The G-Protein Family and Their Interaction with Receptors*

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Abstract
Introduction THE FAMILY of GTP-binding proteins, called Gproteins, provides a signal transduction coupling mechanism for many cell surface receptors. The receptors act catalytically to mediate guanine nucleotide exchange at the GDP-GTP binding site of G-proteins. This process is referred to as activation and results in the displacement of bound GDP for GTP. The GTP-bound form of the G-protein then initiates a cellular response by altering the activity of specific enzymes. Examples of such signal transduction systems include the receptor regulation of adenylyl cyclase activity and the photoreceptor regulation of cyclic (c)GMP phosphodiesterase. Recent evidence also suggests that specific ion channels may be regulated by G-proteins. As detailed in this review, recent elucidation of both receptor and G-protein primary sequence has allowed structural predictions and new experimental approaches to study the mechanism of receptor-catalyzed G-protein regulation of effector systems and the control of cell function.

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