Structural Aspects of Photopharmacology: Insight into the Binding of Photoswitchable and Photocaged Inhibitors to the Glutamate Transporter Homologue
Valentina Arkhipova, Haigen Fu, Mark W. H. Hoorens, Gianluca Trinco, Lucien N. Lameijer, Egor Marin, Ben L. Feringa, Gerrit J. Poelarends, Wiktor Szymański, Dirk Jan Slotboom, Albert Guskov
Abstract
configuration) and with the photocaged compound ONB-hydroxyaspartate. The essential role of glutamate transporters in the functioning of the central nervous system renders them potential therapeutic targets in the treatment of neurodegenerative diseases. The obtained structures provide a clear structural insight into the origins of photocontrol in photopharmacology and lay the foundation for application of photocontrolled ligands to study the transporter dynamics by using time-resolved X-ray crystallography.
Topics & Concepts
ChemistryExcitatory amino-acid transporterTransporterGlutamate receptorStereochemistryBiochemistryGeneReceptorPhotochromic and Fluorescence ChemistryOrganic Chemistry Cycloaddition ReactionsPhotoreceptor and optogenetics research