G Protein-Coupled Receptor
This learning journey is designed to provide an overview of the GPCR family of proteins and their significance as therapeutic targets. It covers several important concepts including structure and function, key GPCR-mediated signalling pathways, involvement in human health and disease, and the development of GPCR-targeted therapies.
Table of Contents
- An introduction to GPCRs (1)
- An introduction to GPCRs (2)
- A summary of GPCR signalling
- Typical GPCR structure and coupling
- GPCR signalling via ligand interactions with agonists/antagonists
- GPCR and G-protein function in hormone signalling
- The topology of adenylyl cyclase
- Arrestins and the modulation of GPCR signalling
- GPCR oligomers and allosterism
- An introduction to adhesion GPCRs
- Adhesion GPCRs as metabotropic mechanosensors
- GPCR involvement in the modulation of pain
- GPCRs as therapeutic targets in neurodegenerative disease
- Utilizing the structure of GPCRs for drug discovery
- Evaluating GPCR signalling for drug discovery
1. An introduction to GPCRs (1)
By Dr. Aylin Hanyaloglu – Imperial College London, UK
An excerpt from Super-resolution imaging of GPCR oligomers: applications and functional roles
2. An introduction to GPCRs (2)
By Prof. Tobias Langenhan – Leipzig University, Germany
An excerpt from Adhesion GPCRs in nervous system development and disease
3. A summary of GPCR signalling
By Dr. Graham Ladds – University of Cambridge, UK
An excerpt from Computational modelling of GPCR signalling dynamics
4. Typical GPCR structure and coupling
By Dr. Sergi Ferré – National Institute on Drug Abuse, USA
An excerpt from Pre-coupling of receptor oligomers and signaling molecules
5. GPCR signalling via ligand interactions with agonists/antagonists
By Prof. Dr. Peter Kolb – Philipps-Universität Marburg, Germany
An excerpt from Drugging conformational states of GPCRs
6. GPCR and G-protein function in hormone signalling
By Prof. Gerald W. Feigenson – Cornell University, USA
An excerpt from Hormone mechanisms
7. The topology of adenylyl cyclase
By Dr. Sergi Ferré – National Institute on Drug Abuse, USA
An excerpt from Pre-coupling of receptor oligomers and signaling molecules
8. Arrestins and the modulation of GPCR signalling
By Prof. Vsevolod V. Gurevich – Vanderbilt University, USA
An excerpt from Biology and structure of arrestin proteins
9. GPCR oligomers and allosterism
By Dr. Sergi Ferré – National Institute on Drug Abuse, USA
An excerpt from Pre-coupling of receptor oligomers and signaling molecules
10. An introduction to adhesion GPCRs
By Prof. Tobias Langenhan – Leipzig University, Germany
An excerpt from Adhesion GPCRs in nervous system development and disease
11. Adhesion GPCRs as metabotropic mechanosensors
By Prof. Tobias Langenhan – Leipzig University, Germany
An excerpt from Adhesion GPCRs in nervous system development and disease
12. GPCR involvement in the modulation of pain
By Prof. Dr. Christoph Stein – Charité - Universitätsmedizin Berlin, Germany
An excerpt from GPCRs and pain
13. GPCRs as therapeutic targets in neurodegenerative disease
By Prof. Andrew B. Tobin – University of Glasgow, UK
An excerpt from Novel approaches to treating symptoms and slowing the progress of neurodegenerative diseases
14. Utilizing the structure of GPCRs for drug discovery
By Prof. Dr. Peter Kolb – Philipps-Universität Marburg, Germany
An excerpt from Drugging conformational states of GPCRs
15. Evaluating GPCR signalling for drug discovery
By Prof. Terry Hébert – McGill University, Canada
An excerpt from What can we learn from conformational profiling of GPCRs?