR Symposium on Structural and Molecular Insights on GPCR Activation is quickly approaching! GPCR Newsletter for updates! Structural and Molecular Insights into GPCR Function Dual mechanisms of cholesterol-GPCR interactions GPCR Ecosystem
- β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the...
β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR cells "β-arrestins mediate regulatory processes for over 800 different G protein-coupled receptors (GPCRs ) by adopting specific conformations that result from the geometry of the GPCR-β-arrestin complex. However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter
- Conservation of Allosteric Ligand Binding Sites in G-Protein Coupled Receptors
November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures The method has found druggable sites overlapping with the cocrystallized allosteric ligands in 21 GPCR We then mapped the 394 GPCR X-ray structures available at the time of the analysis (September 2020). Results show that for each of the 21 structures with bound ligands there exist many other GPCRs that Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells
Introduction Dopamine receptors are G-protein-coupled receptors (GPCRs), which have 5 subtypes -D1-5. Fluorescence anisotropy (FA) assay has been used to study the ligand binding kinetics of many GPCRs.[ parameters of PL-384 binding to D3 receptors from competition binding experiment data by global systems biology Miniaturization is key for HTS application, so achieving good Z’ values for GPCR ligand binding assays Altogether, the development of similar probes for other GPCRs and further development of measurement
- 📰 GPCR Weekly News, June 19 to 25, 2023
Welcome, GPCR buffs! Join us for our weekly round-up of GPCR News. Congratulations to our Dr. GPCR Partner, GPCR Therapeutics, for passing the Technology Evaluation process for listing on the KOSDAQ GPCR Symposium on Structural and Molecular Insights on GPCR Activation. GPCR Newsletter. Let's review the weekly Classified GPCR News from June 19th to June 25th, 2023. GPCR Ecosystem
- 📰 GPCR Weekly News, June 12 to 18, 2023
Greetings GPCR enthusiasts! Join us to explore the fascinating world of GPCRs. GPCR Symposium on Structural and Molecular Insights on GPCR Activation. GPCR Activation and Signaling Single transmembrane GPCR modulating proteins: neither single nor simple GPCRs in Oncology and Immunology The GPCR-Gαs-PKA signaling axis promotes T cell dysfunction and cancer GPCR Ecosystem
- RAB-Symposium - Regulatory Autoantibodies Targeting GPCRs. September 15-16, 2022. Lübeck, Germany...
August 2022 RAB-Symposium - Regulatory Autoantibodies Targeting GPCRs. September 15-16, 2022. GPCRs are involved in a variety of physiological and pathophysiological processes. So far, numerous therapeutics targeting GPCRs have been developed, with a focus on small molecules and Recently, functional autoantibodies targeting GPCRs have been associated with various disease-specific Read more at the source #DrGPCR #GPCR #IndustryNews
- 📰 GPCR Weekly News, June 5 to 11, 2023
Hi there GPCR enthusiasts! Join us this week for a deep dive into the world of GPCRs. GPCR Symposium on Structural and Molecular Insights on GPCR Activation. Adhesion GPCRs Collagen VI Is a Gi-Biased Ligand of the Adhesion GPCR GPR126/ADGRG6. GPCRs in Immunology and Oncology The GPCR–Gαs–PKA signaling axis promotes T cell dysfunction and cancer GPCR Ecosystem
- 📰 GPCR Weekly News, November 6 to November 12, 2023
This week, we've curated 12 GPCR papers. GPCR Symposium for the year, which will focus on GPCRs in Immunology and Oncology. GPCR Newsletter with Dr. Kathleen Caron, as our video guest, subscribe now! for high-throughput gpcrs antibody discovery Reviews, GPCRs, and more Current strategic trends in drug GPCR Ecosystem
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
Notably, G-protein-coupled receptors (GPCRs), representing the biggest drug target, have been revealed Historically, drug discovery efforts targeting GPCRs focused on G-protein-dependent signaling pathways In summary, targeting GPCR-activated ERK pathways represents a promising strategy for developing new Minireview: targeting GPCR activated ERK pathways for drug discovery. Biology of the Cell, 93(1‐2), 71-79. Wei, H., Ahn, S., Shenoy, S. K., Karnik, S.
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed treatment of psychiatric and neurodegenerative diseases, and several allosteric modulators of this GPCR libraries have complementary advantages and illustrate how access to high-resolution structures of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
Originally, β-arrestins were identified for their contribution to GPCR desensitization to agonist-mediated However, current investigations have now recognized that in addition to GPCR arresting (hence the name Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Effect Delta-9-tetrahydrocannabinol and cannabidiol on milk proteins and lipid levels in HC11 cells
Read more at the source #DrGPCR #GPCR #IndustryNews



