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Updated: Jun 2, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Control of nuclear receptor activities in metabolism by post-translational modifications
Wahiba Berrabah1, Pierrette Aumercier, Philippe Lefebvre
1Université Lille Nord de France, INSERM, U1011, Lille, France.
Abstract:
Nuclear receptors (NRs) are molecular transducers of endocrine and dietary signals allowing tissues to adapt their transcriptional responses to endogenous or exogenous cues. These signals act in many cases as specific ligands, converting of NRs into transcriptionally active molecules. This on-off mechanism needs, however, to be finely tuned with respect to the tissue environment and adjusted to the organism needs. These subtle adjustments of NR transcriptional activity are brought about by post-translational modifications (PTMs), which can be, in the case of orphan NRs, the sole regulatory mechanism. The role of PTMs, with a more specific focus on phosphorylation, affecting the functions of NR controlling metabolic events is described in this review.
Insights
Nuclear receptors (NRs) regulate cellular responses to endocrine and dietary signals. Post-translational modifications (PTMs), especially phosphorylation, fine-tune NR activity, impacting metabolic events.
Area of Science:
- Biochemistry
- Molecular Biology
- Endocrinology
Background:
- Nuclear receptors (NRs) are crucial for adapting cellular transcription to environmental signals.
- Ligand binding activates NRs, but precise regulation involves complex mechanisms.
- Post-translational modifications (PTMs) offer a sophisticated layer of control over NR function.
Purpose of the Study:
- To review the role of PTMs in regulating NR activity.
- To specifically examine the impact of phosphorylation on metabolic NR function.
Main Methods:
- Literature review focusing on PTMs and NR regulation.
- Analysis of studies investigating phosphorylation of metabolic NRs.
Main Results:
- PTMs, including phosphorylation, are essential for fine-tuning NR transcriptional activity.
- These modifications allow adaptation to tissue-specific and organismal needs.
- Phosphorylation plays a significant role in modulating the function of NRs involved in metabolic control.
Conclusions:
- PTMs are critical regulators of NR function, particularly for metabolic pathways.
- Understanding NR phosphorylation provides insights into metabolic regulation and potential therapeutic targets.
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