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.
Metabolic Research Unit, University of California School of Medicine, San Francisco 94143-0540, USA.
P
P
Webb
P
P
Nguyen
J
J
Shinsako
C
C
Anderson
W
W
Feng
M P
MP
Nguyen
D
D
Chen
S M
SM
Huang
S
S
Subramanian
E
E
McKinerney
B S
BS
Katzenellenbogen
M R
MR
Stallcup
P J
PJ
Kushner
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