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.
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).READ MORE...
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.READ MORE...
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.READ MORE...
Use of a modified hidden pathway maze test in patients with Alzheimer’s Disease dementia
By Pradeep Nathan | Jul 22, 2019
Professor Pradeep Nathan, VP Clinical Development and Head of Experimental Medicine (Neuroscience) at Sosei Heptares, recently attended the Alzheimer’s Association International Conference (AAIC) 2019 on 16 July 2019 and presented two experimental medicine posters titled “Use of a modified hidden pathway maze test in patients with Alzheimer’s Disease dementia” and “Basal forebrain volumes predict circuit specific functional sensitivity to muscarinic M1 receptor antagonist biperiden on cognition.”READ MORE...
Discovery of A2AR Antagonist AZD4635 (HTL1071) using Structure-based Drug Discovery (SBDD)
By Miles Congreve | Jun 21, 2019
Dr. Miles Congreve, Head of Drug Discovery at Sosei Heptares, recently attended the New Approaches in Medicinal Chemistry symposium in Cambridge, UK on 20 June 2019 and presented on the application of structure-based drug discovery (SBDD) to the discovery of A2AR Antagonist AZD4635.READ MORE...
Sosei Heptares actively participates in the next European Training Network ONCORNET 2.0
By Chris de Graaf | Jun 5, 2019
The EU has awarded 4 million Euros for ITN research programme ONCORNET2.0, which aims to understand and target two oncogenic G protein-coupled receptors (GPCRs) highly expressed in multiple tumors. The consortium will develop new strategies for chemokine receptor modulation and investigate their effects on oncogenic responses, to yield key new knowledge and potential leads for drug development.READ MORE...
QVM149, a potential new inhaled combination treatment, is superior to high-dose salmeterol/fluticasone propionate in improving lung function in patients with asthma (ATS 2019)
By Novartis | May 22, 2019
Novartis presented new clinical data from its Phase II study with QVM149, a potential new inhaled combination treatment for asthma, assessing the bronchodilator effect and safety of two doses of QVM149 compared to a fixed dose combination of salmeterol/fluticasone in adult patients with asthma.READ MORE...
QVM149, a potential new inhaled combination treatment, demonstrates improvements in lung function in patients with asthma irrespective of time of dosing
By Novartis | May 22, 2019
Novartis presented new clinical data from its Phase II study with QVM149, a potential new inhaled combination treatment for asthma, assessing the bronchodilator effects of once daily QVM149 following morning or evening dosing for 14 Days compared to placebo in adult patients with asthma.READ MORE...
Molecular basis for high affinity agonist binding in GPCRs
By Andrew Doré | May 9, 2019
Dr Andrew Doré, Director - Head of Crystallography at Sosei Heptares, recently published a paper in Science, titled "Molecular basis for high affinity agonist binding in GPCRs", alongside fellow co-authors from the MRC Laboratory of Molecular Biology – Tony Warne, Patricia Edwards, Andrew Leslie and Chris Tate (Co-Founder, Heptares Therapeutics).READ MORE...
Aminergic GPCR–Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data
By Chris De Graaf | May 7, 2019
Dr. Chris De Graaf, Head of Computational Chemistry at Sosei Heptares, recently published a paper in the renowned Journal of Medicinal Chemistry, titled “Aminergic GPCR–Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data” alongside fellow co-authors from VU University Amsterdam, Polish Academy of Sciences and University of Copenhagen.READ MORE...
Application of structure-based drug discovery to G Protein-Coupled Receptors
By Rob Cooke | May 2, 2019
We recently attended the 30th Symposium on Medical Chemistry in Eastern England on 2 May 2019 in Hatfield, United Kingdom and presented on the application of structure-based drug discovery to GPCRs.READ MORE...
AZD4635, a novel oral adenosine A2A receptor antagonist, shows clinical activity as a monotherapy or in combination with Imfinzi® (durvalumab) in patients with advanced solid tumors (AACR 2019)
By AstraZeneca | Apr 14, 2019
AstraZeneca presented new clinical data from its Phase 1a study with AZD4635, a next-generation immuno-oncology candidate, as a single agent and in combination with the PD-L1 antibody durvalumab, in patients with advanced solid tumors, at the 2019 American Association for Cancer Research (AACR) Annual Meeting in Atlanta, USA (29 March to 3 April 2019).READ MORE...
AZD4635, a novel adenosine A2A receptor antagonist, restores anti-tumor activity by preventing adenosine-mediated suppression of immune cells (AACR 2019)
By AstraZeneca | Apr 14, 2019
AstraZeneca presented new data from preclinical studies with AZD4635, a next-generation immuno-oncology candidate, demonstrating its ability to restore the anti-tumor activity of dendritic cells (DCs) by preventing their adenosine-mediated immunosuppression. The new data were presented in a poster at the 2019 American Association for Cancer Research (AACR) Annual Meeting in Atlanta, USA (29 March to 3 April 2019).READ MORE...
Fibromyalgia: an urgent need for a harmonised, global and patient-centric regulatory guidance for developing medications for the treatment of pain and associated symptoms
By Dr Nico Merante | Apr 11, 2019
Dr Nico Merante, VP Development of Sosei Heptares recently published an article in Pain Medicine Journal, “Fibromyalgia: an urgent need for a harmonised, global and patient-centric regulatory guidance for developing medications for the treatment of pain and associated symptoms".READ MORE...
Enabling FBDD for GPCRs with Protein Engineering and Biophysics
By Rob Cooke | Apr 5, 2019
We recently attended the 7th RSC-BMCS Fragment-based Drug Discovery meeting on March 24–26th in Cambridge, United Kingdom and presented on fragment-based drug discovery (FBDD) for GPCRs with protein engineering and biophysics.READ MORE...
Basal forebrain volumes predict circuit specific functional sensitivity to the muscarinic M1 receptor antagonist biperiden on cognition
By Geor Bakker, PhD, Pradeep Nathan PhD, Alex Godwood MSc. | Apr 3, 2019
We recently attended the Alzheimer’s & Parkinson’s Diseases (ADPD) Conference on 29th March in Lisbon, Portugal where we presented data in the session “Huntington’s and Other Neurodegenerative Diseases: Imaging, Biomarkers, Diagnostics”. In a collaboration led by Sosei Heptares, with the Amsterdam University Medical Centres and Maastricht University, we presented our novel findings in a poster showing that the basal forebrain nuclei volumes can sensitively predict circuitry specific effects of M1 receptor antagonist biperiden on cognition. This work forms an important part of the goals of the Neuroscience Experimental Medicine group to develop novel biomarkers that could define optimal treatment response as well as support patient stratification into clinical trials for drugs in development at Sosei HeptaresREAD MORE...
Trends and Innovation in Drug Discovery at Sosei Heptares
By Matt Barnes, Lisa Stott, David Tippet | Jan 9, 2019
We recently attended the British Pharmacological Society’s Pharmacology 2018 meeting on December 18th – 20th in London where we made two presentations including: 1 – Oral presentation on our approach to studying GPCRs in immuno-oncology and 2 – Poster presentation detailing a technology evaluation examining binding assay techniques at the histamine H4 receptor.READ MORE...
Single and multiple dose safety, tolerability and pharmacokinetics of the selective M1 receptor partial agonist HTL0018318 in healthy volunteers
By Pradeep Nathan | Dec 18, 2018
We attended the American College of Neuropsychopharmacology meeting on December 9-13, 2018 in Florida, U.S., and presented on the safety, tolerability and pharmacokinetics of the selective M1 receptor partial agonist HTL0018318 in healthy volunteers.READ MORE...
New small molecule HTL0014242 shows early promise for slowing neurodegeneration
By Kirstie Bennett | Dec 9, 2018
Researchers from the Sheffield Institute for Translational Neuroscience (SITraN) at the University of Sheffield, UK working with scientists at Sosei Heptares have presented findings from preclinical studies investigating a new small molecule HTL0014242 in preclinical models of the neurodegenerative condition motor neurone disease (MND).READ MORE...
Our Approach to Drug Discovery
By Sosei Heptares | Nov 28, 2018
An introduction to our unique and rationale approach to drug discovery which we hope will deliver new medicines for patientsREAD MORE...
Introduction to Sosei Heptares
By Sosei Heptares | Nov 27, 2018
Sosei Heptares is an international biopharmaceutical company focused on the design and development of new medicines originating from its proprietary GPCR-targeted StaR® technology and structure-based drug design platform capabilities.READ MORE...
Structure-Based Drug Discovery of G protein-coupled receptors (GPCRs)
By Kirstie Bennett | Aug 29, 2018
We attended the 15th Meeting of the Asian-Pacific Society for Neurochemistry, held in August 27-29, 2018 in Macau, China. The presentation was focussed around our candidate compound HTL0014242 – a negative allosteric modulator of the metabotropic glutamate 5 receptor (mGlu5). We presented the development of HTL0014242 from hit generation, using a fragment screening approach, to some preliminary efficacy data in the SOD1G93A mouse model of amyotrophic lateral sclerosis (also known as motor neurone disease); data generated through a Sosei Heptares-funded PhD student in Dr Richard Mead’s lab at the Sheffield Institute for Translational Neuroscience.READ MORE...
Manipulation of allosteric mechanisms in GPCR drug design
By Stacey Southall | Aug 3, 2018
We attended "Structure and Mechanism of Membrane Proteins", a Biochemical Society meeting on August 2-3, 2018 at Maple House in Birmingham UK, and presented recent case studies of allosteric modulators of GPCRs where Sosei Heptares StaR technology has enabled structural and biophysical characterisation of allosteric binding pockets and the mode of modulation on GPCRs. We explain how understanding of this diverse range of sites and mechanisms opens new avenues in SBDD towards generation of GPCR targeted drugs with improved therapeutic profile.READ MORE...
Beyond the Happy Water
By Ben Tehan | Apr 11, 2018
We presented our research on water molecules and recent advances in the quantification of their contributions at "Structure-Activity Relationships".READ MORE...