Mol Endocrinol 2007,
PMID: 17405905
Kumar, Premlata; Wu, Qian; Chambliss, Ken L; Yuhanna, Ivan S; Mumby, Susanne M; Mineo, Chieko; Tall, Gregory G; Shaul, Philip W
Estrogen induces G protein-dependent nongenomic signaling in a variety of cell types via the activation of a plasma membrane-associated subpopulation of estrogen receptor alpha (ER alpha). Using pull-down experiments with purified recombinant proteins, we now demonstrate that ER alpha binds directly to G alpha i and G betagamma. Mutagenesis and the addition of blocking peptide reveals that this occurs via amino acids 251-260 and 271-595 of ER alpha, respectively. Studies of ER alpha complexed with heterotrimeric G proteins further show that estradiol causes the release of both G alpha i and G betagamma without stimulating GTP binding to G alpha i. Moreover, in COS-7 cells, the disruption of ER alpha-G alpha i interaction by deletion mutagenesis of ER alpha or expression of blocking peptide, as well as G betagamma sequestration with beta-adrenergic receptor kinase C terminus, prevents nongenomic responses to estradiol including src and erk activation. In endothelial cells, the disruption of ER alpha-G alpha i interaction prevents estradiol-induced nitric oxide synthase activation and the resulting attenuation of monocyte adhesion that contributes to estrogen-related cardiovascular protection. Thus, through direct interactions, ER alpha mediates a novel mechanism of G protein activation that provides greater diversity of function of both the steroid hormone receptor and G proteins.
Document information provided by NCBI PubMed
Text Mining Data
nitric oxide synthase → ER alpha-G: "
In endothelial cells, the disruption of
ER alpha-G alpha i interaction
prevents estradiol induced
nitric oxide synthase activation and the resulting attenuation of monocyte adhesion that contributes to estrogen related cardiovascular protection
"
Manually curated Databases
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
Gai/GDP complex (GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1)
→
G beta/gamma complex (GNB1-GNG2)
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
Gai/GDP complex (GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1)
→
ER alpha/Gai/GDP/Gbeta gamma complex (ESR1-GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1-GNB1-GNG2)
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
Gai/GDP complex (GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1)
→
None
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
Gai/GDP complex (GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1)
→
E2/ER alpha (dimer) complex (ESR1)
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
G beta/gamma complex (GNB1-GNG2)
→
ER alpha/Gai/GDP/Gbeta gamma complex (ESR1-GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1-GNB1-GNG2)
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
G beta/gamma complex (GNB1-GNG2)
→
None
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
G beta/gamma complex (GNB1-GNG2)
→
E2/ER alpha (dimer) complex (ESR1)
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
ER alpha/Gai/GDP/Gbeta gamma complex (ESR1-GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1-GNB1-GNG2)
→
None
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
ER alpha/Gai/GDP/Gbeta gamma complex (ESR1-GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1-GNB1-GNG2)
→
E2/ER alpha (dimer) complex (ESR1)
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
None
→
E2/ER alpha (dimer) complex (ESR1)
(modification, collaborate)
Evidence: mutant phenotype, physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
E2/ER alpha (dimer)/PELP1/Src/p52 SHC complex (ESR1-PELP1-SRC-SHC1)
→
E2/ER alpha (dimer)/PELP1/Src/p52 SHC/GRB2/SOS1 complex (ESR1-PELP1-SRC-SHC1-GRB2-SOS1)
(modification, collaborate)
Evidence: physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
E2/ER alpha (dimer)/PELP1/Src/p52 SHC complex (ESR1-PELP1-SRC-SHC1)
→
GRB2/SOS1 complex (GRB2-SOS1)
(modification, collaborate)
Evidence: physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
E2/ER alpha (dimer)/PELP1/Src/p52 SHC/GRB2/SOS1 complex (ESR1-PELP1-SRC-SHC1-GRB2-SOS1)
→
GRB2/SOS1 complex (GRB2-SOS1)
(modification, collaborate)
Evidence: physical interaction
-
NCI Pathway Database Plasma membrane estrogen receptor signaling:
ER alpha/Gai/GDP/Gbeta gamma complex (ESR1-GNAI2_GNAI3_GNAO1_GNAO1_GNAZ_GNAI1-GNB1-GNG2)
→
Src (SRC)
(modification, activates)
Evidence: mutant phenotype
In total, 63 gene pairs are associated to this article in curated databases