Synthesis and Characterization of Photoaffinity Probes that Target the 5-HT<SUB>3</SUB> Receptor

Jack, Thomas; Ruepp, Marc-David; Thompson, Andrew J.; Mühlemann, Oliver; Lochner, Martin (2014). Synthesis and Characterization of Photoaffinity Probes that Target the 5-HT<SUB>3</SUB> Receptor. CHIMIA, 68(4), pp. 239-242. Bern: Schweizerische Chemische Gesellschaft 10.2533/chimia.2014.239

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Abstract: 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.

Item Type:

Journal Article (Original Article)

Division/Institute:

08 Faculty of Science > Departement of Chemistry and Biochemistry

UniBE Contributor:

Jack, Thomas; Ruepp, Marc-David; Mühlemann, Oliver and Lochner, Martin

Subjects:

500 Science > 570 Life sciences; biology
500 Science > 540 Chemistry

ISSN:

0009-4293

Publisher:

Schweizerische Chemische Gesellschaft

Language:

English

Submitter:

Christina Schüpbach

Date Deposited:

25 Jun 2014 09:43

Last Modified:

01 May 2015 02:30

Publisher DOI:

10.2533/chimia.2014.239

BORIS DOI:

10.7892/boris.52634

URI:

https://boris.unibe.ch/id/eprint/52634

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