Modelling the activation of G-protein coupled receptors by a single drug

Woodroffe, P. J.; Bridge, Lloyd; King, J. R.; Hill, S. J.

Abstract

In this paper, the most popular proposed mechanism for activation of G-protein coupled receptors (GPCRs) - the shuttling mechanism - is modelled mathematically. An asymptotic analysis of this model clarifies the dynamics of the system in the presence of a drug, in particular identifying which reactions dominate during the different timescales. The modelling also reveals challenging behaviour in the form of a peak response. This new mechanism gives simple explanations for complex, possibly misunderstood, behaviour. © 2009 Elsevier Inc. All rights reserved.

Citation

Woodroffe, P. J., Bridge, L., King, J. R., & Hill, S. J. (2009). Modelling the activation of G-protein coupled receptors by a single drug. Mathematical Biosciences, 219(1), 32-55. https://doi.org/10.1016/j.mbs.2009.02.003

• Journal Article Type: Article
• Acceptance Date: Feb 13, 2009
• Publication Date: May 1, 2009
• Journal: Mathematical Biosciences
• Print ISSN: 0025-5564
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 219
• Issue: 1
• Pages: 32-55
• DOI: https://doi.org/10.1016/j.mbs.2009.02.003
• Keywords: g-protein coupled receptor, cell signalling, asymptotic analysis
• Public URL: https://uwe-repository.worktribe.com/output/1006510
• Publisher URL: http://dx.doi.org/10.1016/j.mbs.2009.02.003