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Updated: Jul 17, 2026
10:51
Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Modulation of nuclear receptor dependent transcription
1Dept. of Cancer Medicine, Division of Medicine, Faculty of Medicine, Imperial College of Science, Technology & Medicine, Du Cane Road, London W12 0NN, UK. s.hart@ic.ac.uk
Biological Research
|November 6, 2002
Summary
Nuclear receptors are transcription factors regulating gene expression. Aberrant activity of specific nuclear receptors, like estrogen receptor-alpha, is linked to major human cancers.
Area of Science:
- Molecular Biology
- Genetics
- Cancer Biology
Background:
- Nuclear receptors are ligand-dependent transcription factors controlling gene expression.
- They function as homo- or hetero-dimers, binding DNA or interacting with other transcription factors.
- Coactivators and corepressors modulate nuclear receptor activity via chromatin modification.
Purpose of the Study:
- To highlight the critical role of nuclear receptors in gene regulation.
- To establish the association between specific nuclear receptors and human malignancies.
- To provide examples of nuclear receptors implicated in breast cancer, prostate cancer, and leukemia.
Main Methods:
- Review of existing literature on nuclear receptor function.
- Analysis of the mechanisms by which nuclear receptors regulate gene expression.
- Correlation of nuclear receptor activity with the pathogenesis of specific cancers.
Main Results:
- Nuclear receptors directly bind DNA response elements or interact with other transcription factors.
- Complex formation with coactivators/corepressors leads to chromatin remodeling and gene expression changes.
- Estrogen receptor-alpha (ER alpha), androgen receptor (AR), and retinoic acid receptor alpha (RAR alpha) are key players in breast cancer, prostate cancer, and acute promyelocytic leukemia, respectively.
Conclusions:
- Nuclear receptors are central regulators of gene expression with significant implications in human health.
- Dysregulation of specific nuclear receptors is a driving force in the development of several major cancers.
- Targeting these nuclear receptors offers potential therapeutic strategies for cancer treatment.
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