Ontology highlight
ABSTRACT:
SUBMITTER: Kesters D
PROVIDER: S-EPMC3537142 | biostudies-literature | 2013 Jan
REPOSITORIES: biostudies-literature
Kesters Divya D Thompson Andrew J AJ Brams Marijke M van Elk René R Spurny Radovan R Geitmann Matthis M Villalgordo Jose M JM Guskov Albert A Danielson U Helena UH Lummis Sarah C R SC Smit August B AB Ulens Chris C
EMBO reports 20121130 1
The 5-HT(3) receptor is a pentameric serotonin-gated ion channel, which mediates rapid excitatory neurotransmission and is the target of a therapeutically important class of anti-emetic drugs, such as granisetron. We report crystal structures of a binding protein engineered to recognize the agonist serotonin and the antagonist granisetron with affinities comparable to the 5-HT(3) receptor. In the serotonin-bound structure, we observe hydrophilic interactions with loop E-binding site residues, wh ...[more]