Mutagenesis and molecular modeling reveal the importance of the 5-HT3 receptor F-loop.

@article{Thompson2006MutagenesisAM,
  title={Mutagenesis and molecular modeling reveal the importance of the 5-HT3 receptor F-loop.},
  author={Andrew J Thompson and Claire L. Padgett and Sarah C. R. Lummis},
  journal={The Journal of biological chemistry},
  year={2006},
  volume={281 24},
  pages={16576-82}
}
The 5-HT(3) receptor is a member of the Cys-loop family of ligand-gated ion channels. The extracellular domains of these proteins contain six amino acid loops (A-F) that converge to form the ligand binding site. In this study we have mutated 21 residues in or close to the 5-HT(3) receptor F-loop (Ile(192) to Gly(212)) to Ala or to a residue with similar chemical properties. Mutant receptors were expressed in HEK293 cells, and binding affinity was measured using [(3)H]granisetron. Two regions… CONTINUE READING