Rogier Smits wins Mercachem Farmacochemieprijs for best thesis Medicinal Chemistry

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Dr. Rogier Smits received the Mercachem Farmacochemieprijs for the best PhD thesis in Medicinal Chemistry in 2009-2010. Dr. Rogier Smits received the award (€2000) and gave a lecture about his work on the "Design and Synthesis of New Histamine H4 Receptor Ligands" during the Spring Meeting of the KNCV Medicinal Chemistry Division.

During his PhD project in the Division of Medicinal Chemistry of VU University Amsterdam (promotor: Prof. Dr. Rob Leurs, co-promotor: Dr. Iwan de Esch), Dr. Smits designed and synthesized molecules to modulate the histamine H4 receptor, a protein which plays an important role in inflammation is considered as a potential drug target for the treatment of asthma, allergic rhinitis, and pruritis. Starting from different small fragment-like molecules (scaffolds), Smits used computational pharmacophore models and structure-activity relationships to optimize the structures of the ligands and increase their binding affinity and effects at the histamine H4 receptor. The optimized ligands had clear anti-inflammatory activity in vivo animal studies and one molecule was even developed into a radioligand for monitoring inflammatory processes with positron emission tomography (PET).

Interestingly, many of the potent histamine H4 receptor ligand Smits optimized during his PhD work formed the basis of the spin-out company Griffin Discoveries (www.griffindiscoveries.com), which Rogier Smits started in 2009 together with former PhD supervisers Iwan de Esch and Rob Leurs. Griffin Discoveries develops innovative G protein-coupled receptor (GPCR) targeting drugs for therapeutic areas with unmet clinical need and works in close collaboration with the academic VU Medicinal Chemistry group.

14/04/2011