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Open Access Synthesis and Characterization of Photoaffinity Probes that Target the 5-HT3 Receptor

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The 5-HT3 receptor is one of several ion channels responsible for the transmission of nerve impulses in the peripheral and central nervous systems. Until now, it has been difficult to characterize transmembrane receptors with classical structural biology approaches like X-ray crystallography. The use of photoaffinity probes is an alternative approach to identify regions in the protein where small molecules bind. To this end, we present two photoaffinity probes based on granisetron, a well known antagonist of the 5-HT3 receptor. These new probes show nanomolar binding affinity for the orthosteric binding site. In addition, we investigated their reactivity using irradiation experiments.

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Keywords: 5-HT3 RECEPTOR; GRANISETRON; PHOTO-LABELING; PHOTOAFFINITY PROBES; SEROTONIN RECEPTOR

Document Type: Research Article

Affiliations: 1: Universität Bern Departement für Chemie und Biochemie Freiestrasse 3 CH-3012 Bern, Switzerland 2: Universität Bern Departement für Chemie und Biochemie Freiestrasse 3 CH-3012 Bern, Switzerland. [email protected]

Publication date: April 1, 2014

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  • International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions

    CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.

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