The serotonin 5-HT3 receptor is a ligand-gated ion channel, which by virtue of its pentameric architecture, can be considered to be an intriguing example of intrinsically multivalent biological receptors. This paper describes a general design approach to the study of multivalency in this multimeric ion channel. Bivalent ligands for 5-HT3 receptor have been designed by linking an arylpiperazine moiety to probes showing different functional features. Both homobivalent and heterobivalent ligands have shown 5-HT3 receptor affinity in the nanomolar range, providing evidence for the viability of our design approach. Moreover, the high affinity shown by homobivalent ligands suggests that bivalency is a promising approach in 5-HT3 receptor modulation and provides the rational basis for applying the concepts of multivalency to the study of 5-HT3 receptor function.

Cappelli, A., Manini, M., Paolino, M., A., G., Anzini, M., L., M., et al. (2011). Bivalent Ligands for the Serotonin 5-HT3 Receptor. ACS MEDICINAL CHEMISTRY LETTERS, 2, 571-576 [10.1021/ml2000388].

Bivalent Ligands for the Serotonin 5-HT3 Receptor

CAPPELLI, ANDREA;MANINI, MONICA;PAOLINO, MARCO;ANZINI, MAURIZIO;VOMERO, SALVATORE
2011-01-01

Abstract

The serotonin 5-HT3 receptor is a ligand-gated ion channel, which by virtue of its pentameric architecture, can be considered to be an intriguing example of intrinsically multivalent biological receptors. This paper describes a general design approach to the study of multivalency in this multimeric ion channel. Bivalent ligands for 5-HT3 receptor have been designed by linking an arylpiperazine moiety to probes showing different functional features. Both homobivalent and heterobivalent ligands have shown 5-HT3 receptor affinity in the nanomolar range, providing evidence for the viability of our design approach. Moreover, the high affinity shown by homobivalent ligands suggests that bivalency is a promising approach in 5-HT3 receptor modulation and provides the rational basis for applying the concepts of multivalency to the study of 5-HT3 receptor function.
Cappelli, A., Manini, M., Paolino, M., A., G., Anzini, M., L., M., et al. (2011). Bivalent Ligands for the Serotonin 5-HT3 Receptor. ACS MEDICINAL CHEMISTRY LETTERS, 2, 571-576 [10.1021/ml2000388].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/21294
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