August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic reticulum membrane associated with mitochondria. It is classified into two types: Sigma-1 (S1R) and Sigma-2 (S2R) based on their biological functions. S1R has been implicated in many neurological disorders such as anxiety, schizophrenia, and depression. Therefore, S1R ligands possess a variety of potential clinical applications with a great interest in the treatment of neuropathic pain. In this study, we report the discovery of a novel lead compound for S1R binding, based on the thiazolidine-2,4-dione nucleus. We have explored hydrophobic groups of different sizes on both sides of the five-membered ring scaffold guided by the crystal structure of S1R. Six compounds showed more than 50% displacement of the radioligand at 10 µM concentration with compound 6c resulting in 100% displacement and a Ki of 95.5 nM. Moreover, compounds 6c and 6e showed a significant selectivity over S2R. In addition, molecular docking predicted that all the compounds showed the critical salt bridge with Glu172 with variable degrees of π-stacking interaction with Tyr103. Upon optimization, this series of compounds could represent potential clinically useful S1R ligands for pain management." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Abstract Rodent models are commonly used to evaluate parathyroid hormone (PTH) and PTH-related protein (PTHrP) ligands and analogues for their pharmacologic activities and potential therapeutic utility toward diseases of bone and mineral ion metabolism. Divergence, however, in the amino acid sequences of rodent and human PTH receptors (rat and mouse PTH1Rs are 91% identical to the human PTH1R) can lead to differences in receptor-binding and signaling potencies for such ligands when assessed on rodent vs human PTH1Rs, as shown by cell-based assays in vitro. This introduces an element of uncertainty in the accuracy of rodent models for performing such preclinical evaluations. To overcome this potential uncertainty, we used a homologous recombination-based knockin (KI) approach to generate a mouse (in-host strain C57Bl/6N) in which complementary DNA encoding the human PTH1R replaces a segment (exon 4) of the murine PTH1R gene so that the human and not the mouse PTH1R protein is expressed. Expression is directed by the endogenous mouse promoter and hence occurs in all biologically relevant cells and tissues and at appropriate levels. The resulting homozygous hPTH1R-KI (humanized) mice were healthy over at least 10 generations and showed functional responses to injected PTH analog peptides that are consistent with a fully functional human PTH1R in target bone and kidney cells. The initial evaluation of these mice and their potential utility for predicting behavior of PTH analogues in humans is reported here." Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 "Not even a PIPE financing could save X4 Pharmaceuticals from enacting layoffs and trimming its pipeline. The Boston biotech revealed Wednesday afternoon that it would downsize its research to focus on its lead program, mavorixafor, and lay off about 20% of its staff. The move comes less than three weeks after X4 pulled together a $55 million PIPE and amended a loan facility with Hercules Capital to reduce cash burn." Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 "I’m happy to share that I’m starting a new position as Scientific co-founder LASEREDD Therapeutics " Ross Bathgate Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 "July 19, 2022 07:00 AM Eastern Daylight Time BOSTON-- Tectonic Therapeutic , Inc. a pre-clinical stage biotechnology company transforming the discovery of novel GPCR-targeted therapies (G-Protein Coupled Receptors), today announced the promotion of Senior Vice President, Head of Research, Peter McNamara , PhD, to Chief Scientific Officer as well as the appointments of Barry Rubenstein as Senior Vice President, People and Culture and Washington Alves as Vice President, Biologics Manufacturing." Read more at the source #DrGPCR #GPCR #IndustryNews

"We recently hosted our annual Scientific Advisory Board (SAB) summit at our site within Granta Park. It was great to bring everyone together and also welcome new member John Parkinson ." 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 today that it has been awarded a €1.7 million grant from the Flemish Agency for Innovation and Entrepreneurship (VLAIO). 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 "Today we are celebrating ten years of Exscientia ! Founded as a spinout from the University of Dundee on 20 July 2012, Exscientia pioneered the design of novel compounds through artificial intelligence. We have achieved a great deal in the last decade, such as the first-ever AI-designed drug candidates to enter clinical trials, the first AI-driven precision medicine platform clinically validated to guide treatment selection in patients with advanced haematological cancers, international partnerships with pharma and healthcare foundations, and the establishment of a global company with locations in the UK, U.S., Austria, and Japan which IPO’d in October last year. We’re excited about delivering the next ten years of Exscientia and advancing AI to design better drugs, faster. #artificialintelligence #drugdesign #drugdiscovery" Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 " G.CLIPS biotech is 2 years old today🎂. When I came this morning to work this is how I found my desk. So very grateful to the great hard working team we have and all the great achievements we have done together. Looking forward for more 🎊 #team #grateful #biotech #work #birthdaycelebration" Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 " Ad Hoc Announcement Pursuant to Art. 53 LR Geneva, Switzerland, July 22, 2022 – 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 Master Fund LTV, a healthcare-focused institutional investor, to sell 3,300,000 shares in the form of 550,000 American Depositary Shares (“ADSs”) at a gross purchase price of $1.70 per ADS, which is equivalent to CHF 0.27 per share. Each ADS represents six shares. Additionally, Addex has agreed to issue to Armistice Capital unregistered pre-funded warrants to purchase up to 11,700,000 shares in the form of 1,950,000 ADSs (the “Unregistered Pre-Funded Warrants”) at a funded amount of $1.69 with $0.01 payable on exercise as well as unregistered warrants to purchase up to 15,000,000 shares in the form of 2,500,000 ADSs (the “Unregistered Warrants” and together with the “Unregistered Pre-Funded Warrants”, the “Warrants”) in a concurrent private placement. The Unregistered Warrants have an exercise price of $1.90 per ADS, will become exercisable in 60 days after their date of issuance and will expire five years from their date of issuance. " 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 cancers in combination with other immunotherapies Tokyo, Japan, London and Cambridge, UK, 22 July 2022 – Sosei Group Corporation (“the Company”; TSE: 4565), an international biopharmaceutical 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 to bring Sosei Heptares ’ cancer immunotherapy drug candidate into a first-in-human trial." 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. Since then, Celniker has helped usher in an additional fund and headed a few startups as interim CEO. Coming on its 15th year, Third Rock Ventures announced its sixth fund today — and largest one by far — at a whopping $1.1 billion. Adding it all up, Third Rock has raised $3.8 billion since its inception. That money has gone to some 60 biotechs, much of it as early funding." Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "We’re delighted to welcome Dr Ed Brennan as our new Vice President, Head of Clinical Development. Dr Brennan has extensive experience across all phases of clinical development, and across multiple therapeutic areas, including Oncology, Infectious Diseases, Immunology and Critical Care. He has led teams that have filed more than 10 Investigational New Drug Applications (IND), as well as multiple New Drug (NDA) and Supplemental New Drug Applications (SNDA). Previous companies worked at include OrthoBiotech (OBI), a division of Johnson & Johnson and GlaxoSmithKline Consumer Healthcare , L.P. In 2007 he formed IndiPharm which was a full-service Contract Research Organization whose operational headquarters were in Mumbai, India. In 2016 the company was sold to Velocity fund partners and has been rebranded as InClinica . He received his undergraduate Bachelor of Science Degree in Pharmacy from The Philadelphia College of Pharmacy and Science. He went on to study medicine at the Royal College of Surgeons in Ireland before receiving his Medical Degree from Temple University – Lewis Katz School of Medicine. #biotech #lifesciences #appointment #GPCR #Oncology" Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "Ottawa, Canada, May 10, 2022 — Orion Biotechnology Canada Ltd, a drug discovery and development company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs), today announced that it will be presenting important new data at both LSX World Congress and TIDES USA 2022 conference, taking place this week – May 10-12, 2022. Dr. Oliver Hartley , Orion’s Vice-President Drug Discovery, will present Orion’s novel technology for targeting undrugged peptidergic GPCRs. His presentations will describe Orion’s drug discovery platform, one of the fastest drug discovery solutions in the industry for targeting peptidergic GPCRs. Dr. Hartley will also present new data on Orion’s CCR2 antagonist, OB-004, demonstrating the ability of this powerful platform to rapidly identify best-in-class GPCR drug candidates." Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "CRN04894 Selected for Oral Presentation SAN DIEGO, June 8, 2022 — Crinetics Pharmaceuticals , Inc. (Nasdaq: CRNX), announced that results from the company’s Phase 1 study of CRN04894, the company’s investigational candidate for the treatment of Cushing’s disease, congenital adrenal hyperplasia (CAH) and other conditions driven by excess adrenocorticotropic hormone (ACTH), were selected for an oral presentation at ENDO 2022, the Endocrine Society’s annual meeting. Crinetics recently reported that administration of CRN04894 reduced both serum cortisol levels and 24-hour urine free cortisol excretion in the presence of sustained, disease-like ACTH concentrations in multiple-ascending dose cohorts of a Phase 1 study." Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital Adrenal Hyperplasia at ENDO 2022 "06/13/22 - Substantial Reductions in Key Hormones and Hormone Precursors Observed After 14 Days of Crinecerfont Treatment in Adolescents with Classic CAH - Two Phase 3 Global Registrational Studies Currently Underway in Pediatric (2–17 years of age) and Adult (18 years of age and older) Patients with Classic CAH SAN DIEGO, June 13, 2022 -- Neurocrine Biosciences , Inc. (Nasdaq: NBIX) today announced that it will present new Phase 2 data on the use of crinecerfont in adolescent patients with classic congenital adrenal hyperplasia (CAH) due to 21-hydroxylase deficiency (21-OHD), which demonstrated substantial reductions in adrenal androgens and androgen precursors. These data will be shared as an oral presentation by Ron S. Newfield, M.D., University of California , San Diego and Rady Children's Hospital, San Diego on June 13 from 11:00 a.m.–12:30 p.m. ET (Presentation #OR18) at ENDO 2022, the Endocrine Society's 104th annual meeting in Atlanta from June 11–14. The company also presented data highlighting patient preferences and treatment patterns in classic CAH in Hall A1 on Saturday, June 11." Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "G protein-coupled receptors (GPCRs) represent a major therapeutic target class as they play a key role in many (patho-) physiological processes. GPCRs are divided into six classes based on amino acid sequence similarities, but only four of the classes (A, B, C, and F) are found in humans. GPCRs respond to a wide variety of signals that range in size from photons to proteins (Foord et al., 2005). GPCRs continue to be regarded as one of the most tractable classes of drug targets and are targeted by 30%–40% of current drugs (Hauser et al., 2017), with annual sales of GPCR-targeting drugs in 2018 accounting for >114 billion USD. In 2019, 5 out of 20 first-in-class approved therapeutic agents targeted GPCRs. Despite this high number of GPCR targeted drugs, only a small portion (∼110) of the human GPCRome (consisting of approximately 850 GPCRs) has been successfully drugged, and obtaining highly potent and selective small molecules remains a challenge for the remainder." Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "Published on juin 22, 2022 On June 22, 2022, Michel Bouvier , Chief Executive Officer of IRIC, Principal Investigator of the Molecular Pharmacology Research Unit and Professor in the Department of Biochemistry and Molecular Medicine of the Faculty of Medicine of the Université de Montréal , is appointed Knight of the Ordre national du Québec. This honorary decoration, bestowed today by the government of Quebec, is the highest honour in Quebec aimed at promoting excellence. It has been awarded annually since 1985 to distinguished individuals who have strived, in an exceptional way, to enhance Quebec’s image. The rank of Knight specifically rewards the implementation of an exemplary activity in a particular field." Read more at the source #DrGPCR #GPCR #IndustryNews

May 2022 " MONTREAL (CANADA) – May 17, 2022 – Inversago Pharma Inc. (“Inversago”), a clinical stage biotech company with a unique portfolio of CB1 inverse agonists, today announces the appointment of Glenn S. Vraniak to the position of Chief Financial Officer (CFO), effective immediately. Mr. Vraniak’s career spans more than 20 years of financial and commercial experience in the life sciences industry. Before joining Inversago, Mr. Vraniak served as Chief Financial Officer of Evaxion Biotech A/S, an AI enabled immuno-oncology company and led the company through a successful IPO on Nasdaq in February 2021, and successfully raised follow-on capital later that same year. Prior to that, Mr. Vraniak served as the Chief Financial Officer of electroCore, Inc. and was a key member of the management team that led the company through a successful IPO on Nasdaq in June 2018. Additionally, Mr. Vraniak served as an executive in various innovative healthcare and technology companies including GE Capital, where he served as Executive Vice President." Read more at the source #DrGPCR #GPCR #IndustryNews

May 2022 "We are thrilled to announce that our co-founder Margaux Duchamp has been selected as a 30 under 30 Europe Forbes ranking 2022 for science and healthcare. #ForbesUnder30 #ArcoScreen #sciences #EPFL" Read more at the source #DrGPCR #GPCR #IndustryNews

May 2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR Targets for Drug Discovery " Collaboration is part of Sosei Heptares ’ Target Identification and Validation (TIV) strategy to leverage multiple sophisticated technologies that drive creation of new drug discovery programs in key therapeutic areas Kallyope, pioneers in drug discovery involving the gut-brain axis, will gain unique and valuable access to the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR targets and advance the development of new gastrointestinal therapeutics Tokyo, Japan, Cambridge, UK and New York, USA – May 17, 2022 – Sosei Group Corporation, the international biopharmaceutical company, and New York City-based Kallyope , pioneers in drug discovery involving the gut-brain axis, have entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR) targets with a goal of creating new drug discovery programs in the area of gastrointestinal diseases. " Read more at the source #DrGPCR #GPCR #IndustryNews

May 2022 "Published: May 10, 2022 To accelerate clinical development of its best-in-class and first-in-class immuno-oncology programs STRASBOURG, France & MONTREAL- Domain Therapeutics , a biopharmaceutical company specializing in the research and development of innovative drugs targeting G Protein-Coupled Receptors (GPCRs) in immuno-oncology, announced today the closing of a US $42m (€39m) series A financing round co-led by Panacea Venture, CTI Life Sciences and 3B Future Health Fund, and joined by adMare BioInnovations , Schroders Capital, Omnes, Turenne Capital, Theodorus, Viva BioInnovator and existing investor Seventure Partners." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 "By Sophie Bradley | Apr 12, 2022 Summary Sophie Bradley, Translational Sciences Associate Director at Sosei Heptares , recently presented at the Keystone Symposia GPCR 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 benefit of muscarinic M1 selective ligands." Read more at the source #DrGPCR #GPCR #IndustryNews

May 2022 "Seoul, South Korea, 28 April 2022 – GPCR therapeutics , Inc., a venture-backed clinical stage international biopharmaceutical company with an innovative approach to drug discovery based on targeting G Protein Coupled Receptors (GPCR) pairs, today announced four appointments to its Scientific Advisory Board (SAB). Dr. Michel Bouvier , Dr. Luisa Salter-Cid , Dr. Omar Nadeem and Dr. Jon Wigginton will provide scientific expertise to support the company’s research and clinical development. GPCR just had a very successful first meeting including all the Scientific Advisory Board." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 John Streicher talks about his work on terpenes found in cannabis as these may be a novel way to treat pain without the negative side effects " Many people are familiar with cannabis, but John Streicher , PhD, takes a closer look at the plant’s aromatic chemical compounds called terpenes. These compounds may be a novel way to treat pain without the negative side effects of cannabinoids or opioids." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Trevena Announces Receipt of First $15 million Tranche in Connection with its $40 million ex-US Royalty-Based Financing with R-Bridge Healthcare Fund " CHESTERBROOK, Pa., April 18, 2022 - 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 receipt of the first $15 million tranche from its royalty-based financing agreement with an affiliate of R-Bridge Healthcare Fund (the R-Bridge Financing)." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders with Tim Dyer Addex Therapeutics " Tim Dyer is the Co-Founder and CEO of Addex Therapeutics , which is focusing on the pharmacology known as allosteric modulation. This emerging class of small molecule drugs known as allosteric modulators is being explored for treating central nervous system and neurologic disorders, particularly movement disorders like dyskinesia associated with Parkinson's and dystonia. Addex did not invent allosteric modulation but is pioneering the screening technologies to find these difficult to locate molecules." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Trevena Receives up to $40M in OLINVYK ex-US Royalty-Based Financing from R-Bridge Healthcare Fund, an affiliate of CBC Group " CHESTERBROOK, Pa., March 31, 2022 -- 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 that the Company entered into a royalty-based financing with an affiliate of R-Bridge Healthcare Fund (the R-Bridge Financing)." Read more at the source #DrGPCR #GPCR #IndustryNews