Estrogen receptor activation function 1 works by binding p160 coactivator proteins.
Estrogen receptor-alpha contains two transactivation functions, a weak constitutive activation function (AF-1) and a hormone-dependent activation function (AF-2). AF-2 works by recruiting a large coactivator complex, composed of one or more p160s, CREB-binding protein (CBP)/p300, and P/CAF (p300 and CBP-associated factor), via direct contacts with the p160s. We report here that independent AF-1 activity also requires p160 contacts. Unlike AF-2, which binds signature NR boxes in the center of the p160 molecule, AF-1 binds to sequences near the p160 C terminus. We propose that the ability of AF-1 and AF-2 to interact with separate surfaces of the same coactivator is important for the ability of these transactivation functions to synergize.
Webb
P
P
Metabolic Research Unit, University of California School of Medicine, San Francisco 94143-0540, USA.
Nguyen
P
P
Shinsako
J
J
Anderson
C
C
Feng
W
W
Nguyen
M P
MP
Chen
D
D
Huang
S M
SM
Subramanian
S
S
McKinerney
E
E
Katzenellenbogen
B S
BS
Stallcup
M R
MR
Kushner
P J
PJ
D000123:Acetyltransferases / Q000235:genetics / Q000378:metabolism; D001665:Binding Sites; D050882:CREB-Binding Protein; D018797:Cell Cycle Proteins / Q000235:genetics / Q000378:metabolism; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D006367:HeLa Cells / Q000187:drug effects / Q000378:metabolism; D051548:Histone Acetyltransferases; D006801:Humans; D009687:Nuclear Proteins / Q000235:genetics / Q000378:metabolism; D056920:Nuclear Receptor Coactivator 1; D051958:Nuclear Receptor Coactivator 2; D056921:Nuclear Receptor Coactivator 3; D010446:Peptide Fragments / Q000235:genetics / Q000378:metabolism; D011960:Receptors, Estrogen / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000235:genetics / Q000378:metabolism; D013629:Tamoxifen / Q000494:pharmacology; D015534:Trans-Activators / Q000235:genetics / Q000378:metabolism*; D014157:Transcription Factors / Q000235:genetics / Q000378:metabolism*; D050880:p300-CBP Transcription Factors; D000099224:p300-CBP-Associated Factor
D000123:Acetyltransferases; D050882:CREB-Binding Protein; D018797:Cell Cycle Proteins; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D051548:Histone Acetyltransferases; D009687:Nuclear Proteins; D056920:Nuclear Receptor Coactivator 1; D051958:Nuclear Receptor Coactivator 2; D056921:Nuclear Receptor Coactivator 3; D010446:Peptide Fragments; D011960:Receptors, Estrogen; D011994:Recombinant Proteins; D013629:Tamoxifen; D015534:Trans-Activators; D014157:Transcription Factors; D050880:p300-CBP Transcription Factors; D000099224:p300-CBP-Associated Factor; C498001:NCOA2 protein, human; C494363:CREBBP protein, human; C538859:NCOA1 protein, human; C538866:NCOA3 protein, human