Ruepp, Marc-David (11 January 2013). Synthesis and testing of photoaffinity probes for the site-selective chemical modifications of the 5-HT3 receptor (Unpublished). In: 11th Swiss Snow Symposium 2013. Saas-Fee, CH. 11.-13.01.2013.
The 5-HT3 receptor (5-HT3R) is an important ion channel responsible for the transmission of nerve impulses in the central nervous system.[1] It is difficult to characterize transmembrane dynamic receptors with classical structural biology approaches like crystallization and x-ray. The use of photoaffinity probes is an alternative approach to identify regions in the protein that are important for the binding of small molecules. Therefore we synthesized a small library of photoaffinity probes by conjugating photolabile building blocks via various linkers to granisetron which is a known antagonist of the 5-HT3R. We were able to obtain several compounds with diverse linker lengths and different photo-labile moieties that show nanomolar binding affinities for the orthosteric binding site. Further on we developed a stable 5-HT3R overexpressing cell line and a purification method to yield the receptor in a high purity. Currently we are investigating crosslinking experiments and subsequent MS – analysis.
Item Type: |
Conference or Workshop Item (Poster) |
|---|---|
Division/Institute: |
08 Faculty of Science > Department of Chemistry, Biochemistry and Pharmaceutical Sciences (DCBP) |
UniBE Contributor: |
Ruepp, Marc-David |
Subjects: |
500 Science > 570 Life sciences; biology 500 Science > 540 Chemistry |
Language: |
English |
Submitter: |
Christina Schüpbach |
Date Deposited: |
05 Aug 2014 14:25 |
Last Modified: |
05 Dec 2022 14:36 |
Additional Information: |
SCS events |
URI: |
https://boris.unibe.ch/id/eprint/57535 |
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