G Proteins (Heterotrimeric)

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 causes a receptor conformational change, detaching the G protein and switching it 'on'.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
2974 CCG 2046
Inhibitor of regulator of G-protein signaling 4 (RGS4)
4567 CCG 50014
Potent and selective inhibitor of regulator of G-protein signaling 4 (RGS4) protein
4028 CCG 63802
Inhibitor of regulator of G-protein signaling 4 (RGS4) protein
5642 CMPD101
Potent and selective GRK2/3 inhibitor
4773 ESI 09
EPAC inhibitor
1931 G-Protein antagonist peptide
Inhibits G protein activation by GPCRs
3090 Gallein
Inhibitor of βγ signaling
3594 GRK2i
GRK2 inhibitory polypeptide. Gβγ antagonist
4742 Gue 1654
Selective inhibitor of OXE-R Gβγ signaling
1240 NF 023
Inhibitor of Go/i α-subunits; also P2X1 purinoceptor antagonist
1400 SCH 202676 hydrobromide
Inhibitor of ligand binding to G-protein-coupled receptors
1884 [D-Trp7,9,10]-Substance P
Inhibits M1 ACh receptor activation of Gq/11

Activators

Cat No Product Name / Activity
1192 Mastoparan
Activates Gi and Go

Other

Cat No Product Name / Activity
1089 8-Bromo-cGMP, sodium salt
cGMP analog; activates PKG
1193 Melittin
Inhibits Gs and stimulates Gi activity
3097 Pertussis Toxin
Catalyzes ADP-ribosylation of Gi, Go and Gt
1472 Suramin hexasodium salt
Uncouples G proteins from receptors. Also purinoceptor antagonist

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.

Literature for G Proteins (Heterotrimeric)

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Heterotrimeric G Protein Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Gαi
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
Gαi3 Human GNAI3 NM_006496 P08754
Mouse Gnai3 NM_010306 Q9DC51
Rat Gnai3 NM_013106 P08753
Gαz Human GNAZ NM_002073 P19086
Mouse Gnaz NM_010311 O70443
Rat Gnaz NM_013189 P19627
Gαo1/2 Human GNAO1 NM_020988 P09471
Mouse Gnao1 NM_001113384 P18872
Rat Gnao1 NM_017327 Q8R4R5
Gαt1 Human GNAT1 NM_000172 P11488
Mouse Gnat1 NM_008140 P20612
Rat Gnat1 NM_001108780 XP_343481
Gαt2 Human GNAT2 NM_005272 P19087
Mouse Gnat2 NM_008141 P50149
Rat Gnat2 NM_001108950 XP_345272
Gαt3 Human GNAT3 XM_294370 A8MTJ3
Mouse Gnat3 NM_001081143 Q3V3I2
Rat Gnat3 NM_173139 P29348
Gαs
Gαs Human GNAS NM_000516 Q8TBC0
Mouse Gnas NM_010309 Q6R0H7
Rat Gnas NM_021845 Q9Z213
Gαolf Human GNAL NM_182978 P38405
Mouse Gnal NM_177137 Q8CGK7
Gαq
Gαq Human GNAQ NM_002072 P50148
Mouse Gnaq NM_008139 P21279
Rat Gnaq NM_031036 P82471
Gα11 Human GNA11 NM_002067 P29992
Mouse Gna11 NM_010301 P21278
Rat Gna11 NM_031033 Q63229
Gα14 Human GNA14 NM_004297 O95837
Mouse Gna14 NM_008137 P30677
Rat Gna14 NM_001013151 Q5EAP4
Gα15 Human GNA15 NM_002068 P30679
Mouse Gna15 NM_010304 P30678
Rat Gna15 NM_053542 O88302
Gα12/13
Gα12 Human GNA12 NM_007353 Q03113
Mouse Gna12 NM_010302 P27600
Rat Gna12 NM_031034 Q45QM2
Gα13 Human GNA13 NM_006572 Q14344
Mouse Gna13 NM_010303 P27601
Rat Gna13 NM_001013119 Q6Q7Y5
Gβ
Gβ1 Human GNB1 NM_002074 P62873
Mouse Gnb1 NM_008142 P62874
Rat Gnb1 NM_030987 P54311
Gβ2 Human GNB2 NM_005273 P62879
Mouse Gnb2 NM_010312 P62880
Rat Gnb2 NM_031037 Q9QX35
Gβ3 Human GNB3 NM_002075 P16520
Mouse Gnb3 NM_013530 Q61011
Rat Gnb3 NM_021858 Q45QL4
Gβ4 Human GNB4 NM_021629 Q9HAV0
Mouse Gnb4 NM_013531 P29387
Rat Gnb4 NM_001013910 Q45QL2
Gβ5 Human GNB5 NM_006578 O14775
Mouse Gnb5 NM_138719 P62881
Rat Gnb5 NM_031770 P62882
Gγ
Gγt1 Human GNGT1 NM_021955 P63211
Mouse Gngt1 NM_010314 Q61012
Rat Gngt1 NM_001135777 XP_001054660
Gγt2 Human GNGT2 NM_031498 O14610
Mouse Gngt2 NM_001038664 Q61017
Rat Gngt2 NM_001135767 XP_001075781
Gγ2 Human GNG2 NM_053064 P59768
Mouse Gng2 NM_010315 P63213
Rat Gng2 AF022087 Q45QK6
Gγ3 Human GNG3 NM_012202 P63215
Mouse Gng3 NM_010316 P63216
Rat Gng3 XM_001074064 O35356
Gγ4 Human GNG4 NM_004485 P50150
Mouse Gng4 NM_010317 P50153
Rat Gng4 XM_001053747 O35357
Gγ5 Human GNG5 NM_005274 P63218
Mouse Gng5 NM_010318 Q80SZ7
Rat Gng5 NM_024377 P63219
Gγ7 Human GNG7 NM_052847 O60262
Mouse Gng7 NM_001038655 Q61016
Rat Gng7 NM_024138 P43425
Gγ8 Human GNG8 NM_033258 Q9UK08
Mouse Gng8 NM_010320 P63078
Rat Gng8 NM_139185 P63077
Gγ10 Human GNG10 NM_001017998 P50151
Mouse Gng10 NM_025277 Q9CXP8
Rat Gng10 NM_053660 Q3KRE3
Gγ11 Human GNG11 NM_004126 P61952
Mouse Gng11 NM_025331 P61953
Rat Gng11 NM_022396 P61954
Gγ12 Human GNG12 NM_018841 Q9UBI6
Mouse Gng12 NM_025278 Q9DAS9
Rat Gng12 XM_578287 O35359
Gγ13 Human GNG13 NM_016541 Q9P2W3
Mouse Gng13 NM_022422 Q9JMF3
Rat Gng13 NM_001135918 Q45QJ8