Development of Allosteric and Bitopic Ligands to Tune Receptor Signalling. G protein-coupled receptors are the largest protein family encoded by the human genome and the largest class of drug target.

Description

Development of Allosteric and Bitopic Ligands to Tune Receptor Signalling. G protein-coupled receptors are the largest protein family encoded by the human genome and the largest class of drug target. These receptors are located on the cell membrane and transduce extracellular signals into physiological effects within the cell. This proposal aims to develop new chemical-biology probes for selectively targeting signalling pathways mediated by these receptors using the M4 muscarinic acetylcholine receptor as an exemplar. Novel ligands that possess different binding modes to the natural ligand (i.e. allosteric and bitopic ligands) will be developed and their potential to act as pathway selective agents that can preferentially activate the desired signalling pathways and reduce unwanted side effects will be explored.. Scheme: Discovery Projects. Field: 3101 - Biochemistry and Cell Biology. Lead: Prof Peter Scammells