At the start of the project, Domainex conducted a LeadBuilder virtual screen that generated the initial hit matter. Following this success, it worked with the Queen’s team to provide integrated medicinal chemistry services to develop the initial hits. To further advance this cutting-edge research into the role of FLIP inhibitors in cancer, Domainex also supported Queen’s in securing a Wellcome Trust Seeding Drug Discovery award.
FLIP is a major apoptosis-regulatory protein that is frequently overexpressed in haematological and solid tumours (including colorectal, lung and pancreatic cancer). FLIP has been implicated in the regulation of cell death, is a key oncology target and has been shown to be upregulated with tumour progression in a variety of cancers.
Dr Ray Boffey, Executive Director of Medicines Research at Domainex, commented: “The Domainex drug discovery team is proud to have delivered a series of FLIP inhibitors for the Queen’s team, and we hope that these lead to first-in-class drugs that will improve the lives of patients with cancer.”
Tom Mander, CEO of Domainex, added: “We are very pleased that our successful collaboration with Queen’s and the Wellcome Trust has generated a set of FLIP inhibitors to warrant further investigation by Ipsen. It is further testament of the power of our integrated drug discovery engine to deliver potential breakthrough new medicines to treat debilitating diseases and demonstrates the value that our team brings to our partners.”
Professor Daniel Longley, Deputy Director of the Patrick G. Johnston Centre for Cancer Research at Queen’s, added: “It has been an absolute pleasure working with Dr Boffey and the Domainex team on this project. Without their first class medicinal chemistry expertise and the use of their Leadbuilder virtual screening platform at the outset of the programme, we would not have been able to secure the support of The Wellcome Trust and advance the programme to the stage it has now reached.”
Professor Tim Harrison, McClay Professor of Medicinal Chemistry at Queen’s and Co-PI, went on to comment: “We are excited about the potential of the novel, first-in-class small molecule FLIP inhibitors that we have been able to develop and thank Domainex for its support of the medicinal chemistry programme which has allowed us to progress the programme to this stage”.
Dr Lynsey Bilsland, Wellcome Trust Innovation Lead, added: “The FLIP inhibitor program is an excellent example of using novel ideas in drug discovery to try and improve cancer outcomes. Domainex was instrumental in supporting this. We have high confidence in the teams at Ipsen and Queen’s in further developing this technology into the clinic.”