VU Medicinal Chemist Niels Hauwert wins EHRS Young Investigator award
Niels Hauwert, PhD student in the Medicinal Chemistry research group, has received the Young Investigator Award from the European Histamine Research Society (EHRS) for his work and presentation on “A bi-directional photoantagonist toolbox for histamine H3 receptor photopharmacology” at the Joint meeting of the European and Japanese Histamine Research Societies, 11-13 May 2017 in Amsterdam.
Hauwert focuses on the modulation of histamine receptors using ligands that isomerize under the influence of light (see figure below). These photoswitchable ligands have a large difference in binding affinity for the histamine H3 receptor when they are isomerized using light as an external bio-orthogonal trigger. The photoswitching process is a fast and reversible process that can be repeated numerous times. Using two-electrode voltage clamp it was confirmed that the ligands were able to modulate the histamine H3 receptor on a second-scale in a light dependent fashion. The developed tool compounds allow for novel avenues in receptor signaling research and can ultimately give insights into how this complex receptor communicates with various cellular processes. These insights may help to understand why most developed ligands for the histamine H3 receptor have a low success rate in clinical trials.
The work presented at the meeting is part of the PhD project of Hauwert under the supervision of Dr Maikel Wijtmans and Prof. Rob Leurs in the Medicinal Chemistry research group of VU Amsterdam, where he is working together with synthetic medicinal chemists, molecular pharmacologists, and biochemists on the multidisciplinary NWO Chemical Sciences TOP-PUNT project 7 ways to 7TMR modulation. Together with his colleagues Hauwert is studying different ways to modulate the function of seven-transmembrane G protein-coupled receptors (GPCRs).