Photopharmacology: shedding light on the future of photoswitchable GPCR ligands

Niels Hauwert MSc
Division of Medicinal Chemistry
University of Amsterdam

Photopharmacology is a discipline that uses photoswitchable ligands as pharmacological tool compounds to yield spatiotemporal control of protein activity with light. However, photopharmacology in the G protein-coupled receptor (GPCR) field is still in its infancy. In this presentation, our general approach towards GPCR photopharmacology will be discussed as well as recent contributions from our laboratory including several series of photoisomerisable azobenzene-based GPCR ligands. First-generation series involve photoswitchable antagonist or agonist ligands that shift affinity/potency for an aminergic GPCR upon illumination. In a second-generation series, we incorporated a change in the ligand efficacy for a peptidergic GPCR upon illumination, thus establishing a photoswitch from antagonism to agonism. Our contributions deliver a toolbox of compounds capable of photomodulating GPCR signaling in complementary ways.

Niels Hauwert received his bachelor’s degree in chemistry from the Hogeschool Utrecht and a master’s degree in Drug Discovery and Safety from the Vrije Universiteit Amsterdam. Currently, he is a last year PhD student in the division of Medicinal Chemistry of the Vrije Universiteit Amsterdam under supervision of prof. dr. Rob Leurs, prof. dr. Iwan De Esch and Dr. Maikel Wijtmans. His research focusses on the development of photoactive ligands for histamine receptors. In 2017 he was the recipient of the Young Investigator award of the European Histamine Research Society (EHRS).

Niels Hauwert MSc

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