September 2022 Structure of Mycobacterium tuberculosis Cya, an evolutionary ancestor of the mammalian membrane adenylyl cyclases " Mycobacterium tuberculosis adenylyl cyclase (AC) Rv1625c/Cya is an evolutionary ancestor of the mammalian membrane ACs and a model system for studies of their structure and function. Although the vital role of ACs in cellular signalling is well established, the function of their transmembrane (TM) regions remains unknown. Here, we describe the cryo-EM structure of Cya bound to a stabilizing nanobody at 3.6 Å resolution. The TM helices 1–5 form a structurally conserved domain that facilitates the assembly of the helical and catalytic domains. The TM region contains discrete pockets accessible from the extracellular and cytosolic side of the membrane. Neutralization of the negatively charged extracellular pocket Ex1 destabilizes the cytosolic helical domain and reduces the catalytic activity of the enzyme. The TM domain acts as a functional component of Cya, guiding the assembly of the catalytic domain and providing the means for direct regulation of catalytic activity in response to extracellular ligands." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma via the PI3K/AKT signaling pathway "Background CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand CCL25 to promote tumor proliferation and metastasis. However, the effect of CCR9 on salivary adenoid cystic carcinoma (SACC) malignant behavior remains unknown. This study aimed to investigate the specific molecular mechanism by which CCR9/CCL25 modulates malignant progression in SACC. Methods Immunohistochemistry staining and RT–qPCR analyses were performed to detect the correlation of CCR9 expression and tumor progression-associated markers in SACC. In vitro , SACC cell proliferation and apoptosis were evaluated using Cell Counting Kit-8 and colon formation, and cell migration and invasion were detected by wound healing and transwell assays. Vercirnon was used as an inhibitor of CCR9, and LY294002 was used as an inhibitor of the PI3K/AKT pathway in this study. Western blot and RT–qPCR assays were carried out to measure the downstream factors of the interaction of CCL25 and CCR9. The effect of CCL25 on the development of SACC in vivo was examined by a xenograft tumor model in nude mice following CCL25, Vercirnon and LY294002 treatment." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid receptor-dependent activation of EGFR "Background Fentanyl is an opioid analgesic and is widely used in ovarian cancer patients for pain management. Although increasing evidence has suggested the direct role of fentanyl on cancer, little is known on the effect of fentanyl on ovarian cancer cells. Methods Proliferation, migration and apoptosis assays were performed in ovarian cancer cells after fentanyl treatment. Xenograft mouse model was generated to investigate the in vivo efficacy of fentanyl. Combination index was analyzed for the combination of fentanyl and chemotherapeutic drugs. Immunoblotting approach was used to analyze signaling involved in fentanyl’s action focusing on EGFR." Read more at the source #DrGPCR #GPCR #IndustryNews

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The 3rd edition of the Dr. GPCR Summit is between October 10th to the 16th! 💡Trainees are invited to participate by presenting a trainee talk, a poster, or a pre-recorded talk Become a site member for FREE and submit your info! ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr

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We're very excited to announce the next episode of the Dr. GPCR podcast! 🥁 Drum rolls, please! Our guest is the wonderful Dr. Rosie Dawaliby! Watch the full video with a Dr. GPCR Ecosystem paid membership ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ep-84-with-rosie-dawaliby #gpcr #drgpcr

🌟 We're so excited about our upcoming Dr. GPCR Summit 2022. This is a great opportunity for us to come together and talk GPCRs. Do you want to be part of it? Our Summit is FREE for all Ecosystem site members, which is also free! Join us now ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr

December 2021 "Geneva, Switzerland, December 17, 2021 – Addex Therapeutics Ltd (SIX: ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug discovery and development, today announced that it has entered into a definitive agreement with Armistice Capital LLC, a healthcare-focused institutional investor, pursuant to which the Company agreed to sell 3,752,202 shares in the form of 625,367 American Depositary Shares (“ADSs”) at a gross purchase price of $6.50 per ADS, which is equivalent to CHF 1.00 per share. Each ADS represents six shares. Additionally, Addex has agreed to issue to Armistice Capital unregistered warrants to purchase up to 9,230,772 shares in the form of 1,538,462 ADSs (the “Unregistered Warrants”), as well as unregistered pre-funded warrants to purchase up to 5,478,570 shares in the form of 913,095 ADSs (the “Unregistered Pre-Funded Warrants” and together with the Unregistered Warrants, the “Warrants”) in a concurrent private placement. The Unregistered Warrants have an exercise price of $6.50 per ADS, will become exercisable in 60 days after their date of issuance and will expire six years from their date of issuance. The Unregistered Pre-Funded Warrants have been funded to the amount of $6.49 with $0.01 payable on exercise." Read more at the source #DrGPCR #GPCR #IndustryNews

💻Did you know that Dr. GPCR is much more than a podcast? Come check out the brand new Dr. GPCR Ecosystem and explore its benefits! We have #GPCR News, Learning Center, Events, and more to discover! Learn More HERE ➡️ https://www.ecosystem.drgpcr.com/learning-center #gpcr #drgpcr

February 2022 "Switzerland Today, InterAx Biotech is pleased to announce that Carola Weiss has joined the company as VP Business Development. Carola Weiss is a Senior Executive with more than 20 years of international experience in the biopharmaceutical industry. Carola Weiss ’ professional career brings deep expertise in business development, marketing & sales, licensing, alliance management, and strategic partnering. Her expertise guided numerous global negotiations, conclusions of partnership agreements, and fostered growth for her employers." Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "Watch our CEO Tim Dyer on AlphaStreet. In his interview, Mr. Dyer provides an overview of our #allostericmodulator pipeline and the potential $4 billion market for our lead compound #dipraglurant in #PDLID (#Parkinsonsdisease levodopa-induced #dyskinesia)." Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 Exscientia and Sanofi Establish Strategic Research Collaboration to Develop AI-driven Pipeline of Precision-Engineered Medicines "Collaborative efforts aim to accelerate drug discovery and improve clinical success Agreement to utilize Exscientia ’s AI-based capabilities and personalised medicine platform from target identification through patient selection Research will be focused on up to 15 novel small molecule candidates across oncology and immunology Exscientia will receive an upfront cash payment of $100 million with the potential of $5.2 billion in total milestones plus tiered royalties PARIS & OXFORD, England & BOSTON-- Sanofi and Exscientia announced today a groundbreaking research collaboration and license agreement to develop up to 15 novel small molecule candidates across oncology and immunology, leveraging Exscientia ’s end-to-end AI-driven platform utilizing actual patient samples. The companies have been working together since 2016 and in 2019, Sanofi in-licensed Exscientia ’s novel bispecific small molecule candidate capable of targeting two distinct targets in inflammation and immunology." Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 "3-part randomized, double-blind, placebo-controlled Phase 1 study will evaluate TRV045 safety, tolerability, and PK in healthy volunteers Enrollment expected to start in early Q1 2022 CHESTERBROOK, Pa., Dec. 13, 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 it is advancing TRV045 into clinical development, following receipt of a notification from the U.S. Food and Drug Administration (FDA) that the study may proceed. TRV045 is the Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic neuropathic pain (DNP). In addition, through a collaboration with the National Institutes of Health, the Company is also exploring TRV045 as a potential treatment for epilepsy." Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 Neurocrine Biosciences Announces Positive Phase 3 Data for KINECT-HD Study Evaluating Valbenazine for Chorea Associated with Huntington Disease " Highly Statistically Significant Reduction in Chorea Movements (p < 0.0001) as Measured by the Unified Huntington's Disease Rating Scale (UHDRS®) Total Maximal Chorea (TMC) Score- Placebo-Adjusted Mean Reduction in TMC Score of 3.2 Units in Valbenazine-Treated Patients- Company Plans to Submit Supplemental New Drug Application to U.S. Food and Drug Administration in 2022 SAN DIEGO, Dec. 7, 2021 /PRNewswire/ -- Neurocrine Biosciences (Nasdaq: NBIX) today announced positive top-line data from its Phase 3 KINECT-HD study evaluating the efficacy, safety and tolerability of valbenazine, a selective vesicular monoamine transporter 2 (VMAT2) inhibitor being investigated as a once-daily treatment in adults with chorea associated with Huntington disease (HD). The study met the primary endpoint of reduction in severity of chorea, the cardinal motor feature in Huntington disease, as measured by change in the Unified Huntington's Disease Rating Scale (UHDRS®) Total Maximal Chorea (TMC) score from baseline to the average score at weeks 10 and 12. " Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 " Dame Carol Robinson DBE, FRS, FRSC, FMedSci, Oxford University’s first female Professor of Chemistry, former president of the Royal Society of Chemistry and Founder of (and ongoing consultant to) OMass Therapeutics , which is based at Oxford Science Park, has been awarded the 2022 Louis-Jeantet Prize for Medicine. This is a highly prestigious international award – exemplified by the fact that other winners this year are the co-founders of BioNTech for their invention of the ( Pfizer ) Covid vaccine." Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 " Tokyo, Japan and Cambridge, UK, 24 December 2021 – Sosei Group Corporation (“ Sosei Heptares ”; TSE: 4565) today announces that in connection with the Collaboration and License Agreement (“License Agreement”) with Neurocrine Biosciences , Inc. (“ Neurocrine Biosciences ”) announced 22 November 2021, the applicable waiting period under the Hart-Scott-Rodino Antitrust Improvements Act of 1976 (“HSR Act”) expired on 22 December 2021. As such, the License Agreement became effective on 22 December 2021. With completion of the applicable waiting period under the HSR Act, under the terms of the License Agreement Neurocrine Biosciences has agreed to pay Sosei Heptares an upfront payment of US$100 million, with the amount to be recognized as revenue in the fourth quarter of the financial year ending December 31, 2021." Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 "Meet Peter McNamara , Ph.D., Tectonic ’s SVP, Head of Research. Peter joined Tectonic to help chart new territory in GPCR science. We’re glad to have Peter's dedication, experience, and passion in building innovative therapeutics." Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "OXFORD, England--Professor Charlotte Deane , Ph.D., of the University of Oxford , has joined Exscientia as Chief Scientist of Biologics AI. In this newly created role, she will focus on the application of artificial intelligence (AI), machine learning, and the design of protein structures in the discovery and development of novel drug candidates. Professor Deane joins Exscientia’s technology leadership team, reporting to Chief Technology Officer, Garry Pairaudeau . Professor Deane is one of the UK’s most accomplished bioinformaticians. She has held numerous senior roles at the University of Oxford , where she is currently Professor of Structural Bioinformatics and leads the University’s Protein Informatics group. She will maintain both of these roles, in addition to her role at Exscientia . Prior to this, Professor Deane was Deputy Executive Chair of the Engineering and Physical Sciences Research Council at UK Research and Innovation (UKRI). She has played an active role during the COVID-19 pandemic as the UKRI’s COVID Response Director, and was a member of SAGE, the UK Government’s Scientific Advisory Group for Emergencies. Professor Deane holds a B.A. in Chemistry from the University of Oxford and a Ph.D. in Biochemistry from the University of Cambridge ." R ead more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "G-protein-coupled receptors’ star has been on the rise in biotech in recent years as researchers have discovered the vast potential for GPCR-targeting drugs in treating a range of health conditions, from cancer and genetic disorders to inflammation and metabolic imbalances. Among those hitching their wagons to that star are Verily and Sosei Heptares , which have struck a research agreement to discover new GPCR targets that’ll fuel the development of potential drug candidates. The financial details of the strategic collaboration weren’t released, but Sosei Heptares ’ past two team-ups in GPCR-based drug discovery have clocked in at $1 billion—with Genentech—and, just last November, $2.6 billion in a partnership with Neurocrine." Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "The Neurocrine Biosciences story puts into words what makes the work and people at Neurocrine Biosciences so special. It captures our values and vision for the future, our culture, and our unique approach to science. Simply put, it represents what we do and why we do it. Hear the story from our colleagues in this video." Read more at the source #DrGPCR #GPCR #IndustryNews

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 within the European Union in combination with a rituximab or cyclophosphamide regimen for the treatment of adult patients with severe, active granulomatosis polyangiitis (GPA) or microscopic polyangiitis (MPA), the two main forms of ANCA-associated vasculitis. This approval follows the U.S. Food and Drug Administration (FDA) approval of TAVNEOS in October 2021. TAVNEOS will receive marketing authorization in all member states of the European Union, as well as in Iceland, Liechtenstein and Norway." Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "After securing FDA approval for Wegovy last year, Novo Nordisk is strengthening its position in the obesity space through a collaboration with EraCal Therapeutics. Under the joint research plan, the Danish giant will work with EraCal to identify novel drug targets relevant for food intake regulation and additional metabolic phenotypes. Although specific details of the collaboration are yet to be released, EraCal has confirmed that the duo will utilise its phenotypic drug discovery platform to identify potential targets." Re ad more at the source #DrGPCR #GPCR #IndustryNews

February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with pioneer as co-founder "J an 27, 2022 07:00am Septerna wants to spark a second golden age in G-protein-coupled receptor drug discovery. Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous decades—but the two-year-old biotech believes the area is still ripe for development, and it now has $100 million to help power its efforts. The company's co-founder, GPCR pioneer and Nobel laureate Robert Lefkowitz , M.D., has 50 years of experience with the target and analogizes the search for new drugs to oil drilling around the world." Read more at the source #DrGPCR #GPCR #IndustryNews

February 2022 " InterAx Biotech AG and Boehringer Ingelheim take first steps towards collaborating to unlock orphan targets leveraging InterAx AI driven discovery platform. Collaborative efforts aim to accelerate and improve the prediction of first-in-class small molecule agonists for a challenging orphan GPCR for a highly relevant therapeutic need. 💊 InterAx Biotech AG discovery platform was already successfully applied in projects with biopharmaceutical companies and also used in-house to discover first-in-class compounds for a novel oncology target that are now being tested in-vivo. #ai #biotech #systemsbiology #drugdiscovery #gpcr #deeptech #orphandrugs #pharma #partnerships #AI4drugdiscovery" Read more at the source #DrGPCR #GPCR #IndustryNews

February 2022 " Ermium Therapeutics Announces the Formation of a Scientific Advisory Board comprising international leaders in GPCRs pharmacology, immunology, drug discovery and development for auto-immune diseases" Read more at the source #DrGPCR #GPCR #IndustryNews

March 2022 ERNEST has established an Emergency Fund for Ukrainian researchers. "General Eligibility Researchers affiliated to any legal entity in Ukraine (for example, schools and universities, research centers, governmental institutions, or private companies) Deadlines Start of the project: now End of the project: 31 October 2022 SHORT-TERM SCIENTIFIC MISSIONS (STSM) We offer short-term scientific mission grants to Ukrainian researchers who have been recently displaced by the war, or those who can travel to institutions participating in ERNEST COST Action. The purpose of the STSM is to carry out a collaborative research project on topics relevant to the network. Our scientific perspective is broad, and we are happy to consider any research proposals from those in need." Read more at the source #DrGPCR #GPCR #IndustryNews