Structural models and conformational dynamics of the G protein coupled bile acid receptor TGR5 (B02)

• Subject Area: Structural Biology
• Term: from 2012 to 2016
• Project identifier: Deutsche Forschungsgemeinschaft (DFG) - Project number 190586431

The project focuses on the structural investigation of signaling properties of the bile acid G-protein coupled receptor TGR5 as well as the structure-based development of small molecule modulators/ inhibitors of TGR5 signaling. Using the binding model of TGR5-agonists, TGR5-antagonist will be identified using a computer-based approach, further characterized in vitro using NMR and fluorescence-spectroscopy and validated using ex vivo functional studies. In addition, a novel approach to modulate the TGR5/ G-protein interaction by small molecule inhibitors will be pursued.

• DFG Programme: Collaborative Research Centres
• Subproject of: SFB 974: Communication and System Relevance in Liver Injury and Regeneration
• Applicant Institution: Heinrich-Heine-Universität Düsseldorf
• Project Heads: Professor Dr. Holger Gohlke; Professorin Dr. Verena Keitel-Anselmino; Professor Dr. Claus Seidel