March 2016 – Vanderbilt / Leipzig University

The joint publication of Hu, Stern, Gimenez, Wanka, Zhu, Rossi, Meister, Inoue, Beck-Sickinger, Gurevich and Wess was named as “Paper of the Week” by the Journal of Biological Chemistry’s editorial board, landing it in the top 2 percent of all papers published over the year in the journal. The joint publication focussed on designer receptors exclusively activated by a designer drug – short DREADDs. This are CNO sensitive designer G protein-coupled receptors which are able to activate heterotrimeric G proteins and also trigger arrestin-dependent signaling. In the present study the development of a mutationally modified version of a non-biased DREADD derived from the M3 muscarinic receptor that can activate Gq/11 with

During an internship in the lab of Dave Weaver at Vanderbilt University, I got the opportunity to gain more information about the Y4R, by testing a variety of similar structurally related compounds. I was introduced in the workflow of a high throughput screening laboratory. The technical equipment in the Vanderbilt HTS center makes it possible to test thousands of different chemical compounds in a very short time. Therefore, I learned to perform Ca2+-flux based signal transduction screening assays to monitor the activation of the Y4R. Using this system, I could test new hit compounds out of the ongoing screening for activity and selectivity. Furthermore, I tested structurally similar compounds of a

Journal of Biological Chemistry selects Vanderbilt-Leipzig article as paper of the week

Short report by Mario Schubert: HTS to Identify and Characterize Small Molecule Allosteric Modulators of the Human Y4 Receptor at Vanderbilt University (Oct 19 – Dec 15)