Site-directed mutagenesis of the serotonin 5-Hydroxytryptamine2c receptor: identification of amino acids responsible for sarpogrelate binding.

@article{Muntasir2006SitedirectedMO,
  title={Site-directed mutagenesis of the serotonin 5-Hydroxytryptamine2c receptor: identification of amino acids responsible for sarpogrelate binding.},
  author={Habib Abul Muntasir and Jyuniti Takahashi and Mamunur Rashid and Maruf Ahmed and Tadazumi Komiyama and Murad Hossain and Jun Kawakami and Masayuki Nashimoto and Takafumi Nagatomo},
  journal={Biological & pharmaceutical bulletin},
  year={2006},
  volume={29 8},
  pages={
          1645-50
        }
}
Site-directed mutagenesis was used to investigate the molecular interactions involved in sarpogrelate binding to the human 5-Hydroxytryptamine(5-HT)2C receptor. Based on molecular modeling studies, Aspartic acid (Asp)155[3.32] in transmembrane region III and Serine(Ser)361[7.46] in transmembrane region VII of the 5-HT2C receptor were found to interact with sarpogrelate. Asp3.32 and Ser7.46 were mutated to alanine (Ala) and expressed in COS-7 cells. The radioligand [3H]mesulergine did not show… CONTINUE READING

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