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This version published online on April 30, 2009
Molecular Endocrinology, doi:10.1210/me.2009-0131
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Submitted on March 19, 2009
Accepted on April 24, 2009

Role of Protein Methylation and Demethylation in Nuclear Hormone Signaling

Susan C. Wu and Yi Zhang*

Howard Hughes Medical Institute, Department of Biochemistry and Biophysics, Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599-7295

* To whom correspondence should be addressed. E-mail: yi_zhang{at}med.unc.edu.

Nuclear receptors (NRs) are transcription factors responsible for mediating the biological effects of hormones during development, metabolism, and homeostasis. Induction of NR target genes is accomplished through the assembly of hormone-bound NRs complexes at target promoters and coincides with changes in histone modifications that promote transcription. Some coactivators and corepressors of NR can enhance or inhibit NR function by covalently modifying histones. One such modification is methylation, which plays important roles in transcriptional regulation. Histone methylation is catalyzed by histone methyltransferases and reversed by histone demethylases. Recent studies have uncovered the importance of these enzymes in the regulation of NR target genes. In addition to histones, these enzymes have non-histone substrates and can methylate and demethylate NRs and coregulatory proteins in order to modulate their function. This review discusses recent progress in our understanding of the role of methylation and demethylation of histones, NRs, and their coregulators in NR mediated transcription.


Key words: histones • methylation • demethylation • nuclear hormone receptors • transcription

NURSA Molecule Pages Link:

Nuclear Receptors:   RARα  |  PPARγ  |  LXRβ  |  LXRα  |  RXRγ  |  ERα  |  ERβ  |  GR  |  PR  |  AR
Coregulators:   RIP140  |  PGC-1  |  CARM1  |  CBP  |  p300  |  REA  |  HDAC1  |  HDAC3  |  PRMT1  |  SRC-1  |  GRIP1  |  AIB1
Ligands:   17β-Estradiol  |  R1881






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