Oss, the Netherlands – 9 December 2022
The novel chemical hit series discovered through the ultra-High Throughput Screening of the European Lead Factory (ELF) compound library and carried out at Pivot Park Screening Centre (PPSC), is now progressing to hit-to-lead phase in collaboration with the EU-OPENSCREEN partner site the Latvian Institute of Organic Synthesis (LIOS) within the ISIDORe project.
During the first year of the Covid-19 pandemic, the ELF decided to prioritise Covid-19-related proposals through a fast-track procedure. The target proposal submitted by the PPSC was the first proposal to be selected by the ELF. Its aim was to identify novel small-molecule inhibitors of viral entry into host cells as a prophylactic and therapeutic option for SARS-CoV-2 infection.
The programme resulted in high-quality hits comprised of various compound clusters and singletons, from which the most promising compounds were resynthesized and validated for their inhibitory activity. The bespoke novel hit series and associated high-quality biological data generated within the ELF hit discovery programme formed the foundation of a successful proposal to access the medicinal chemistry services available within EU-OPENSCREEN partner sites. This paved the way for the continuation of the programme towards hit-to-lead phase.
The plan is to progress this early drug discovery project to hit-to-lead phase including chemical modifications of the hits to increase the in-vitro potency and selectivity of the compounds. The hope is to increase the understanding of the Structure-Activity Relationship together with computer-assisted drug design including pharmacophore generation and docking.
Dr. Saman Honarnejad, Chief Scientific Officer at PPSC
“This is an excellent example of how public-private partnerships can bridge the innovation gap and valley of death, with the goal to tackle unmet medical needs. We have been privileged to benefit from the industry-standard expertise, know-how and infrastructure available at the European Lead Factory and look forward to exploiting the complimentary knowledge and capabilities within the EU-OPENSCREEN partner site LIOS.”
Dr. Jon de Vlieger, ELF Coordinator and Strategy Director at Lygature
“Working together on such an important topic shows the complementarity of the ELF and EU-OPENSCREEN. This work has resulted from excellent science by an ELF partner and the entire ELF consortium and I’m excited to see this now progress in collaboration with the EU-OPENSCREEN team in Latvia.”
Dr. Wolfgang Fecke, General Director at EU-OPENSCREEN
“We are proud that our experienced medicinal chemistry partner site at the LIOS in Riga can support this first hit-to-lead programme in the framework of the ISIDORe pandemic preparedness project.”
Prof. Aigars Jirgensons, Scientific Director at LIOS
“It is a great pleasure for LIOS as EU-OPENSCREEN MedChem partner site to support the ISIDORe pandemic preparedness project by applying our drug discovery expertise. We are looking forward to collaborating in this exciting project with PPSC to develop antiviral leads from high-quality hits.”