TY - JOUR
T1 - Activation Functions 1 and 2 of Nuclear Receptors
T2 - Molecular Strategies for Transcriptional Activation
AU - Wärnmark, Anette
AU - Treuter, Eckardt
AU - Wright, Anthony P.H.
AU - Gustafsson, Jan Åke
N1 - Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.
PY - 2003/10/1
Y1 - 2003/10/1
N2 - Nuclear receptors (NRs) comprise a family of ligand inducible transcription factors. To achieve transcriptional activation of target genes, DNA-bound NRs directly recruit general transcription factors (GTFs) to the preinitiation complex or bind intermediary factors, so-called coactivators. These coactivators often constitute subunits of larger multiprotein complexes that act at several functional levels, such as chromatin remodeling, enzymatic modification of histone tails, or modulation of the preinitiation complex via interactions with RNA polymerase II and GTFs. The binding of NR to coactivators is often mediated through one of its activation domains. Many NRs have at least two activation domains, the ligand-independent activation function (AF)-1, which resides in the N-terminal domain, and the ligand-dependent AF-2, which is localized in the C-terminal domain. In this review, we summarize and discuss current knowledge regarding the molecular mechanisms of AF-1- and AF-2-mediated gene activation, focusing on AF-1 and AF-2 conformation and coactivator binding.
AB - Nuclear receptors (NRs) comprise a family of ligand inducible transcription factors. To achieve transcriptional activation of target genes, DNA-bound NRs directly recruit general transcription factors (GTFs) to the preinitiation complex or bind intermediary factors, so-called coactivators. These coactivators often constitute subunits of larger multiprotein complexes that act at several functional levels, such as chromatin remodeling, enzymatic modification of histone tails, or modulation of the preinitiation complex via interactions with RNA polymerase II and GTFs. The binding of NR to coactivators is often mediated through one of its activation domains. Many NRs have at least two activation domains, the ligand-independent activation function (AF)-1, which resides in the N-terminal domain, and the ligand-dependent AF-2, which is localized in the C-terminal domain. In this review, we summarize and discuss current knowledge regarding the molecular mechanisms of AF-1- and AF-2-mediated gene activation, focusing on AF-1 and AF-2 conformation and coactivator binding.
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U2 - 10.1210/me.2002-0384
DO - 10.1210/me.2002-0384
M3 - Short survey
C2 - 12893880
AN - SCOPUS:0345650665
SN - 0888-8809
VL - 17
SP - 1901
EP - 1909
JO - Molecular Endocrinology
JF - Molecular Endocrinology
IS - 10
ER -