Regulation of a proton-sensing G-protein-coupled receptor for cancer therapy: a combined in vitro and in silico study

Arianna Fornili (primary)
School of Biological and Chemical Sciences
Queen Mary University of London
Lesley Howell (secondary)
School of Biological and Chemical Sciences
Queen Mary University of London


G-protein coupled receptors (GPCRs) are transmembrane proteins involved in a wide range of cell signalling processes. Their regulation through small molecule modulators is used for the treatment of different types of diseases and GPCRs currently account for more than 30% of drug targets. Recent evidence has highlighted the role of the pH-sensing GPR68 receptor in different cancers, so that it is considered as a new potential target in cancer therapy. The aim of this project is to understand the regulation mechanism of GPR68 and identify both selective antagonists and allosteric modulators using a combination of computational and experimental techniques.


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* Ludwig M-G, Vanek M, Guerini D, Gasser JA, Jones CE, Junker U, et al. Proton-sensing G-protein-coupled receptors. Nature. 2003;425:93
* Pandini A, Fornili A, Fraternali F, Kleinjung J. Detection of allosteric signal transmission by information-theoretic analysis of protein dynamics. The FASEB Journal. 2012;26: 868.

Molecules, cells and industrial biotechnology
Area of Biology
Chemical BiologyStructural Biology
Techniques & Approaches
BiochemistryBioinformaticsChemistryMathematics / StatisticsMolecular BiologySimulation / Modelling