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of PAR2 that induces unique cellular signaling, distinct from trypsin and PAR2-activating peptide (AP delayed and sustained manner compared to the rapid and transient signals induced by trypsin and PAR2-AP Interestingly, unlike PAR2-AP, GB83 and trypsin induced sustained receptor endocytosis and PAR2 colocalization

February 2022 Trevena Announces Submission of New Drug Application in China for OLINVYK® by its Partner IV morphine, conducted in China by Nhwa Trevena is eligible to receive future success payments upon approval that China’s National Medical Products Administration (NMPA) has accepted submission of a New Drug Application of a Phase 3 bridging trial for OLINVYK (oliceridine) injection, a novel IV analgesic that has been approved

Deficiency of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in primary Sjögren's In vivo, we found that inhibition of GRP78-ATF6-CHOP apoptosis signaling improved ESS symptoms, and the apoptosis, and the effect depended on the interaction between GRP78 and β-arrestin2. in the pathogenesis of pSS and that β-arrestin2 encourages inflammation-induced epithelial apoptosis through GRP78-ATF6-CHOP apoptosis signaling.

The research team, led by Brandon Novy and colleagues, utilized an innovative APEX2/AUR biosensor that The critical player is Apurinic/Apyrimidinic Endodeoxyribonuclease 2 (APEX2). Therefore, it’s a great molecular tool for proximity labeling approaches in living cells.  In this study, the DOR receptor was genetically fused to APEX2, creating a DOR-APEX2 construct. APEX2 biosensor utilizes a fluorogenic substrate called Amplex UltraRed (AUR).

GPCR Ecosystem Premium Membership (restrictions apply) Early bird discount on future courses (restrictions apply) Dr. Let’s dive into the Classified GPCR News from April 22nd to 28th, 2024 Adhesion GPCRs Dysfunction of

GPCR Ecosystem Premium Membership (restrictions apply) Early bird discount on future courses (restrictions apply) Check our conversation with Dr. Let’s dive into the Classified GPCR News from April 15th to 21st, 2024 GPCR Activation and Signaling Biopharma Drug Discovery Nexus Salipro Biotech will participate in BioKorea2024 Domain Therapeutics Appoints Korea Amgen To Present Tezspire® Phase 2A COPD Data At ATS 2024 GPCR Events, Meetings, and Webinars April

GPCR Ecosystem Premium Membership (restrictions apply) Early bird discount on future courses (restrictions apply) Save 25% with early bird registration that ends TODAY!! GPCR Partnered Events April 22 - 23, 2024 | Endocrine Metabolic GPCRs Join the Endocrine Metabolic GPCRs event in Birmingham, UK, on April 22-23, 2024. Let’s dive into the Classified GPCR News from April 8th to 14th, 2024 Adhesion GPCRs High incidence of

Early bird registration ends on April 18th. Join our upcoming Dr. GPCR Ecosystem Premium Membership (restrictions apply) Early bird discount on future courses (restrictions apply) Save 25% with early bird registration until April 18th. GPCR Partnered Events April 22 - 23, 2024 | Endocrine Metabolic GPCRs Join the Endocrine Metabolic GPCRs event in Birmingham, UK, on April 22-23, 2024.

PKC-dependent phosphorylation site in the receptor C-tail, both showed that PKC isozymes facilitate approximately 3 (GRK2 and GRK3) KO cells, and a receptor containing a mutated putative adaptor protein complex 2 (AP internalization of rat mGlu5a is mediated by Gαq/11 proteins (77% of the response), GRK2 (27%), and AP

Below is your Classified GPCR News at a glance for April 24 to 30, 2023. detecting peptide variants The Galien Foundation Announces 2023 Prix Galien UK Award Candidates Exscientia Appoints Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

Below is your Classified GPCR News at a glance for April 17 to 23, 2023. attended the Swiss Biotech Day Sosei Heptares presented novel Computational Chemistry and Cheminformatics approaches Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

Hello readers! We got a little busy with all the major events at Dr.GPCR, so our weekly news looks slightly different. We will be back next week with our regular weekly GPCR news digest. In the meantime, you can always check the  Classified GPCR News from the last weeks. Today, we celebrate a huge milestone by releasing Episode #150 of the Dr. GPCR Podcast. Join us in this wonderful episode to meet the team of volunteers behind the work you see. The story behind how Dr.GPCR came to be, the people behind the process, the great anecdotes, and what’s coming next. We also have some important announcements in today’s episode, so join us in this celebration and be the first to know about all the changes coming to Dr. GPCR. Today is also the first session of our hands-on workshop with Dr. Sam Hoare. If you aren't joining us this time, stay tuned for more Dr. GPCR University content coming soon.

Below is your Classified GPCR News at a glance for April 10 to 16, 2023. presented a poster at AACR 2023 GPCR Events, Meetings, and Webinars NEW FREE 7th ERNEST GPCR zoominar (April (April 20 - 21, 2023) Swiss Biotech Day (April 24 - 25, 2023) ASPET 2023 - American Society for Pharmacology Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

or present a poster, email us at Hello@DrGPCR.com Below is your Classified GPCR News at a glance for April GPCR Events, Meetings, and Webinars NEW AACR 2023 - American Association for Cancer Research (April 14 (April 20 - 21, 2023) Swiss Biotech Day (April 24 - 25, 2023) NEW ASPET 2023 - American Society for Pharmacology Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

poster, email us at Hello@DrGPCR.com Below is your Classified GPCR News at a glance for March 27th to April Reviews, GPCRs, and more NMR applications to GPCR recognition by peptide ligands. (April 20 - 21, 2023) Swiss Biotech Day (April 24 - 25, 2023) SLAS Europe 2023 Conference and Exhibition Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

August 2022 "The apelin receptor (APJ) is a target for cardiovascular indications. In summary, a potent and selective APJ agonist suitable for in vivo studies of APJ in peripheral tissues

August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs

Here, we determine that GRKs phosphorylate a non-canonical substrate, anterior pharynx-defective 1A (APH1A GRKs generate distinct phosphorylation barcodes in intracellular loop 2 (ICL2) and the C terminus of APH1A , which differentially regulate recruitment of the scaffolding protein β-arrestin 2 (βarr2) to APH1A simulation studies reveal an interaction between the βarr2 finger loop domain and ICL2 and ICL3 of APH1A Collectively, these studies provide insight into the molecular and structural determinants of the APH1A-βarr2

January 2022 ChemoCentryx Announces EU Approval of TAVNEOS® (avacopan) for the Treatment of ANCA-Associated Vasculitis "SAN CARLOS, Calif., Jan. 19, 2022, today announced that TAVNEOS® (avacopan) has been approved This approval follows the U.S. Food and Drug Administration (FDA) approval of TAVNEOS in October 2021.

of Biochemistry and Molecular Medicine of the Faculty of Medicine of the Université de Montréal, is appointed

clinical stage biotech company with a unique portfolio of CB1 inverse agonists, today announces the appointment

April 2022 Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders

March 2022 Crinetics Pharmaceuticals Expands Executive Team With Appointment Of James Hassard As Chief of novel therapeutics for rare endocrine diseases and endocrine-related tumors, today announced the appointment

November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in high-resolution techniques to investigate peptidergic transmission and expression throughout the brain in model systems. Neuropeptides exhibit distinct characteristics which includes their post-translational processing, release from dense core vesicles, and ability to activate G-protein-coupled receptors (GPCRs). These complex properties have driven the need for development of specialized tools that can sense neuropeptide expression, cell activity, and release. Current research has focused on isolating when and how neuropeptide transmission occurs, as well as the conditions in which neuropeptides directly mediate physiological and adaptive behavioral states. Here we describe the current technological landscape in which the field is operating to decode key questions regarding these dynamic neuromodulators." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment

HDX-MS-optimized approach to characterize nanobodies as tools for biochemical and structural studies

December 2021 Perkins’ Head of Molecular Endocrinology and Pharmacology, Professor Kevin Pfleger, was appointed “I am honoured to be appointed President of ASCEPT, and am particularly excited given the Society’s conference held in Perth next year, in collaboration with the Australasian Pharmaceutical Science Association (APSA

October 2022 "Single-molecule counting techniques enable a precise determination of the intracellular abundance and stoichiometry of proteins and macromolecular complexes. These details are often challenging to quantitatively assess yet are essential for our understanding of cellular function. Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate in many vital physiological functions making them a popular target for drug development. While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical and biophysical assays, innovations in single-molecule measurements are now driving a paradigm shift in our understanding of its relevance. Here, we review recent developments in single-molecule counting with a focus on photobleaching step counting and the emerging technique of quantitative single-molecule localization microscopy-with a particular emphasis on the potential for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor signaling." Read more at the source #DrGPCR #GPCR #IndustryNews