G Proteins (Heterotrimeric)

Supporting information

Heterotrimeric G proteins are membrane bound GTPases that are linked to 7-TM receptors. Each G protein contains an α-, β- and γ-subunit and is bound to GDP in the 'off' state. Ligand binding to a 7-TM receptor causes a conformational change in the receptor, which detaches the G protein. This switches the G protein to an 'on' state, allowing GTP to displace GDP, thus Gα can activate second messenger signaling cascades.

There are several types of Gα proteins; Gαs and Gαi bind directly to adenylyl cyclase and stimulate or inhibit its activity, leading to an increase or decrease in cAMP levels respectively. Gαq/11 stimulates PLCβ which catalyzes the hydrolysis of PIP2 to the second messengers IP3 and DAG. Gα12/13 are involved in Rho family GTPase signaling. In addition, some Gβγ subunits have active functions; Gβγ coupled to H1 receptors can activate PLA2 and Gβγ coupled to M1 receptors can activate KIR channels.

Rapid termination of the cellular response is required once the concentration of the stimulating ligand decreases. GTP bound to Gα is hydrolyzed rapidly to GDP, Gα is converted to its inactive form and re-associates with the β- and γ-subunits returning to the 'off' state.

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Gαi1 Human GNAI1 NM_002069 P63096
Mouse Gnai1 NM_010305 NP_034435
Rat Gnai1 NM_013145 P10824
Gαi2 Human GNAI2 NM_002070 P04899
Mouse Gnai2 NM_008138 P08752
Rat Gnai2 NM_031035 Q5EEY4
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Literature for G Proteins (Heterotrimeric)

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