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.

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Development

A journal article titled “A Novel Somatostatin Receptor Ligand for Human ACTH- and GH-secreting Pituitary Adenomas” has been published in the European Journal of Endocrinology

By Sosei Heptares Research Team | Jan 4, 2024

A journal article has been published on a study conducted by members of the Sosei Heptares team in the European Journal of Endocrinology. In this study, HTL0030310 was found to inhibit hormonal secretion in human ACTH- and GH-secreting pituitary adenomas in vitro. HTL0030310 is a novel somatostatin receptor agonist which is selective for subtype 5 over subtype 2, thus with a different receptor profile compared to clinical somatostatin receptor ligands.

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Platform Technology

Sosei Heptares presenting novel Computational Chemistry and Cheminformatics approaches for GPCR SBDD at UK QSAR Spring Meeting 2023

By Sosei Heptares Computational Chemistry Team | Apr 20, 2023

The biannual meetings of the UK QSAR and Cheminformatics Group offer an opportunity for a community drawn from both academia and industry to present the latest developments in the field of chemical property prediction, data analysis and molecular modelling.

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Drug Discovery

A review paper entitled ‘A Growing Understanding of the Role of Muscarinic Receptors in the Molecular Pathology and Treatment of Schizophrenia,’ has been published in Frontiers of Cell

By | Mar 1, 2023

A review paper co-authored by members of our Translational Medicine team* and others, entitled ‘A Growing Understanding of the Role of Muscarinic Receptors in the Molecular Pathology and Treatment of Schizophrenia,’ has been published in Frontiers of Cellular Neuroscience. The paper explores the evidence for the critical role that the muscarinic M1 and M4 receptors have in CNS functions that are dysregulated by the pathophysiology of schizophrenia. 

*Geor Bakker, External Consultant to Sosei Heptares – Translational Medicine (Neuroscience), Alastair Brown, Senior Vice President, Translational Medicine 

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Platform Technology

Sosei Heptares presents latest methodological advances in Computer-Aided Drug Design Capabilities for GPCR SBDD at leading Computational Chemistry and GPCR conferences

By Sosei Heptares Computational Chemistry Team | Oct 2, 2022

Brian Bender, Pierre Matricon and Chris de Graaf from the Sosei Heptares Computational Chemistry team have recently presented Sosei Heptares’ methodological advances in Computer-Aided Drug Design (CADD) capabilities for GPCR Structure-Based Drug Discovery (SBDD) at leading GPCR and Computational Chemistry conferences: 4GPCRnet International Symposium 2022, 23rd EuroQSAR meeting, and 2022 Computational Chemistry Gordon Research Conference (GRC).

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Drug Discovery

Verily and Sosei Heptares Highlight Early Success of Strategic Collaboration to Identify GPCR Targets for Immune-mediated Diseases

By | Sep 1, 2022

Application of Verily Immune Profiler enables prioritization of GPCR targets with strong potential for future Drug Discovery

Drug targets selected by combining genetic or genomic data with mechanistic evidence for roles in human diseases hold the greatest potential for therapeutic development. This has formed the basis for an ongoing drug-discovery collaboration between Verily, developer of the Immune Profiler platform, and Sosei Heptares, a world-leader in G protein-coupled receptor (GPCR) structure-based drug design, which in just six months has reached its first milestones in identifying and prioritizing targets that are now entering validation, hit generation, and lead selection over the next year. 

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Drug Discovery

Targeting the M1 muscarinic receptor in neurodegenerative disease: the role of receptor phosphorylation

By Sophie Bradley | Aug 25, 2022

Sophie Bradley, an associate director in our Pre-Clinical Translational Neuroscience department, presented at the FASEB G Protein-coupled Receptor Kinases and Arrestins Conference: Key Modulators of Signal Transduction. The presentation focussed on the M1 receptor as a potential therapeutic target in neurodegenerative disease and highlighted research conducted at both Sosei Heptares and the University of Glasgow. 

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Platform Technology

Sosei Heptares presents latest methodological advances in AI applied to SBDD at 12th International Conference on Chemical Structures, the Netherlands

By Sosei Heptares Computational Chemistry Team | Aug 10, 2022

The International Conference on Chemical Structures (ICCS) takes place every three years at Noordwijkerhout (the Netherlands), bringing together experts in the field of cheminformatics (including AI/machine learning) from both academia and industry. Due to the pandemic, the 12th meeting (June 12-16 2022) took place after a four-year gap and thus it gave an opportunity for the community to come together after a long hiatus. Three representatives from Sosei Heptares presented their work this year: Mr Morgan Thomas, Ms Dominique Sydow and Dr Noel O’Boyle.

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Drug Discovery

Discovery of HTL0039732: A Potent and Selective EP4 Receptor Antagonist for Cancer Immunotherapy

By Nigel Swain | Aug 7, 2022

Nigel Swain, a senior director in our Medicinal Chemistry department, recently presented at the 2022 Medicinal Chemistry Gordon Research Conference, showcasing rational design using Structure Based Drug Design (SBDD) and X-ray crystallography of the Sosei Heptares EP4 receptor antagonist preclinical candidate HTL0039732.

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Development

Targeting the M1 muscarinic receptor in neurodegenerative disease

By Sophie Bradley | Apr 12, 2022

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 characterising the role of the muscarinic M1 receptor in cognitive and neurodegenerative disorders and the potential therapeutic benefit of muscarinic M1 selective ligands.

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Development

Identification and characterisation of a dual GLP-1/GLP-2 agonist peptide, HTL0030023 using structure based drug design

By Rie Suzuki | Mar 29, 2022

Rie Suzuki, Director Translational Sciences at Sosei Heptares presented a poster at the American Chemical Society (ACS) Spring 2022 meeting, describing the design strategy and pharmacodynamic evaluation of HTL0030023, a novel GLP-1/ GLP-2 agonist.  

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Development

Identification and characterisation of a novel GLP-1 receptor antagonist peptide HTL0033097

By Alastair Brown | Mar 29, 2022

Alastair Brown, VP Translational Sciences at Sosei Heptares presented a poster at the American Chemical Society (ACS) Spring 2022 meeting, describing the design strategy and pharmacodynamic evaluation of HTL0033097, a novel selective GLP-1 antagonist.  

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Development

Identification of Subtype Selective SST5 Receptor Agonist Peptide HTL0030310 using Structure-Based Drug Design

By Miles Congreve | Mar 29, 2022

Miles Congreve, CSO at Sosei Heptares presented a poster at the American Chemical Society (ACS) Spring 2022 meeting, describing the SBDD based identification of HTL0030310, a novel selective SST5 agonist.  

 

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Drug Discovery

How an AI drug discovery collaboration between Sosei Heptares and PharmEnable is accelerating complex science: generating new hit molecules against a difficult GPCR target

By Sosei Heptares and PharmEnable | Jan 25, 2022

Artificial Intelligence (AI) is becoming an increasingly important part of drug discovery – as demonstrated by the significant progress in the ongoing collaboration between Sosei Heptares and PharmEnable focused on a challenging peptidergic G protein-coupled receptor (GPCR) target associated with neurological disease. The collaboration brings together Sosei Heptares’ expertise in GPCRs with PharmEnable’s AI technology and has greatly accelerated the usual timelines for such a project. Matt Barnes, VP Drug Discovery at Sosei Heptares, and James Dale, Director of Drug Discovery at PharmEnable, tell us more.

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Development

From structure to clinic: Design of a M1 muscarinic acetylcholine receptor agonist with the potential for symptomatic treatment of Alzheimer’s disease

By Sosei Heptares | Nov 24, 2021

An extensive review in the prestigious journal Cell describes ground-breaking research – led by Sosei Heptares in collaboration with the University of Glasgow and others – that describes, for the first time, the process of designing a new molecule (HTL9936) to selectively target the muscarinic M1 receptor in the brain and demonstrating, through laboratory preclinical and human clinical studies, the potential of this approach to create superior new drugs to improve cognitive function in Alzheimer’s Disease patients, while minimizing side-effects associated with previous attempts to target the M1 receptor.   

 

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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).

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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.

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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.

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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.

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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.

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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".

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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.

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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.

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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.

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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.

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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.

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