April 2022 "By Cliona MacSweeney | Apr 20, 2022 Cliona MacSweeney, a project director in our Translational Medicine department, recently presented this important pre-clinical work at SIRS2022 confirming the This work highlights an important interplay between the adenosinergic and dopaminergic systems and suggests to control neuropsychiatric symptoms in conditions such as schizophrenia. " Read more at the source #DrGPCR

Selective M4 Positive Allosteric Modulator Program For The Treatment Of Schizophrenia & Other Psychotic Disorders ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug discovery and development, announced today that it has moved a selective and potent M4 muscarinic receptor M4 PAMs have the potential to treat schizophrenia and other types of debilitating neuropsychiatric disorders Read more at the source #DrGPCR #GPCR #IndustryNews

partnerships and collaborations across pharma and #biotech⁠ and is an advocate for the role of #AI in drug discovery." Read more at the source #DrGPCR #GPCR #IndustryNews

Pharmaceuticals Expands Executive Team With Appointment Of James Hassard As Chief Commercial Officer "SAN DIEGO (Nasdaq: CRNX), a clinical stage pharmaceutical company focused on the discovery, development, and commercialization of novel therapeutics for rare endocrine diseases and endocrine-related tumors, today announced the operations for both global and domestic biotechnology companies." Read more at the source #DrGPCR #GPCR #IndustryNews

Methods: Rats were divided into sham, sham + Exendin-4 (10 μg/day, i.p), MI, and MI + Exendin-4. Results: On day 7 post-infraction, MI rats showed LV dysfunction with higher serum levels of cardiac in the levels of cyclic adenosine monophosphate (cAMP), mRNA of manganese superoxide dismutase (MnSOD Under normal conditions, β-catenin is degraded in the cytoplasm by the active GSK3β-dependent degradation (DVL) protein which in turn phosphorylates and inhibits GSK3β.

The Dr. GPCR Virtual Cafe is back! Our first guest speaker is none other than Dr. Ben Myers! https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe

fundraising gives us the means to achieve our ambitions: to become a leading player in the field of brain diseases #IPO #biotech #innovation #traitements #addiction #cannabis #Trisomie21 #Downsyndrome" Read more at the source #DrGPCR #GPCR #IndustryNews

February 2022 Read more at the source #DrGPCR #GPCR #IndustryNews

Dr. Xavier Leroy for his new role as CEO of GIO Therapeutics Dr. Dr. to Drug Discovery,' which will be led by Dr. Dr. GPCR Volunteers Join our dynamic team as a volunteer! cyclase/ cyclic AMP signaling pathway The non-nutritive sweetener sucralose increases β-arrestin signaling

"We are an experienced, innovative, global team on a bold mission to improve health by creating and developing Read more at the source #DrGPCR #GPCR #IndustryNews

Simply put, it represents what we do and why we do it. Read more at the source #DrGPCR #GPCR #IndustryNews

receptor type 9 (CCR9) antagonist and previous phase III clinical candidate for the treatment of Crohn's disease , we developed a chemical biology toolbox targeting the IABS of CCR9. Applying this molecular tool in a membrane-based setup and in living cells, we discovered a 4-aminopyrimidine To chemically induce CCR9 degradation, we then developed the first PROTAC targeting the IABS of 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 of diseases The molecular diversity of GPCR signaling systems is likely to be closely associated with disease-associated In the past decade, however, attention has focused upon how stable multiprotein GPCR superstructures, termed receptorsomes, both at the cell surface membrane and in the intracellular domain dictate and

secretagogue receptor 1a (GHSR1a) is intriguing because of its potential as a therapeutic target and its diverse Typically, ghrelin-dependent and constitutive GHSR1a activation occurs via Gαq/11 pathways. In vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors (GPCRs), including dopamine D1 and D2, serotonin 2C, orexin, oxytocin and melanocortin 3 receptors ( This review discusses the signalling mechanisms of GHSR1a alone and in combination with other GPCRs,

Objective: The goal of this study was to determine the glucometabolic effects of acute activation of Methods: To address this question, we studied mice that express a Gs-coupled designer G protein-coupled receptor (Gs-DREADD or GsD) selectively in skeletal muscle. UCN2 injection resulted in decreased glucose tolerance associated with lower plasma insulin levels. receptors enriched in SKM has only a limited impact on whole-body glucose homeostasis, most likely due

shown to affect the lifespan of animal and human models, and in which we put a special interest in describing Our compilation of data revealed that the mechanisms most involved in the role of GPCRs in lifespan are those that mimic dietary restriction, those related to insulin signaling and the AMPK and TOR pathways We also discuss the possibility of using agonist or antagonist drugs, depending on the beneficial or

protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are the targets for many different review, we have compared expression of GPCR mRNAs in human islets obtained from normal weight range donors GPCR expression status confers and the possible impact that adipokines, secreted from expanded fat depots

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants Here we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone Seventeen FSHR mutations described in patients with reproductive dysfunction were expressed in HEK 293T cells, and cell surface expression was determined by enzyme-linked immunosorbent assay of epitope-tagged

Therefore, the identification of such modulators as drug candidates is highly desirable. Toll-like receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent Moreover, the dysregulation of TLR4 contributes to numerous diseases, which highlights the importance of biased modulator development targeting TLR4. The discovery of biased modulators of TLR4 would provide insight for the future development of biased

December 2021 Perkins’ Head of Molecular Endocrinology and Pharmacology, Professor Kevin Pfleger , was Coincidentally, on the same day, Prof Pfleger was announced as a Fellow of the British Pharmacological Society. " ASCEPT is the peak professional society devoted to advancing excellence in Clinical and collaboration with the Australasian Pharmaceutical Science Association ( APSA ).” " Read more at the source #DrGPCR

December 2021 "Early-stage studies of COVID-19 treatments from the likes of Vir Biotechnology Inc. and variant, the monoclonal antibody sotrovimab from Vir and partner GlaxoSmithKline PLC posted results Dec . 7 demonstrating activity against the omicron spike protein. and omicron mutations, Vir CEO George Scangos said on a Dec. 7 call with analysts." Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 OMass Therapeutics 's founder, Carol Robinson , has been awarded the prestigious Louis-Jeantet Her work in the field has been instrumental and is set to shape the future of drug discovery for years #DrugDiscovery #MassSpec #Award #massspectrometry" Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 Crinetics Pharmaceuticals announced the formation of an independently operated new company Radionetics aims to develop a deep pipeline of novel, targeted, nonpeptide radiopharmaceuticals for the (Nasdaq: CRNX), a clinical stage pharmaceutical company focused on the discovery, development, and commercialization Radionetics aims to develop a deep pipeline of novel, targeted, nonpeptide radiopharmaceuticals for the Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 "Ottawa, Ontario, Canada, Nov. 30, 2021 -- Orion Biotechnology , a clinical stage company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs) with a novel drug modality , proven discovery platform and best-in-class molecules, today announced the successful completion of The CCL2/CCR2 pathway plays an important role in oncology, inflammatory, metabolic, and neurological disorders Read more at the source #DrGPCR #GPCR #IndustryNews

ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug discovery and development, today announced that Janssen Pharmaceuticals, Inc., part of the Janssen Pharmaceutical completion of this Phase 1 safety program will enable centers in Japan to be included in a potential global development of ADX71149 for the treatment of epilepsy. " Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 "November 11, 2021 7:00am EST Patricia Drake appointed new Chief Commercial Officer CHESTERBROOK (Nasdaq: TRVN), a biopharmaceutical company focused on the development and commercialization of novel medicines for patients with central nervous system (CNS) disorders, today announced the addition of Patricia Drake to its senior leadership team as Chief Commercial Officer." Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 "Cambridge’s Japanese-owned life sciences company Sosei Heptares has clinched a lucrative deal The vision is to develop novel muscarinic receptor agonists for schizophrenia and other neuropsychiatric disorders. study with the selective M4 agonist HTL-0016878 in schizophrenia in 2022 and Phase 1 studies for a dual Read more at the source #DrGPCR #GPCR #IndustryNews