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

AstraZeneca presents new clinical data at the 2020 ASCO Virtual Scientific Program

By AstraZeneca | Jun 4, 2020

AstraZeneca presented new clinical data from its Phase 1a study with AZD4635, a next-generation immuno-oncology candidate, as a monotherapy and in combination with the PD-L1 antibody durvalumab (Imfinzi), in patients with advanced prostate cancer, at the 2020 ASCO Virtual Scientific Program (29-31 May 2020).

AZD4635 is a oral inhibitor of adenosine 2A receptor (A2AR) signaling discovered by Sosei Heptares and exclusively licensed to AstraZeneca in 2015.

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Drug Discovery

Preclinical Pharmacodynamic and Pharmacokinetic Characterisation of HTL A a Selective GPR52 Agonist

By Clíona MacSweeney, Simon Poulter, Nigel Austin, Andy Mead, Alastair Brown, Matt Barnes, Ben Grayson, Nagi Idris, Jo Neill, Steve Watson | 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, Greg Osborne, Chris de Graaf, Kirstie Bennett, Stacey Southall, Matt Barnes | 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, Ammar Ali, Kirstie Bennett, Jason Brown, Sarah Bucknell, Miles Congreve, Robert Cooke, Gabriella Cseke, Chris de Graaf, Andrew Doré, James Errey, Ali Jazayeri, Fiona Marshall, Jonathan Mason, Richard Mould, Jayesh Patel, Benjamin Tehan, Ma | 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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Drug Discovery

Development of Histamine H4 Receptor Target Engagement Assays in Immune Cell Populations Involved in Atopic Dermatitis Pathophysiology

By Eugenia Sergeev, Susan Brown, Nicola Davis, Kirstie Bennett, Greg Osborne, Richard May, Matt Barnes | 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.

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Drug Discovery

Pharmacological characterisation of the LPS challenge human whole blood assay demonstrates EP4 dominance as a target engagement marker

By Hannah Neale, Susan Brown, Kirstie Bennett, Jason Brown, Matt Barnes | 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.

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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.

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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, Steve Watson, Alastair Brown, Geor Bakker, Richard Mould, Matt Barnes, Pradeep Nathan | 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.

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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.

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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”.

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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”.

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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”.

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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.

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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.

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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.

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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.

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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.

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Drug Discovery

Discovery of Pre-Clinical Candidate Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist HTL0022562

By John Christopher | Sep 13, 2019

Dr. John Christopher, Director of Medicinal Chemistry at Sosei Heptares, recently attended the 20th SCI/RSC Medicinal Chemistry Symposium in Cambridge, UK on 8-11 September 2019 and presented on the application of structure-based drug discovery (SBDD) to the identification of the Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist HTL0022562.

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Corporate

Interview with Dr. Simon Gabe, a leading UK gastroenterologist

By | Sep 12, 2019

Dr. Rie Suzuki, Director, Translational hosts an interview with Dr. Simon Gabe, a leading UK gastroenterologist consulting at St Mark’s Hospital (London, UK), to talk about the devastating physical and emotional burden of gastrointestinal (GI) diseases such as Short Bowel Syndrome (SBS) and Inflammatory Bowel Disease (IBD).

Dr. Rie Suzuki is one of many scientists at Sosei Heptares involved in the development of new therapies for GI diseases, one of the Company’s core therapeutic areas.

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Corporate

Virtual Tour of Sosei Heptares’s State-of-the-Art R&D Center

By Sosei Heptares | Sep 12, 2019

Dr. Rie Suzuki, Director, Translational Sciences, leads us on a virtual tour of Sosei Heptares’s state-of-the-art UK R&D facilities in Granta Park, Cambridge. The new 35,000 square foot facility, named the Steinmetz Building, houses the Company’s UK R&D team. The facility brings together over 130 highly skilled staff from all over the world, who are focused on the discovery and development of novel GPCR-targeted medicines.

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Drug Discovery

Computational Medicinal Chemistry Approaches for GPCR Structure-Based Drug Discovery

By Juan Carlos Mobarec | Sep 10, 2019

Juan Carlos Mobarec, Senior Scientist Computational Chemistry at Sosei Heptares, recently attended the 20th SCI/RSC Medicinal Chemistry Symposium in Cambridge, UK on 8 September 2019 and presented on the computational medicinal chemistry approaches for GPCR Structure-Based Drug Discovery (SBDD).

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Development

Cholinergic muscarinic M1 and M4 receptors as therapeutic targets for cognitive, behavioural and psychological symptoms in psychiatric and neurological disorders

By Pradeep Nathan, Geor Bakker, Alastair Brown, Tim Tasker | Sep 9, 2019

Professor Pradeep Nathan, VP Clinical Development and Head of Experimental Medicine (Neuroscience) at Sosei Heptares, was recently invited to publish a Short Review in leading drug discovery journal, Drug Discovery Today, together with fellow Sosei Heptares colleagues including Geor Bakker, Alastair Brown and Tim Tasker and peers from the Institute of Neuroscience, Newcastle University in the UK. The review article titled "Cholinergic muscarinic M1 and M4 receptors as therapeutic targets for cognitive, behavioral and psychological symptoms in psychiatric and neurological disorders" provides an overview of the human cholinergic system and how it is affected in neuropsychiatric conditions, such as schizophrenia and several neurodegenerative disorders. In particular, the authors focus on the potential opportunities afforded by targeting cholinergic muscarinic receptors.

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Drug Discovery

Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design

By Alistair O'Brien | Aug 12, 2019

Alistair O'Brien, and several other current and former Sosei Heptares scientists, have published a paper titled "Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure-based drug design" in Bioorganic & Medicinal Chemistry Letters. A series of novel allosteric antagonists of the GLP-1R, exemplified by HTL26119, are described.

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