September 2022 "Introduction Protease activated receptors 1 (PAR1) and 4 (PAR4) agonists are used to Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Recent studies revealed butyrate and secondary bile acids, produced by the intestinal microbiome, potentiate RNA sequencing of intestinal epithelial cells responding to butyrate and secondary bile acids in combination sequencing findings and discovered a role for intestinal HNF4α in P-gp regulation. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 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 Considering this, we investigated the role of RGS20 as a potential prognostic marker in 28 different Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Ginsenoside Rg5 allosterically interacts with P2RY12 and ameliorates deep venous thrombosis by counteracting neutrophil NETosis and inflammatory response "Deep venous thrombosis (DVT) highly occurs DVT formation is a time-dependent inflammatory process in which NETosis plays an important role. However, whether ginsenoside Rg5 from species of Panax genus could alleviate DVT and its underlying mechanism Read more at the source #DrGPCR #GPCR #IndustryNews

The vision is to develop novel muscarinic receptor agonists for schizophrenia and other neuropsychiatric Neurocrine Biosciences anticipates initiating a Phase 2 study with the selective M4 agonist HTL-0016878 Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin However, controversy remains regarding its role in breast cancer since both pro- and anti-metastatic roles have been ascribed to it. Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression. 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. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings developments and use of GPR84 pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "We are proud to announce that SYnAbs is now officially accredited as a Research Tax Credit by the French Ministry of Higher Education and Research for 2022-2023-2024. trust us in the generation of their monoclonal antibodies against small molecules and transmembrane receptors antibodies #medicine #cancer #innovation #gpcr #synabs #monoclonalantibodies #drugdiscovery #biotechnology #research biologics #biotech #pharma #pharmaindustry #pharmaceuticals #oncology #healthcare #drugdevelopment" Read

August 2022 "August 10, 2022 Cancer Research UK is working with global biopharma Sosei Heptares on Cancer Research UK , a charity dedicated to funding lifesaving oncology research, spent £388 million on cancer research last fiscal year. Much of that funding is distributed to support third party research, but the group also does its own Read more at the source #DrGPCR #GPCR #IndustryNews

neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor Treatment of 5-HTR1E stable cells with NF-α1/CPE increased pERK 1/2 and pCREB levels which prevented Molecular dynamics studies revealed that NF-α1/CPE interacts with 5-HTR1E via 3 salt bridges, stabilized Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB Read full article

Elizabeth Johnstone were awarded one of the 2022 Diabetes Research Grants at the World Diabetes Day Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of the 2022 Diabetes Research This $60,000 grant from Diabetes Research WA will assist the Perkins' Molecular Endocrinology and Pharmacology are investigating new ways to tackle the disease-inducing chronic inflammation that is linked to type 2 Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators for rare diseases "29/06/2022 Confo Therapeutics , founded in 2015 as a spin-off from VIB and VUB, announced The grant should help expand Confo Therapeutic ’s research on G protein-coupled receptor (GPCR) drug candidates. " Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 Cancer Research UK and Sosei Heptares sign agreement to advance cancer immunotherapy candidate into clinical trials " HTL0039732 is a novel EP4 antagonist with potential to treat a wide range of company and world-leader in GPCR1-focused structure-based drug design (SBDD) and development, an d Cancer Research UK , the world’s largest private funder of cancer research, today announce the signing of an agreement Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "June 15, 2022 06:30 AM EDT - In 2016, Abbie Celniker was promoted to partner at Third Rock Ventures as the firm raised just over $600 million for its fourth fund. Coming on its 15th year, Third Rock Ventures announced its sixth fund today — and largest one by far Adding it all up, Third Rock has raised $3.8 billion since its inception. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and Somatostatin receptors (SSTs) are class A GPCRs abundantly expressed in pituitary tumors where they represent The cytoskeletal protein filamin A (FLNA) directly interacts with both somatostatin receptor type 2 ( organization have remained elusive. robust receptor internalization at shorter times than in A7 cells.

Apr 12, 2022 Summary Sophie Bradley, Translational Sciences Associate Director at Sosei Heptares , recently Conference, a summary of work performed both at Sosei Heptares and Glasgow University characterizing the role of the muscarinic M1 receptor in cognitive and neurodegenerative disorders and the potential therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews

Albert Kooistra & Gáspár Pándy-Szekeres ) will present and demonstrate the newest resources of the GPCRdb : 1) the new G protein resources and 2) the structural analysis platform. Reserve your spot for free at: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #GPCR #GPCRs #DrGPCR

November 2021 Twist Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID Diseases " Nov 15, 2021 -- Executive Leadership Team Established with Demonstrated Success in Clinical, Regulatory offering of high-quality synthetic DNA using its silicon platform, today announced it has launched Revelar Biopharma, a division of Twist Bioscience , that neutralizes all known variants of concern of the SARS-CoV-2 In addition, Revelar will have the ability to leverage the antibody discovery and optimization platform

APRIL 06 - 09, 2022 | | SNOWBIRD RESORT, UTAH, UNITED STATES The superfamily of G protein-coupled receptors Coupled with their ability to respond to a highly diverse range of chemical stimuli, they represent the mechanisms of GPCR function has revealed new paradigms with increasingly complex models of receptor Spatial-temporal signaling of GPCRs and physiological functions; 2. The structural basis for GPCR activation of down-stream signaling and regulatory proteins; and 4.

Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR (pertussis toxin-sensitive G proteins, whose βγ subunits activate multiple signals, including ERK1/2) in regulating parathyroid hormone secretion. We here describe 3 patients with symptomatic AHH who shared characteristics with the 2 cases we previously Read more at the source #DrGPCR #GPCR #IndustryNews

Information flow from a source to a receiver becomes informative when the recipient can process the are responsible for signal recognition at the membrane level and information transduction inside the The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 played by receptor homo- and hetero-oligomerization in cell biology. Read full article

Successful Lead Optimization of Candidate Molecules Dates:  September 5th to 26th, 2024 Course 2: Extracellular ATP and the tumor microenvironment in cancer progression and therapy Agonists of galanin subtype 2 receptor may prevent pancreatic cancer and agonists of angiotensin II type 2 receptor may prevent colorectal Targeting Neurological Diseases Achieves First R&D Milestone Tectonic bets on GPCR heart failure drug of GPCR cell-based assays in drug discovery October 2024 | Biologics US 2024   October 2 - 4, 2024 |

With the cloning revolution, several unidentified receptors have been found and were labelled as “orphan and 2. which ligands can be used as tool compounds to study the function and biology of this receptor Regarding the first question, GPR84 overexpression in immune cells in a range of pro‐inflammatory disorders Regarding the second question, there is still a lot to be done in respect to tool compounds to study the function of this receptor towards clinical validation, as well as radiopharmaceuticals, including

Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine receptor CXCR4 WHIM syndrome is a rare immunodeficiency disorder that is characterized by warts, hypogammaglobulinemia Here, we report on a new WHIM syndrome mutation that results in a frame shift within the codon for Ser339 very high basal level of degradation compared to that of R334X and wild type CXCR4. Read full article

ligand type and receptor activation state G protein-coupled receptors (GPCR) are the largest family of cell surface receptors in vertebrates. Likewise, the relative importance of receptor activation state and ligand function differences have also cross-docking, respectively. Read full article

Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall webworm Hyphantria of attractive targets for RNA interference (RNAi)-based pest control. A functional study of the leucine-rich repeat-containing (LGR2) gene in Hyphantria cunea (HLGR2) was HLGR2 RNAi led to a low pupation rate (45.00%), body malformation, abnormal wing expansion, failed cuticle Read full articles

Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled receptors expressed in tumors G protein-coupled receptors (GPCRs) are the largest family of human proteins. that cognate mutations with similar effects on GPCR function are distributed across many receptors. We also discovered that no single receptor drives this pattern, but rather multiple receptors contain Read full article

GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease GPCRs arguably represent the most effective current therapeutic targets for a plethora GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and of protein expression patterns, cellular stress responses and DNA integrity management. Read full article