In DDT 2013, 1158, we described a practical drug discovery project for third-year chemistry undergraduates at the University of Nottingham. No previous knowledge of medicinal chemistry is assumed. Initial lecture workshops cover the basic principles; then students, in teams, seek to improve the profile of a weakly potent, insoluble phosphatidylinositide 3-kinase (pi3k?) inhibitor through compound array design, molecular modelling, screening data analysis and the synthesis of target compounds in the laboratory. The project benefits from significant industrial support from GlaxoSmithKline (GSK) including lectures, student mentoring experiences and consumables. GSK also screen compounds made by the students and return data for their use. The aim is to make the learning experience as close as possible to real life industrial situations. This project has now run for over five years and has proven so popular that related projects are now also run in The School of Pharmacy at the University and at Queen Mary University of London.
In a forthcoming article in DDT, we describe a 4th year undergraduate module built on final year research projects. It is a radically different industry-academia collaboration between the School of Chemistry, University of Nottingham, and GSK, with similar aims to the 3rd year module. In this case the project concerns the discovery of potent and selective avb6 integrin antagonists to treat idiopathic pulmonary fibrosis; the synthetic chemistry is performed by a group of ten final-year undergraduates and the biological/physicochemical screening data are generated by GSK. The project planning, organisation and operation are discussed, together with some of the challenges and rewards of working with undergraduates – some of their feedback is particularly illuminating.
To date, well over 100 students have experienced these modules and they have produced compound sets with samples and accompanying data on over 200 compounds. Beyond these modules, the data and samples have seeded a number of new collaborative projects with other academics and clinicians at Nottingham.
The more world-weary reader may interpret these modules as another way of carrying out research at reduced cost but this is not the case. Any intellectual property arising is owned by the University and some of the research so far has resulted in a number of peer reviewed publications in quality journals.
The benefits to the industry are clear. For all involved, the broadening of perspective and the opportunities for personal development, combined with the unexpected scientific insights that somehow keep emerging, provide substantial long term benefits. Why not try a variation of these modules at your institution? It is an investment in your staff and the future scientists who will drive our industry forward, promoting collaboration and economic benefit.
Whilst this editorial is written by Simon Macdonald, both Jonathan Fray (former GSK Teaching Fellow at the University of Nottingham) and Tom McInally (Business Science Fellow in Medicinal Chemistry at the University of Nottingham) have been integral to the design and implementation of these undergraduate modules.
Biography:
Simon Macdonald was born, bred and educated in Manchester (UK) and has over 20 years’ experience as a medicinal chemist in the pharmaceutical industry. He has spent his entire career at GlaxoSmithKline in its various incarnations. He is currently a director of medicinal chemistry in the Fibrosis Discovery Performance Unit in the Respiratory Therapeutic Area at the Medicines Research Centre at GSK in Stevenage, UK. He has worked on numerous respiratory programmes including elastase inhibitors, glucocorticoid agonists, neuraminidase inhibitors and most recently with avb6 antagonists for idiopathic pulmonary fibrosis. On a recent GSK volunteer partnership and in a departure from respiratory drug discovery, he spent 6 months working with Medicines for Malaria Venture in Geneva assisting them in their goal to discover new medicines for malaria.
Undaunted by synthetic complexity, he has delivered candidates from many of these areas into development. Unusually for a medicinal chemist based in industry, he has published over 100 papers and patents across a broad range of interests indicating a willingness to embrace new approaches and methodologies. Collaborating across scientific boundaries is a common theme.
Most recently, as part of ongoing collaborations, he was appointed a visiting professor at the University of Nottingham where he has helped design, coordinate and teach medicinal chemistry modules to undergraduate students which have proved great fun and unusually fruitful.
A principle motivator is to help discover a useful medicine and amidst all the programme work and e-mails he still occasionally carries out a reaction in the lab!