6zl4

the structure of glutamate transporter homologue GltTk in complex with the photo switchable compound (cis)

spinqualitylabelsall models 6zl4, resolution 3.00Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6zl4 is a 3 chain structure with sequence from Thermococcus kodakarensis. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 3Å Ligands: 1PE, DMU, NA, PEG, PG4, PGE, QM5 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function Q5JID0_THEKO Publication Abstract from PubMed Photopharmacology addresses the challenge of drug selectivity and side effects through creation of photoresponsive molecules activated with light with high spatiotemporal precision. This is achieved through incorporation of molecular photoswitches and photocages into the pharmacophore. However, the structural basis for the light-induced modulation of inhibitory potency in general is still missing, which poses a major design challenge for this emerging field of research. Here we solved crystal structures of the glutamate transporter homologue GltTk in complex with photoresponsive transport inhibitors-azobenzene derivative of TBOA (both in trans and cis 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. Structural Aspects of Photopharmacology: Insight into the Binding of Photoswitchable and Photocaged Inhibitors to the Glutamate Transporter Homologue.,Arkhipova V, Fu H, Hoorens MWH, Trinco G, Lameijer LN, Marin E, Feringa BL, Poelarends GJ, Szymanski W, Slotboom DJ, Guskov A J Am Chem Soc. 2021 Jan 15. doi: 10.1021/jacs.0c11336. PMID:33449695 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Symporter 3D structures

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