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Updated: Jun 22, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Allosteric effects govern nuclear receptor action: DNA appears as a player
Hinrich Gronemeyer1, William Bourguet
1Department of Cancer Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC), BP 10142, 67404 Illkirch Cedex, CU de Strasbourg, France. hg@igbmc.fr
DNA can allosterically modulate glucocorticoid receptor activity, revealing a novel regulatory mechanism for nuclear receptors (NRs). This discovery offers new insights into how NRs fine-tune gene networks involved in various physiological processes.
Area of Science:
- Molecular Biology
- Genetics
- Endocrinology
Background:
- Nuclear receptors (NRs) are transcription factors regulating gene networks critical for physiology and disease.
- Dysfunctional NR signaling is implicated in cancer, metabolic disorders, and reproductive issues.
- NRs sense and modulate cellular status via transcriptional and nongenomic effects.
Purpose of the Study:
- To elucidate a novel mechanism of NR regulation.
- To investigate the potential of DNA as an allosteric effector for NRs.
Main Methods:
- Investigated allosteric modulation of nuclear receptor activity.
- Focused on the interaction between DNA and the glucocorticoid receptor.
Main Results:
- Revealed a mechanism where DNA acts as an allosteric effector.
- Demonstrated modulation of glucocorticoid receptor activity by DNA.
Conclusions:
- DNA can allosterically regulate nuclear receptor function, presenting a new paradigm.
- This mechanism may explain how NRs fine-tune target gene networks.
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