Protein Docking verified with experiment to explain how G-proteins activate GIRK channels

What is it about?

G-proteins are fundamental to cell signalling in converting extracellular signals to intracellular actions. Although the alpha subunit of G-proteins has been studied since the 1950s, the Beta-Gamma subunit of G-proteins was first showed to directly regulate proteins in 1987 when it was shown they activate GIRK channels critical to cardiac and neuronal physiology. How the Beta-gamma subunit interacts with GIRK channels and controls their activity has been an open question since 1987 with various cell biology/protein chemistry methods employed to explore the question with limited success. We thus used computational protein docking to tackle the problem and developed a model which was verified by experiments and suggested a mechanism by which these important channels are activated.

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Why is it important?

Unique combination of protein docking tools was used to answer an open question about G-protein regulation of an effector protein critical to heart, neuronal, endocrine, and immune system physiology.