期刊
PROTEIN SCIENCE
卷 27, 期 11, 页码 1876-1892出版社
WILEY
DOI: 10.1002/pro.3496
关键词
nuclear receptor; ligand binding domain; DNA binding domain; co-regulator; transactivation; transrepression
资金
- American Heart Association [17-POST3366011014GRNT20460124]
- W.M. Keck Foundation
- National Institutes of Health [1F31GM113397-01A1R01DK095750]
- NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES [R01DK095750] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [F31GM113397] Funding Source: NIH RePORTER
Nuclear receptors (NRs) are a family of transcription factors that regulate numerous physiological processes such as metabolism, reproduction, inflammation, as well as the circadian rhythm. NRs sense changes in lipid metabolite levels to drive differential gene expression, producing distinct physiologic effects. This is an allosteric process whereby binding a cognate ligand and specific DNA sequences drives the recruitment of diverse transcriptional co-regulators at chromatin and ultimately transactivation or transrepression of target genes. Dysregulation of NR signaling leads to various malignances, metabolic disorders, and inflammatory disease. Given their important role in physiology and ability to respond to small lipophilic ligands, NRs have emerged as valuable therapeutic targets. Here, we summarize and discuss the recent progress on understanding the complex mechanism of action of NRs, primarily from a structural perspective. Finally, we suggest future studies to improve our understanding of NR signaling and better design drugs by integrating multiple structural and biophysical approaches.
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