ESR dimerizes

Stable Identifier
Reaction [transition]
Homo sapiens
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Upon ligand binding, estrogen receptors form homo- or heterodimers mediated by dimerization domains in the DNA-binding and ligand-binding regions (White et al, 1991; Schwabe et al, 1993; Kuntz et al, 1997; Kumar and Chambon, 1998; Powell et al, 2010). Estrogen receptor dimers regulate transcription of estrogen-responsive genes either by direct binding to estrogen response elements (characterized by a palindromic consensus sequence AGGTCA separated by a 3bp spacer) or by interacting with other DNA binding transcriptional regulators (reviewed in Smith and Toft, 2008; Bai and Gust, 2009; Ikeda et al 2015; Liu and Cheung, 2014). Binding of estrogen receptors to the DNA promotes the assembly of higher order transcriptional complexes containing methyltransferases, histone acetyltransferases and other transcriptional activators, which promote transcription by establishing active chromatin marks and by recruiting general transcription factors and RNA polymerase II. ESR1- and estrogen-dependent recruitment of up to hundreds of coregulators has been demonstrated by varied co-immunoprecipitation and proteomic approaches (Kittler et al, 2013; Mohammed et al, 2013; Foulds et al, 2013; Mohammed et al, 2015; Liu et al, 2014; reviewed in Magnani and Lupien, 2014; Arnal, 2017).

Literature References
PubMed ID Title Journal Year
25303530 Enhancer activation requires trans-recruitment of a mega transcription factor complex

Li, W, Friedman, MJ, Krones, A, Yang, F, Rosenfeld, MG, Song, X, Oh, S, Ma, Q, Liu, Z, Merkurjev, D, Zhang, F, Ohgi, KA

Cell 2014
24071518 Estrogen receptor-mediated long-range chromatin interactions and transcription in breast cancer

Liu, MH, Cheung, E

Mol. Cell. Endocrinol. 2014
26153859 Progesterone receptor modulates ERα action in breast cancer

Tarulli, GA, Hadfield, J, Birrell, SN, Perou, CM, Hickey, TE, Serandour, AA, Launchbury, R, Pugh, M, Silva, G, Russell, IA, Bruna, A, Stingl, J, Caldas, C, Raj, GV, D'Santos, C, Saadi, A, Mohammed, H, Rueda, OM, Serandour, AA, Robinson, JL, Tilley, WD, Brown, GD, Stark, R, Menon, S, Carroll, JS

Nature 2015
23403292 Endogenous purification reveals GREB1 as a key estrogen receptor regulatory factor

Ross-Innes, CS, D'Santos, C, Saadi, A, Palmieri, C, Mohammed, H, Atkins, A, Rueda, OM, Chin, SF, Serandour, AA, Holmes, KA, Ali, HR, Robinson, JL, Zwart, W, Stingl, J, Caldas, C, Brown, GD, Menon, S, Carroll, JS, Theodorou, V

Cell Rep 2013
23375374 A comprehensive nuclear receptor network for breast cancer cells

Hua, S, Cheng, C, Zhou, J, White, KP, Pendleton, E, Ma, L, Gerstein, M, Liu, Y, Kittler, R

Cell Rep 2013
25500870 Identification of estrogen-responsive genes based on the DNA binding properties of estrogen receptors using high-throughput sequencing technology

Ikeda, K, Horie-Inoue, K, Inoue, S

Acta Pharmacol. Sin. 2015
18451092 Minireview: the intersection of steroid receptors with molecular chaperones: observations and questions

Toft, DO, Smith, DF

Mol. Endocrinol. 2008
23684889 Chromatin and epigenetic determinants of estrogen receptor alpha (ESR1) signaling

Magnani, L, Lupien, M

Mol. Cell. Endocrinol. 2014
3167974 The estrogen receptor binds tightly to its responsive element as a ligand-induced homodimer

Chambon, P, Kumar, V

Cell 1988
8221895 The crystal structure of the estrogen receptor DNA-binding domain bound to DNA: how receptors discriminate between their response elements

Schwabe, JW, Rhodes, D, Finch, JT, Chapman, L

Cell 1993
1720327 Analysis of oestrogen receptor dimerisation using chimeric proteins

Fawell, SE, Parker, MG, White, R

J. Steroid Biochem. Mol. Biol. 1991
23850489 Proteomic analysis of coregulators bound to ERα on DNA and nucleosomes reveals coregulator dynamics

Tsai, SY, Malovannaya, A, Tsai, MJ, Feng, Q, Qin, J, Gates, LA, O'Malley, BW, Bailey, S, Bajaj, A, Foulds, CE, Callaway, CG, Edwards, DP, Hunsaker, TL, Hamilton, RA, Zhang, Z, Lonard, DM, Chan, D, Ding, C, Li, C

Mol. Cell 2013
19274700 Breast cancer, estrogen receptor and ligands

Bai, Z, Gust, R

Arch. Pharm. (Weinheim) 2009
9346945 Dimerizing the estrogen receptor DNA binding domain enhances binding to estrogen response elements

Kuntz, MA, Shapiro, DJ

J. Biol. Chem. 1997
20353944 Differential requirements of Hsp90 and DNA for the formation of estrogen receptor homodimers and heterodimers

Xu, W, Shapiro, DJ, Powell, E, Wang, Y

J. Biol. Chem. 2010
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