December 2021 "Early-stage studies of COVID-19 treatments from the likes of Vir Biotechnology Inc. and Trevena Inc. could offer potential new weapons against omicron and future viral variants. The omicron strain of the virus was first identified in South Africa in early November, and an existing treatment has already shown positive results in the lab. While vaccine-makers race to test their shots against the variant, the monoclonal antibody sotrovimab from Vir and partner GlaxoSmithKline PLC posted results Dec. 7 demonstrating activity against the omicron spike protein. Sotrovimab is the first monoclonal antibody showing preclinical efficacy against all COVID-19 variants, including the delta 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 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery platform to enable functional antibody discovery. VIB spin-off Confo Therapeutics today announced that it has entered into a collaborative agreement with Regeneron Pharmaceuticals, Inc. whereby Confo’s technology platform, which uses conformationally selective VHH antibodies – ConfoBodies® – to stabilize GPCRs (G protein-coupled receptors) in disease-relevant conformations, will be applied with the goal of enabling the discovery of novel therapeutic antibody drug candidates. " Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 OMass Therapeutics 's founder, Carol Robinson , has been awarded the prestigious Louis-Jeantet Prize for Medicine 2022 by the Louis-Jeantet Foundation and the 2022 Benjamin Franklin Medal in Chemistry from The Franklin Institute " Huge congratulations to our founder, Carol Robinson , who has been awarded the prestigious Louis-Jeantet Prize for Medicine 2022 by the Louis-Jeantet Foundation and the 2022 Benjamin Franklin Medal in Chemistry from The Franklin Institute yesterday for contributions to the field of mass spectrometry and establishing it as method to analyse proteins in their native state. Her work in the field has been instrumental and is set to shape the future of drug discovery for years to come. #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 Oncology . Radionetics aims to develop a deep pipeline of novel, targeted, nonpeptide radiopharmaceuticals for the treatment of a broad range of oncology indications "– Co-founded by Crinetics, 5AM Ventures and Frazier Healthcare Partners, the New Company Launches with $30M in Initial Financing Provided by 5AM and Frazier – Pipeline is Built from Crinetics’ Core Nonpeptide Platform and Includes Drug Candidates and Leads Against 10 Oncology Targets – Radionetics and Crinetics to Collaborate on Multiple Additional targets SAN DIEGO, October 18, 2021 — Crinetics Pharmaceuticals , Inc. (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, together with 5AM Ventures and Frazier Healthcare Partners, today announced the formation of an independently operated new company, Radionetics Oncology . Radionetics aims to develop a deep pipeline of novel, targeted, nonpeptide radiopharmaceuticals for the treatment of a broad range of oncology indications." 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 its OB-004 lead optimization. OB-004 is a GPCR targeted protein analog of CCL2 that targets the CCR2 receptor. The CCL2/CCR2 pathway plays an important role in oncology, inflammatory, metabolic, and neurological disorders." Read more at the source #DrGPCR #GPCR #IndustryNews

December 2022 Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop Novel Therapeutic Antibodies against GPCR Targets " Collaboration aims to combine Twist’s proprietary synthetic antibody libraries and sophisticated bioinformatics expertise with Sosei Heptares’ world-leading StaR® (stabilized receptor) platform to generate novel antibody leads to disease-relevant GPCR targets Tokyo, Japan and Cambridge, UK, 16 December 2021 – Sosei Group Corporation (“the Company”; TSE: 4565), the world leader in GPCR-focused structure-based drug design (SBDD) and development, and Twist Bioscience Corporation (Nasdaq: TWST), a company enabling customers to succeed through its offering of high-quality synthetic DNA using its silicon platform, announced a strategic collaboration to discover therapeutic antibodies against G protein-coupled receptors (GPCR) identified by Sosei Heptares . " Read more at the source #DrGPCR #GPCR #IndustryNews

Excited to hear Dr. Sandra Berndt talk about new structural perspectives in GPCR-mediated Src family kinase activation. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe #drgpcr #gpcr #virtualcafe

Ep 57 of the Dr. GPCR podcast is now available! Our guest is Dr. Peter Banks, Scientific Director at BioTek Instruments! Learn about his career today! Listen where you get your podcasts. https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #podcast

Episode 56 of the Dr. GPCR podcast is now available! Our guest is Dr. Adriano Marchese! Learn about his remarkable career and research in #GPCR signaling and trafficking. Listen where you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #drgpcr #gpcr #podcast

Excited to hear Dr. Joe Clayton from BioTek Instruments talk about automated micro-plate-based methods for quantifying #GPCR activation. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #drgpcr #gpcr #virtualcafe

Episode 54 of the Dr. GPCR podcast is now available! Our guest is Dr. JoAnn Trejo! Sharing how she became a scientist, educator, mentor, and the powerhouse we know today. Listen where you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast #gpcr #drgpcr #podcast

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early evolution of eukaryotic species, therefore, the genome-wide identification of GPCR genes can provide insight into the adaptive strategy and evolutionary tendency in an animal taxon. Here, we identified a total 216 full-length GPCR genes in the marine water flea Diaphanosoma celebensis genome, which were classified into five distinct classes (A, B, C, F, and other). Phylogenetic comparison of GPCRs in D. celebensis to those in humans (Homo sapiens), fruitfly (Drosophila melanogaster), and freshwater water flea (Daphnia magna) reveals a high level of orthological relationship of amine, neuropeptide, and opsin receptor repertoire, while purinergic and chemokine receptors were highly differentiated in humans. Our findings suggest sporadic evolutionary processes within the GPCR gene families identified in D. celebensis. In this study, these results may provide a better understanding on the evolution of GPCRs, and expand our knowledge of the cladoceran GPCR gene repertories which in part, mediate cell physiological mechanisms in response to various environmental stimuli.

November 2021 Addex's strategic partner The Janssen Pharmaceutical Companies of Johnson & Johnson, Inc. has completed Phase 1 studies in Japan with JNJ-40411813 (ADX71149) " Geneva, Switzerland, November 15, 2021 – Addex Therapeutics (SIX: 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 Companies of Johnson & Johnson , has successfully completed Phase 1 studies in Japan with JNJ-40411813 (ADX71149). ADX71149 is a selective metabotropic glutamate type 2 (mGlu2) receptor positive allosteric modulator (PAM). The successful 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, Pa., Nov. 11, 2021 -- Trevena , Inc. (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

November 2021 Dr. Kevin Pfleger and Dr. Elizabeth Johnstone were awarded one of the 2022 Diabetes Research Grants at the World Diabetes Day Breakfast! " Congratulations to Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of the 2022 Diabetes Research Grants at yesterday's annual World Diabetes Day Breakfast! This $60,000 grant from Diabetes Research WA will assist the Perkins' Molecular Endocrinology and Pharmacology Laboratory team who are investigating new ways to tackle the disease-inducing chronic inflammation that is linked to type 2 diabetes." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 Positive Recommendation for Use of TAVNEOS™ (avacopan) in ANCA Vasculitis Adopted by European Medicines Agency (EMA) Committee for Medicinal Products for Human Use (CHMP) "SAN CARLOS, Calif. , Nov. 12, 2021 (GLOBE NEWSWIRE) -- ChemoCentryx , Inc. , (Nasdaq: CCXI), today announced that the European Medicines Agency’s (EMA) Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion recommending marketing authorization for the Company’s TAVNEOS (avacopan), an orally administered selective complement 5a receptor inhibitor, in combination with a rituximab or cyclophosphamide regimen, indicated for the treatment of adult patients with severe, active granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA)." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 "So proud and grateful to receive honorary doctorate yesterday from Karolinska Institute and celebrate with my family in Stockholm." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, but Omass Therapeutics Ltd.’s new structure-based technology has passed a key test, in enabling the discovery of orally available small molecules aimed at intractable and poorly drugged membrane and complex-bound protein targets. The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute carriers, are relevant to immunology indications and rare diseases with high unmet need." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 Twist Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID-19 and Other Antibody Therapeutics for Difficult to Treat Diseases " Nov 15, 2021 -- Executive Leadership Team Established with Demonstrated Success in Clinical, Regulatory and Commercial Development -- SOUTH SAN FRANCISCO, Calif.--(BUSINESS WIRE)--Nov. 15, 2021-- Twist Bioscience Corporation (NASDAQ: TWST), a company enabling customers to succeed through its offering of high-quality synthetic DNA using its silicon platform, today announced it has launched Revelar Biotherapeutics , Inc., an independently operated, new biotechnology company to develop and commercialize an antibody, discovered and optimized by Twist Biopharma, a division of Twist Bioscience , that neutralizes all known variants of concern of the SARS-CoV-2 virus in preclinical studies. In addition, Revelar will have the ability to leverage the antibody discovery and optimization platform of Twist Biopharma to license additional antibodies for up to five targets over the next four years."

November 2021 "Cambridge’s Japanese-owned life sciences company Sosei Heptares has clinched a lucrative deal with California-based NASDAQ-quoted business Neurocrine Biosciences. The vision is to develop novel muscarinic receptor agonists for schizophrenia and other neuropsychiatric disorders. Neurocrine Biosciences anticipates initiating a Phase 2 study with the selective M4 agonist HTL-0016878 in schizophrenia in 2022 and Phase 1 studies for a dual M1/M4 and selective M1 agonist in 2023." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 "Target class-specific libraries mean you need to screen less to identify high-quality antibodies. Aaron Sato , Chief Scientific Officer at Twist Bioscience , elaborates. Antibody developers are increasingly utilising antibody libraries to derive high-quality, drug-like biologics. However, only a few general-purpose libraries have been commercially available for drug discovery. As a result, most approved library-derived antibodies originate from just three libraries. The drugs also target relatively low-hanging fruit: like cytokines or tyrosine kinase receptors. To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better and more targeted libraries, are needed." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 " Chronic use of most opioids causes tolerance; the new compounds avoid this and other unwanted qualities. November 22, 2021 JUPITER, FL— Scientists at Scripps Research in Florida have created a collection of new pain-relieving compounds that, like morphine and other drugs, provide relief via activation of opioid receptors, but without inducing many dangerous and unwanted side-effects that have driven opioid-related overdose and deaths." Read more at the source #DrGPCR #GPCR #IndustryNews

Deficiency of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in primary Sjögren's syndrome The etiology of primary Sjögren's syndrome (pSS) remains unknown, and there is no ideal drug for the specific treatment of pSS. β-arrestin2 is a key protein that mediates desensitization and internalization of G protein-coupled receptors (GPCRs) and it participates in inflammatory and immune responses that have been found to mediate apoptosis in autoimmune disease. In this study, we established an experimental Sjögren's syndrome (ESS) mouse model to elucidate the molecular mechanisms of β-arrestin2 in pSS. First, excessive activation of β-arrestin2 and GRP78-ATF6-CHOP apoptosis signaling were detected in specimens from pSS patients. In vivo, we found that inhibition of GRP78-ATF6-CHOP apoptosis signaling improved ESS symptoms, and the targeted deletion of β-arrestin2 significantly increased saliva flow, alleviated salivary gland indices, and improved tissue integrity in the ESS model by downregulating GRP78-ATF6-CHOP apoptosis signaling. In vitro, we used IFNα to stimulate human salivary gland epithelial cells (HSGECs), and the results showed that IFNα activated GRP78-ATF6-CHOP apoptosis signaling, decreased cell viability, and induced apoptosis, which were negatively regulated by the ERS inhibitor 4-PBA. In addition, β-arrestin2 depletion downregulated GRP78-ATF6-CHOP apoptosis signaling to alleviate cell apoptosis, and the effect depended on the interaction between GRP78 and β-arrestin2. In summary, our results suggest that excessive activation of GRP78-ATF6-CHOP apoptosis signaling is involved in the pathogenesis of pSS and that β-arrestin2 encourages inflammation-induced epithelial apoptosis through GRP78-ATF6-CHOP apoptosis signaling. This research further clarified the underlying role of β-arrestin2 and provided an experimental foundation for β-arrestin2 depletion in the treatment of the human autoimmune disorder pSS. Read full article

Come attend this month's virtual café talk to see the awesome work of Dr. Stuart Maudsley on how an aging physiological context affects #GPCR signaling #drgpcr. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

Episode 53 of the Dr. GPCR podcast is now available! Our guest is Dr. Tim De Groof! It’s not often when you get the best of both worlds - nano-bodies and #GPCRs. Listen where you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast #gpcr #drgpcr #podcast

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs). The experimental structure of these receptors has yet to be determined, and key-residues controlling their function remain mostly unknown. We designed an integrative approach to improve comparative modeling of TAS2Rs. Using current knowledge on class A GPCRs and existing experimental data in the literature as constraints, we pinpointed conserved motifs to entirely re-align the amino-acid sequences of TAS2Rs. We constructed accurate homology models of human TAS2Rs. As a test case, we examined the accuracy of the TAS2R16 model with site-directed mutagenesis and in vitro functional assays. This combination of in silico and in vitro results clarifies sequence-function relationships and proposes functional molecular switches that encode agonist sensing and downstream signaling mechanisms within mammalian TAS2Rs sequences. Read full article

Episode 52 of the Dr. GPCR podcast is now available! Our guest is Dr. Ben Myers! From studying sensory #ionchannels to the group leader at the University of Utah investigating Class F #GPCRs in #cancer. Listen nowhere you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #podcast