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Bioinformatics Advance Access originally published online on April 15, 2004
Bioinformatics 2004 20(15):2411-2420; doi:10.1093/bioinformatics/bth263
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Bioinformatics 20(15) © Oxford University Press 2004; all rights reserved.

Explicit formulation of different receptor–G-protein interactions and effector regulation

Jyrki P. Kukkonen

Department of Neuroscience, Unit of Physiology, Uppsala University, BMC, P.O. Box 572, SE-75123 Uppsala, Sweden

Received on September 15, 2003; revised on March 17, 2004; accepted on April 2, 2004
Advance Access Publication April 15, 2004

Motivation: G-protein-coupled receptors (GPCRs) can create different intracellular signals depending on which G-proteins they couple to and which intracellular signal-integrators, such as adenylyl cyclases, are expressed in the cell. One and the same GPCR can activate multiple G-protein species, generating signals, which either inhibit or amplify each other. Because of this complexity, extraction of mechanistic information from concentration–response curves is not straightforward.

Results: To tackle this problem, I describe in this paper explicit equations for GPCR-interaction with two G-protein species by different possible mechanisms, and also an equation for the regulation of an effector enzyme by the activated G-proteins or their effectors. Arithmetic solutions to these equations are presented, which resulted in the equations being applicable in a spreadsheet program environment. These equations are useful in simulations to analyze results, to design experiments and to test hypotheses. Some examples of this are presented in this study.

Contact: jyrki.kukkonen{at}fysiologi.uu.se


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