Tackling unmet medical needs: Exciting new hits for a novel drug target involved in depression and pain unveiled in the EU Lead Factory

An exciting innovative target involved in these debilitating conditions was discovered by Dr Patrick McHugh, University of Huddersfield. “We don’t have the facilities to carry out large scale screening campaigns to fully assess the possibilities of our findings. That’s why we’ve used the connections in ELF and formed a partnership with Taros Chemicals and PPSC to counter this problem and enable further investigation of this target and its potential to modulate disease,” said Dr McHugh, Director of the University of Huddersfield’s CeBioR.

The collaboration between the three organizations perfectly combines their respective skills: drug target engineering and development of advanced disease models at the CeBioR, medicinal chemistry and synthesis expertise available at Taros Chemicals and PPSC’s excellence in high throughput screening (HTS).

“This project is an example where a medium sized contract research organization such as Taros takes the leadership in bridging the gap between early discovery results obtained in academia and industrial requirements for the development of new drugs. In the following steps of the project, Taros Chemicals will be making initial hit analog compounds at its Dortmund based labs and drive their transformation into the potential drug candidates. This will be supported by our medicinal chemistry and computer-aided drug discovery expertise,” says Dr Anna Karawajczyk, Principal Computational Chemist and Project Leader at Taros Chemicals.

“We applied our assay development and HTS expertise on the target discovered by Dr McHugh’s research team to develop an assay that could be submitted to the ELF. Subsequently, the entire Joint European Compound Library of approximately 400,000 compounds was screened, followed by triaging using several orthogonal and deselection assays. This resulted in 50 confirmed hits. These promising compounds will now be further developed by the consortium,” said Dr Helma Rutjes, COO at PPSC.

This collaborative project forms an excellent starting point for further study and validation of the target’s role in depression and the development of a new therapy against major depressive disorder. Further analysis and testing of the different compounds is predicted to lead to an alternative medicine to treat depression as well as chronic pain, extending the range of treatments available on the market. 

About Taros Chemicals GmbH & Co. KG

Taros, a privately owned CRO / CMO has been serving the needs of pharmaceutical, chemical and biotech companies since 1999. More than 10.000 synthesis, research and process chemistry projects have successfully been delivered to the global customer base. Taros’ scientists combine more than 140 years industrial organic chemistry experience and over 60 years of active drug discovery experience. They have expertise in major therapeutic areas and in all small molecule target classes. Taros Chemical covers the full range of organometallic chemistry research and production from lab scale size to several hundred Kgs supply per year. This includes screening/focused library design and production, computer aided drug design, medicinal chemistry services engaged in hit finding, hit to lead and lead optimization works as well as material science and specialty chemistry driven R&D services including research, design, route scouting, process development and non-GMP production & delivery of up to 1.000kg / year of such performance chemicals. Taros Chemicals have developed TarosGate®, a unique software suite putting cost, time and chemistry information at a Project Leader’s finger tips - 24h/7 from anywhere in the world. TarosGate® is a major cornerstone of the 196 Mio. Euro European Lead Factory (ELF) drug discovery platform. Taros Chemicals is leading ELF’s chemistry activities since 2013. http://www.tarosdiscovery.com 

About Pivot Park Screening Centre

With our partners, we accelerate the discovery of new medicines for a healthier society. Pivot Park Screening Centre (PPSC) provides drug discovery services in the field of assay development, lab automation and (ultra) High Throughput Screening ((u)HTS) to find new leads for drug development. PPSC specializes in the screening of large libraries for pharma companies. In addition, PPSC is the central screening site in the European Lead Factory, collaborating with a large number of academia and SMEs.  The screening facility includes state-of-the-art robotic systems and an extensive collection of 300,000 high quality drug-like compounds. The open access facilities provide instrumentation for hit-to-lead testing and technology development. Pivot Park Screening Centre is based at Pivot Park in Oss, the Netherlands. For more information please visit www.ppscreeningcentre.com.

About the Centre for Biomarker Research, University of Huddersfield

The CeBioR is at the forefront of health or medical-related research within the University of Huddersfield and beyond. The centre brings together academics and researchers in areas of biomarker discovery and drug development for CNS diseases. CeBioR was founded in 2016 by Dr McHugh and since its inception the CeBioR has been instrumental in developing high quality research in a broad range of areas relating to the improvement of human lives through the understanding of biological processes relating to disease aetiology and identifying new ways to improve diagnosis and treatment. The CeBioR network stretches through and beyond the University through prestigious national and international researchers including industry, consortia and highly QS ranked universities, as well as the NHS, where several studies, co-ordinated by Dr McHugh, have been adopted to the National Institute of Health Clinical Research Network (NIHR CRN). For more information, please visit https://research.hud.ac.uk/institutes-centres/cebior/.

About the European Lead Factory

IMI’s European Lead Factory is a unique, collaborative platform for early drug discovery. It offers unrivalled opportunities to any European academic or SME working in any therapeutic area for the discovery of new diagnostic or drug lead molecules; compounds that can result in the development of novel treatment options for patients. To this end, the European Lead Factory provides a high-quality compound library, industry-standard screening facilities and drug discovery expertise. The European Lead Factory was launched in 2013 and is managed by an international consortium of 30 partners. The research leading to these results has received support from the Innovative Medicines Initiative Joint Undertaking (IMI-JU) under grant agreement n°115489, resources of which are composed of financial contribution from the European Union’s Seventh Framework Programme (FP7/2007-2013) and EFPIA companies’ in kind contribution. For more information, please visit www.europeanleadfactory.eu.

Scientific Contact:

Dr. Anna Karawajczyk
Taros Chemicals GmbH & Co. KG
Phone: +49 231 9742 7211

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