ABOUT US OUR SCIENCE OUR PIPELINE OUR MEDICINES MINORITY INVESTMENTS INVESTORS SEARCH NEWSROOM SCIENCE CENTER - CHISHIKI CAREERS CONTACT Science Center - CHISHIKI Sosei Heptares group welcomes you to CHISHIKI, the destination for updates on our progress in the world of GPCRs. CHISHIKI is the Japanese word for “knowledge.” CHISHIKI is our online voice for communicating the scientific progress of our research and development activities, together with our broader contributions to the area of GPCRs. RSS Feed Page 1 of 3 > >> PLATFORM TECHNOLOGY Sosei Heptares boosts Artificial Intelligence and Computer-Aided Drug Design capabilities focused on GPCR-targeted drug discovery with new partnered initiatives By Sosei Heptares | Oct 20, 2021 Sosei Heptares has recently presented progress in the development of novel approaches in combining AI molecule generation and GPCR Structure-Based Drug Design (SBDD) and will be participating in new collaborative initiatives in training in AI and Computer-Aided Drug Discovery (CADD). READ MORE... DRUG DISCOVERY The Identification of GPR52 Agonist HTL0041178, a potential therapy for schizoaffective and related psychiatric disorders By Steve Watson | Sep 22, 2021 Steve Watson, Medicinal Chemistry Director at Sosei Heptares, recently attended the 21st RSC/SCI Medicinal Chemistry Symposium and presented “The Identification of GPR52 Agonist HTL0041178: A potential therapy for schizoaffective & related disorders” – the first public disclosure of HTL0041178. READ MORE... DRUG DISCOVERY Decoding the activity of acetylcholine in memory formation and opportunities for drug discovery By Sosei Heptares | Sep 16, 2021 A research collaboration between the University of Bristol’s Centre for Synaptic Plasticity and Sosei Heptares has identified specific drug targets within neural circuits in the brain that encode memories, paving the way for significant advances in the treatment of a broad spectrum of brain disorders. READ MORE... DEVELOPMENT Flattening the ‘valley of death’: New tools in the hunt for better preclinical R&D By Paul Morgan | Feb 23, 2021 Paul Morgan, Vice President Preclinical Development at Sosei Heptares, was recently invited to be part of a panel of senior pharma executives to discuss key trends and challenges faced by the industry in preclinical R&D. The webinar, hosted by Endpoints News, will be broadcasted on February 23, 2021 at 2-3pm EST. READ MORE... DEVELOPMENT Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity By Sosei Heptares | Jul 30, 2020 Our publication, jointly authored with AstraZeneca, titled “Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity” was accepted into the Journal for ImmunoTherapy of Cancer. READ MORE... DRUG DISCOVERY Accurate Prediction of GPCR Ligand Binding Affinity with Free Energy Perturbation By Francesca Deflorian et al. | Jun 26, 2020 Francesca Deflorian, Senior Scientist II, Computational Chemistry, together with fellow scientists from Sosei Heptares, Janssen Pharmaceutica N. V., and Leiden University, recently published a paper in Journal of Chemical Information and Modeling. Alchemical relative binding free energy (RBFE) calculations were performed on two GPCR systems, the adenosine A2A and the orexin 2 receptors, investigating parameters and protocols to improve the accuracy of the predictions and emphasizing GPCR-specific features. READ MORE... DRUG DISCOVERY Structure-Based Drug Discovery of HTL22562: a CGRP Receptor Antagonist For Acute Treatment of Migraine By Sarah Bucknell et al. | Jun 23, 2020 Sarah Bucknell, Senior Scientist II Chemistry, together with fellow scientists from Sosei Heptares and Teva Pharmaceuticals, recently published a paper in the Journal of Medicinal Chemistry, titled "Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): a Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist For Acute Treatment of Migraine". READ MORE... DRUG DISCOVERY Preclinical Pharmacodynamic and Pharmacokinetic Characterisation of HTL A a Selective GPR52 Agonist By Clíona MacSweeney et al. | May 7, 2020 Clíona MacSweeney, Associate Director, Translational Sciences at Sosei Heptares, recently shared her poster describing the pharmacodynamic and pharmacokinetic characterisation of our novel GPR52 agonist on the Society of Biological Psychiatry 75th Anniversary Meeting website portal. READ MORE... DRUG DISCOVERY Discngine announces that Sosei Heptares will use its 3decision® software to create an unprecedented structural GPCR chemogenomics platform By Chris de Graaf | Apr 6, 2020 Discngine, a software company specializing in developing applications for life sciences research, announced today that Sosei Heptares, an international biopharmaceutical group focused on G protein-coupled receptors (GPCRs), has selected its 3decision software to be part of an unprecedented structural GPCR chemogenomics platform. READ MORE... DRUG DISCOVERY Impact of GPCR Structures on Drug Discovery By Miles Congreve, Chris de Graaf, Nigel Swain, Christopher Tate | Apr 6, 2020 Co-founder Christopher Tate and scientists from Sosei Heptares recently published a paper in Cell which reviews the state of the art of GPCR structural biology and how it correlates with launched GPCR drugs and agents in clinical trials. READ MORE... DRUG DISCOVERY Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification By Mathew Leveridge et al. | Jan 28, 2020 Mathew Leveridge, Senior Scientist, Pharmacology, attended the SLAS (Society for Laboratory Automation and Screening) 2020 conference in San Diego on 25-29th Jan to present on Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification. READ MORE... DRUG DISCOVERY Comparison of orexin 1 and orexin 2 ligand binding modes using X-ray crystallography and computational analysis By Mathieu Rappas et al. | Dec 22, 2019 Mathieu Rappas, Head of Protein Expression and Biochemistry at Sosei Heptares, together with fellow scientists, recently published a Featured Article titled “Comparison of orexin 1 and orexin 2 ligand binding modes using X-ray crystallography and computational analysis” in the renowned Journal of Medicinal Chemistry. In the paper he presents X-ray structures of the orexin receptors in complex with ten new antagonist ligands from diverse chemotypes and discusses how selectivity between OX1 and OX2 can be achieved. READ MORE... DRUG DISCOVERY Development of Histamine H4 Receptor Target Engagement Assays in Immune Cell Populations Involved in Atopic Dermatitis Pathophysiology By Eugenia Sergeev et al. | Dec 18, 2019 Eugenia Sergeev, Research Scientist, Molecular Pharmacology, attended Pharmacology 2019 organised by the British Pharmacological Society held on 15-17 December in Edinburgh, UK to present on Development of Histamine H4 Receptor Target Engagement Assays in Immune Cell Populations Involved in Atopic Dermatitis Pathophysiology. READ MORE... DRUG DISCOVERY Pharmacological characterisation of the LPS challenge human whole blood assay demonstrates EP4 dominance as a target engagement marker By Hannah Neale et al. | Dec 18, 2019 Hannah Neale, Scientist, Molecular Pharmacology, attended Pharmacology 2019 organised by the British Pharmacological Society held on 15-17 December in Edinburgh, UK to present on Pharmacological characterisation of the LPS challenge human whole blood assay demonstrates EP4 dominance as a target engagement marker. READ MORE... DRUG DISCOVERY Discovery of A2AR antagonist HTL1071/AZD4635 using SBDD By Miles Congreve | Dec 13, 2019 Miles Congreve, Chief Scientific Officer at Sosei Heptares, recently attended the 24th Japanese Foundation for Cancer Research-International Symposium on Cancer Chemotherapy (JFCR-ISCC) named “New Drugs in Development in Japan, Europe and the USA” held in Tokyo, Japan on 11-12 Dec and presented on discovery of A2AR antagonist AZD4635 (HTL1071) using SBDD. The presentation was based on the one given previously in the New Approaches in Medicinal Chemistry symposium in Cambridge, UK on 20 June 2019. READ MORE... DRUG DISCOVERY Modulation of dopaminergic and glutamatergic function by GPR52 agonist supports therapeutic utility as novel treatment for positive symptoms and cognitive dysfunction in psychotic disorders including schizopherenia By Cliona MacSweeney et al. | Dec 12, 2019 Cliona MacSweeney, Associate Director, Translational Sciences, attended American College of Neuropsychopharmacology (ACNP) 2019 in Florida, US on 8-11 December and presented on Modulation of dopaminergic and glutamatergic function by GPR52 agonist supports therapeutic utility as novel treatment for psychosis. READ MORE... DRUG DISCOVERY Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification By Greg Osborne | Nov 26, 2019 Greg Osborne, Principal Scientist, Molecular Pharmacology at Sosei Heptares, recently attended The European Laboratory Research & Innovation Group (ELRIG) conference named Drug Discovery 2019 at ACC in Liverpool, UK on November 6 and presented on “Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification”, at Hit Finding Strategies session. READ MORE... DRUG DISCOVERY Drug Discovery Using Stabilised GPCR Technology By Eugenia Sergeev | Nov 20, 2019 Eugenia Sergeev, Research Scientist, Molecular Pharmacology, attended the educational conference named “What A Chemist Needs To Know About Biology 1: In Vitro Biology” organised by SCI’s Young Chemists’ Panel within the Society of Chemical Industry (SCI) in London, UK on 11th November and delivered a lecture on “Drug Discovery Using Stabilised GPCR Technology”. READ MORE... PLATFORM TECHNOLOGY Expanding the scope of GPCR structure-based drug design with cryoEM By Stacey Southall, Mathieu Rappas, Gabriella Cseke, Giancarlo Tria, Rob Cooke | Nov 15, 2019 Stacey Southall, Associate Director, Head of Biophysics, attended the 27th Protein Structure Determination in Industry Meeting (PSDI) 2019 organised by AstraZeneca in Cambridgeshire, UK on 4th November and presented on “Expanding the scope of GPCR structure-based drug design with cryoEM”. READ MORE... PLATFORM TECHNOLOGY Protein Engineering of G-Protein Coupled Receptors Using Directed Evolution in Saccharomyces cerevisiae By Daniel Jones | Nov 15, 2019 Dr. Dan Jones, Research Scientist, Protein Engineering at Sosei Heptares, recently attended The European Laboratory Research & Innovation Group (ELRIG) conference named “Drug Discovery 2019” at ACC in Liverpool, UK on November 5 - 6 and presented on “Protein Engineering of G-Protein Coupled Receptors Using Directed Evolution in Saccharomyces cerevisiae”. READ MORE... DRUG DISCOVERY Computational Medicinal Chemistry Approaches for GPCR Structure-Based Drug Discovery By Chris de Graaf | Nov 1, 2019 Dr. Chris De Graaf, Head of Computational Chemistry at Sosei Heptares, recently attended the first conference of the European Research Network on Signal Transduction (ERNEST, COST Action CA18133) named “GPCR Pharmacology: Activation, signalling and drug design”, at the Queen’s University Belfast in Northern Ireland on October 28-30, 2019. As an invited speaker, he addressed several important repercussions and learnings from the analysis of GPCR structures for ligand design that should be transferable and relevant for many targets. READ MORE... CORPORATE Dr. Malcolm Weir and Dr. Chris Tate named as 2019 BBS Honorary Members By Dr. Malcolm Weir and Dr. Chris Tate | Oct 10, 2019 Dr. Malcolm Weir, Executive Vice President, Chief R&D Officer, and Dr. Chris Tate, founding scientist of Heptares Therapeutics Ltd. and a member of Sosei Heptares’ Scientific Advisory Board, have been selected as Honorary Members of The British Biophysical Society (BBS) for 2019. Cate MacPhee, Professor at the University of Edinburgh, was also named as a 2019 BBS Honorary Member alongside Dr. Malcolm Weir and Dr. Chris Tate. READ MORE... PLATFORM TECHNOLOGY Structure-based Drug Design for GPCRs By Jana Broecker, Mathieu Rappas, Robert Cooke | Oct 8, 2019 Jana Broecker, Senior Scientist, Protein Expression and Biochemist at Sosei Heptares, recently presented at an EMBO Workshop session named “Tools for Structural Biology of Membrane Proteins” in Hamburg, Germany on 7 - 9 October 2019. The presentation titled “Structure-based Drug Design for GPCRs”, co-authored by Sosei Heptares colleagues Mathieu Rappas and Robert Cooke, highlights the strong potential of GPCRs as a drug target and how Sosei Heptares’ proprietary StaR® technology has been revolutionary to GPCR drug discovery. READ MORE... DRUG DISCOVERY Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors By Rie Suzuki, Giles Brown, John Christopher, Conor Scully and Miles Congreve | Oct 4, 2019 Summary Dr. Rie Suzuki, Director, Translational Sciences at Sosei Heptares, recently published a Review article titled “Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors” in the Journal of Medicinal Chemistry, alongside Giles Brown from OMass Therapeutics and fellow Sosei Heptares colleagues John Christopher, Conor Scully and Miles Congreve. The article indicates how the recent emergence of three-dimensional structures of GPCRs such as GLP-1R and glucagon receptor has helped to drive the rational design of innovative peptide molecules that hold promise as novel peptide therapeutics in disease areas of high unmet needs. READ MORE... DEVELOPMENT Sosei Heptares scientists selected as guest speakers for NIHR Maudsley BRC Experimental Medicine and Neuroimaging Course By Pradeep Nathan, Geor Bakker | Sep 24, 2019 Prof. Pradeep Nathan and Dr. Geor Bakker from the Sosei Heptares Experimental Medicine (Neuroscience) team were invited to be guest lecturers of an Experimental Medicine and Neuroimaging Course organized by the National Institute for Health Research (NIHR) Maudsley Biomedical Research Centre. Hosted at the Institute of Psychiatry, Psychology and Neuroscience, Kings College London, the course showcased the latest neuroimaging techniques used in experimental medicine research. The course is also designed to train students and clinical fellows with skills in experimental medicine and imaging and facilitate academic-industry collaborations. READ MORE... 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