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Keapstone Therapeutics and Sygnature Discovery collaborate to discover new therapies for Parkinson’s and Motor Neuron Disease

Keapstone Therapeutics, a new biotech company formed by the University of Sheffield and Parkinson’s UK to develop new drugs for Parkinson’s and other neurodegenerative diseases, and Sygnature Discovery, the UK’s largest independent provider of integrated drug discovery resource and expertise, today announced they will collaborate to discover new treatments for Parkinson’s and Motor Neuron Disease (MND).

 

Keapstone Therapeutics will build on pioneering research undertaken at the Sheffield Institute for Translational Neuroscience (SITraN) and an international collaboration with the European Lead Factory, during which Dr Richard Mead of SITraN discovered novel small molecules which prevent the interaction between two proteins known as Kelch-like ECH-associated protein-1 (KEAP1) and Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) to increase the survival of neurons in both Parkinson’s and MND.  In close collaboration with Sygnature Discovery, Keapstone Therapeutics will now further optimise these molecules to afford drug candidates with the potential to slow or even prevent the progression of these neurodegenerative diseases.

 

Dr Richard Mead of Keapstone Therapeutics said: “We are very excited about this new partnership with Parkinson’s UK.  It is a great opportunity for us to pursue a novel drug discovery programme for both Parkinson’s and MND.  We will now progress these molecules through the next stage of drug development with Sygnature Discovery and Peak Proteins.”

 

Dr Arthur Roach, Director of Research and Development at Parkinson’s UK, said: “Keapstone is a pioneering project and a world-first in terms of its formation.  By seeking early collaboration with Sheffield in the creation of a spin-out biotech company, we will be able to investigate and develop potential Parkinson’s treatments with an intensity that is unprecedented for a charity.  This exciting new venture would not have been possible without our supporters and partners. We’re looking forward to sharing the developments of this new project with them.”

 

Dr Simon Hirst, Founder and CEO of Sygnature Discovery commented, “We are delighted to be collaborating with Keapstone Therapeutics and Parkinson’s UK to discover new drugs to treat Parkinson’s and other neurodegenerative diseases.  Keapstone’s novel therapeutic approach offers huge potential of developing treatments for these debilitating and ultimately fatal diseases.  Sygnature has considerable experience in undertaking drug discovery research directed towards neurodegenerative diseases and has a successful track record of success in delivering clinical candidates.”



Sygnature Discovery, Mironid®, and Peak Proteins to collaborate to discover new therapies for life-threatening and currently incurable kidney disease, ADPKD

Sygnature Discovery, Mironid® Limited, a leader in cell signalling-directed drug discovery and Peak Proteins, have announced they will work closely together to discover new therapies against diseases driven by elevated cyclic AMP (cAMP), such as Autosomal Dominant Polycystic Kidney Disease (ADPKD).

ADPKD is a devastating, life-threatening and currently incurable genetic disorder in which kidney cysts progressively form throughout life. Cyst formation is driven by excessive generation of the cell signalling molecule, cAMP and causes a wide range of health problems including abdominal pain, high blood pressure and urinary tract infections, eventually leading to kidney failure. ADPKD affects around 12.5 million people worldwide, with around 50% requiring treatment for kidney failure by the age of 60.

Professor Miles Houslay, CSO of Mironid®, said, “The cAMP signalling pathway and, in particular, the PDE4 enzyme class, is an under-exploited target class with still so much to offer in the way of novel therapies. My colleagues and I are delighted with this strong support and recognition from Innovate UK. This funding will allow Mironid to leverage its expertise in PDE4 mechanistic biochemistry, together with the advanced capabilities of the UK’s first class life science contract research sector to deliver effective medicines more quickly”.

Dr Simon Hirst, Founder and CEO of Sygnature Discovery commented, “We are delighted to be collaborating with Mironid® and Peak Proteins to discover new high quality chemical starting points for Mironid®’s novel LoAc® molecules. This novel therapeutic approach offers the possibility of developing treatments for ADPKD and other diseases driven by elevated cAMP.”

The £606,000 programme, 70% funded by the UK’s innovation agency, Innovate UK, will expand Mironid®’s repertoire of proprietary LoAc® molecules by discovering new high quality chemical starting points for this novel therapeutic approach. This programme exploits the pioneering work of Professor Miles Houslay, one of the founders of Mironid®, to develop small molecule positive modulators of Phosphodiesterase 4 (PDE4) enzymes, which break down cAMP, a critical intra-cellular signalling molecule. A high-quality compound library from BioAscent, plus computational modelling and protein X-ray crystallography will be used to generate the next wave of PDE4 regulating molecules unique to Mironid®. These molecules will form the basis of new therapies against diseases driven by elevated cAMP.



Pelago Bioscience and Sygnature Discovery collaborate to Provide CETSA® based Target Engagement Assays

Sygnature Discovery today announced that it will collaborate with Pelago Bioscience, a Swedish biotech company to provide target engagement assays with Pelago’s patented Cellular Thermal Shift Assay (CETSA®) method.

While target engagement has long been recognised as pivotal to targeted drug efficacy. Pelago’s CETSA method adds a new dimension to this valuable assay, as it enables measurements to be made within cellular systems. For the first time researchers can now measure directly how a compound interacts with its target within the cell and even within patient tissue. Furthermore the CETSA MS method enables the systemic effects of a drug within the cell to be explored, by measuring its impact on up to 7000 key proteins. Such quantification of the physiologically relevant form of the target in live cells and tissue samples, will accelerate and improve the discovery of high quality drugs.

The collaboration between Sygnature and Pelago will enable more pharmaceutical R&D and biotech companies to incorporate CETSA within their drug discovery process, and will allow the development new and better drugs more quickly and cost-effectively. Specifically, the collaboration will effectively facilitate the integration of CETSA assays for hit confirmation, lead profiling and biomarker discovery in Sygnature projects. Likewise, Pelago customers will have the opportunity to access the full value chain service portfolio at Sygnature.

“We are excited about the opportunity of adding our CETSA target engagement quantifications to projects in the Sygnature portfolio” said Dr Michael Dabrowski, CEO of Pelago Bioscience. “This collaboration, with a UK based service provider will enable more CETSA data to benefit existing and new customers.”

“The CETSA platform is a valuable addition and highly complementary to our own assay platforms and capabilities,” said Dr Paul Clewlow, Senior Vice President, Business Development at Sygnature Discovery, “We believe that the CETSA platform can be rapidly integrated and deliver detailed target engagement information to our clients to inform their discovery programs.”

For more information
Pelago Bioscience AB, Dr Michael Dabrowski, CEO, Tel. +46 (0)730 715 334, michael@pelagobio.com
Sygnature Discovery Limited, Dr Paul Clewlow, Senior Vice President, Business Development, Tel: +44 (0)115 9415401, busdev@sygnaturediscovery.com



Sygnature further enhances capabilities and services within the translational sciences.

Sygnature Discovery has released a biology publication focusing on our collaboration with Corcept Therapeutics. This work highlights our biomarker validation work and reports the outcome of phase I QBR116598 study that was also recently presented at Sygnature by Quotient clinical. The publication, sets the scene to support further phase II studies where FKBP5 might be utilized as a predictive biomarker to assess the treatment response of patients with Cushing’s syndrome.

To summarize, the publication highlights the discovery and validation of FKBP5 as a biomarker for GR antagonism and showcases the quantitative PCR assay, used to detect the FKBP5 mRNA transcript levels, from total RNA extracted from whole blood. Follow up analysis of FKBP5 levels in phase II trial, investigating the effect of CORT125134 in patients with Cushing’s disease, will be carried out at US based Neogenomics. They will be aiming to use their cGCP platform to platform to determine FKBP5 mRNA transcripts in these samples.

Dr Hazel Hunt, Vice President, Research at Corcept Therapeutics stated;

‘The measurement of FKBP5 provides a simple and convenient method to assess the activity of cortisol, the endogenous agonist of the glucocorticoid receptor. Disregulated cortisol production is associated with many diseases, including the archetypal disease of cortisol excess, Cushing’s syndrome’.

The publication has been released in the peer reviewed Journal of Clinical Endrocrinology and Metabolism and an online link to the Early Release version of the manuscript can be accessed via this link at the journal website



Sygnature Discovery expands DMPK team with appointment of Dr. Edward Browne

Sygnature announces the expansion of its DMPK team with the appointment of Dr Ed Browne as Associate Director of DMPK.

Ed is an experienced drug discovery scientist who brings a thorough understanding of developing and prosecuting a lead optimisation strategy, having worked at GSK, Singapore for the last ten years as head of the Drug Metabolism and Pharmacokinetics team (DMPK).

Ed commented, “I have been really impressed by the integrated set-up at Sygnature Discovery. I’m used to this approach, having worked for the past 10 years in a small group of 60 scientists across DMPK, Chemistry and Biology at GSK in Singapore. It is a very similar environment at Sygnature Discovery, but with larger teams of scientists here.”

He continued, “The executive team at Sygnature Discovery are very enthusiastic about their business model, which involves the cross-sharing of information, creating dynamism across all capabilities, speeding up problem solving and efficiency.”

He concludes, “Sygnature Discovery is not a standard CRO, it operates as a consultancy, working on real drug discovery rather than routine assays. Clients range from spin-outs to large pharma. I particularly like the positive impact Sygnature has on smaller companies by identifying key data and helping them make cost-effective decisions and helping them to achieve their goals.”

Sygnature’s Director of DMPK, Dr Timothy Schulz-Utermoehl, added, “I am delighted to welcome Ed to the team here at Sygnature. Ed brings significant DMPK and drug discovery experience to our rapidly expanding department as we continue to build our CNS expertise and large molecule bio analysis.”



Sygnature Discovery and Viramatix announce anti-viral drug discovery strategic alliance

Nottingham, UK and Kuala Lumpur, Malaysia; 5th October 2016 – Sygnature Discovery Limited, the UK’s largest independent provider of integrated drug discovery resources and expertise, and Viramatix Sdn. Bhd., a biopharmaceutical company involved in the discovery of peptide based anti-viral therapeutics, today announced their ongoing collaboration on innovative anti-influenza therapeutics.

Influenza virus infection remains a serious threat to human health. Every year, nearly 5 million people are seriously affected by this illness and some 250,000 – 500,000 die globally. Currently, there are very few approved drugs available for the treatment and these treatment options possess many drawbacks such as short treatment window, resistant virus development and lack of broad-spectrum activity among other issues. This presents a significant unmet medical need in the development of new therapeutics with novel mechanisms of action. Viramatix’s pipeline candidates have shown excellent activity against all types of human influenza viruses and even against animal and avian influenza viruses.

“Taking our research offshore was no small decision. After evaluating the market of CRO providers across Europe, Sygnature Discovery really impressed us with a comprehensive range of services and an accomplished team to match under one roof. Their professionalism and communication with our scientists has made all the difference in progressing our research forward. With Sygnature Discovery we had a seamless transition to managing our research remotely,” explained Robert Hercus, Managing Director of Viramatix.

Sygnature Discovery has already provided services on DMPK characterization and optimization of Viramatix’s lead candidates. The ongoing collaboration will see Sygnature Discovery continue to undertake various studies to understand and optimize the drug-like characteristics of the lead candidates as Viramatix pursues clinical development of their therapeutic.

“We are impressed with Viramatix’s capabilities and its research, which has produced very promising results in all characteristics of the company’s Flu Peptide Therapeutic (FPT) which have been examined to date, “stated Dr Timothy Schulz-Utermoehl, Director of DMPK at Sygnature Discovery. He added, “We look forward to being involved in Viramatix’s continuation studies.”

“To achieve such rapid success in the project has required excellent science and smooth communication between the two groups. I am delighted that Viramatix has chosen to continue and expand our collaboration” said Simon Hirst, Sygnature Discovery’s CEO. “I feel confident that the combination of Viramatix’s novel approach and Sygnature Discovery drug discovery expertise opens up some exciting possibilities for new therapeutics.”



The Corona sculpture starts to take shape on the new ‘Discovery’ building

Sygnature Discovery today saw the start of the Brise Soleil installation on the front of the new £30m ‘Discovery’ building. which will reduce the risk of the building overheating. The sculpture known as Corona forms a curtain of metal tubes 17 metres high across the front of the building which are linked to NASA satellites by computer. These will determine how the building and surrounding areas are lit up , providing a stunning entrance to the east of the city and Sygnature’s new laboratory and office facility.



Sygnature are exhibiting at ELRIG’s Drug Discovery 2016 event at the ACC, Liverpool. Stand G1

Drug Discovery 2016 will bring together 1000 delegates and 50 world-class speakers from academia and industry, each representing critical areas in drug discovery.

Scientific Sessions:
Innovations in Chemistry
Oncology & Immunology
Innovations in Predictive & Translational Models
Assay Development, Screening & Emerging Technologies
Coming Closer to the Patient – Cells & Genes in Therapy & Diagnostics
Target Identification & Validation

Plenary Keynote Speakers:
Professor Chas Bountra
Chief Scientist (SGC), Professor of Translational Medicine, University of Oxford

Professor Munir Pirmohamed
David Weatherall Chair in Medicine, Royal Liverpool University Hospital

Professor Dame Carol Robinson OBE
Professor of Chemistry, University of Oxford

elrig-liverpool



Sygnature Discovery’s drug discovery capabilities enhanced by acquisition of BMG LABTECH PHERAstar® FSX

July 20th 2016 – Nottingham, UK – Sygnature Discovery Limited, the UK’s largest independent provider of integrated drug discovery resource and expertise, today announced the addition of the BMG LABTECH PHERAstar® FSX into its portfolio of advanced in vitro screening capabilities.

In order to maximise assay performance during drug discovery projects, Sygnature is striving to add the latest screening technologies that will facilitate an increase in assay through-put and minimise sample usage, whilst maintaining assay quality and controlling costs.  The PHERAstar® FSX is the most sensitive microplate plate reader currently on the market and is able to perform all leading non-isotopic detection technologies and has unmatched sensitivity in Fluorescence Intensity and Fluorescence Polarization modes.  In addition, the reader offers an ultra-high dynamic range in High Performance Luminescence enabling greater flexibility and measurement precision.

The instrument is equipped with Simultaneous Dual Emission in all read modes, top and bottom reading with automatic switching, an advanced cell monolayer scanning function and temperature control (25 – 45°C).  Also with BMG LABTECH’s Stackers, 50 plates can be read at one time making the instrument fully enabled for both medium- and high-throughput screening.

 

Read Modes routinely used at Sygnature Discovery:

  • High Performance Luminescence
  • Nano Bioluminescence Resonance Energy Transfer (nBRET)
  • Time Resolved Fluorescence including TR-FRET/HTRF®
  • Fluorescence Polarization
  • Fluorescence Intensity
  • AlphaScreenTM
  • AlphaLISATM
  • Absorbance (UV/Vis Spectral Scanning) 220-1000nm

Time Resolved Fluorescence Resonance Energy Transfer (TR- FRET) is based on the transfer of energy between two fluorophores, a donor and an acceptor.  Combining FRET technology with time-resolved measurement of fluorescence eliminates short-lived background interfering fluorescence.
Graph

Example screening data for 2 compounds run on the BMG LABTECH PHERAstar® FSX at Sygnature





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