Medicinal Chemist and Molecular Toxicologist win PerkinElmer Prizes at FIGON Dutch Medicines Days
Jelle Reinen and Kristina Orrling, researchers from the VU University Amsterdam have won the PerkinElmerPrizes for the best Presentation and best Poster at the FIGON Dutch Medicines Days 2012.
Kristina Orrling, post-doc in the Division Medicinal Chemistryof VU University Amsterdam, received the 2012 PerkinElmer Poster Award in Medicinal Chemistry (500 Euros) for her work on “Jointly changing the future for human African sleeping sickness - PDE inhibitors as Trypanocidals” at the FIGON Dutch Medicine Days. Kristina works on the design and synthesis of new molecules that efficiently kill the parasite, which cause African sleeping sickness, by blocking the action of so-called phosphodiesterase (PDE) enzymes in the parasite. Kristina and her collaborators (united in a Dutch Top Institute Pharma consortium) have recently used a so-called fragment-based drug discovery (FBDD) approach to develop compounds that specifically target PDEs of parasites that cause this neglected tropical disease, but are selective against the human PDEs.
Jelle Reinen, post-doc in the Division of Molecular Toxicology of VU University Amsterdam received the 2012 PerkinElmer Presentation Award in Medicinal Chemistry (500 Euros) for his presentation on “Screening and employment of bacterial cytochrome P450 BM3 mutants for biocatalytic production of drug metabolites”, in the KNCV-Pharmacochemistry session at the FIGON Dutch Medicine Days. Jelle is using P450 BM3 mutants in different biocatalytic setups and managed to stereoselectively produce milligram quantities of hydroxysteroid products of the drug norethisterone. This can be seen as an important step in the approach of the Molecular Toxicology research group (under supervision of Dr. Jan Commandeur and Prof. Dr. Nico Vermeulen) to use bacterial P450 enzymes as general biocatalysts for lead diversification in the drug development process and the biosynthesis of drug(-like) metabolites.