The DOI matches its Crossref record; 168 of the 168 references it cites were found in a registry or an index.
Structural Overview of the Nuclear Receptor Superfamily: Insights into Physiology and Therapeutics
Open accessAbstract
As ligand-regulated transcription factors, the nuclear hormone receptors are nearly ideal drug targets, with internal pockets that bind to hydrophobic, drug-like molecules and well-characterized ligand-induced conformational changes that recruit transcriptional coregulators to promoter elements. Yet, due to the multitude of genes under the control of a single receptor, the major challenge has been the identification of ligands with gene-selective actions, impacting disease outcomes through a narrow subset of target genes and not across their entire gene-regulatory repertoire. Here, we summarize the concepts and work to date underlying the development of steroidal and nonsteroidal receptor ligands, including the use of crystal structures, high-throughput screens, and rational design approaches for finding useful therapeutic molecules. Difficulties in finding selective receptor modulators require a more complete understanding of receptor interdomain communications, posttranslational modifications, and receptor-protein interactions that could be exploited for target gene selectivity.
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1 retracted
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Cited by
Lipids and cancer: Emerging roles in pathogenesis, diagnosis and therapeutic intervention
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Molecular mechanism of estrogen–estrogen receptor signaling
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The Androgen Receptor in Health and Disease
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Metadata
- Authors
- Huang, P., Chandra, V., & Rastinejad, F.
- Venue
- Annual Review of Physiology
- Publisher
- Annual Reviews
- Published
- 2010-03-17
- Volume
- 72
- Issue
- 1
- Pages
- 247-272
- ISSN
- 0066-4278 (ISSN-L)
- 1545-1585
- OpenAlex
- W2149044745
- Cited by
- 533
- References
- 168
- FWCI
- 2.78
- Type
- journal article
- Language
- en
- Open access
- green
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- Huang, P., Chandra, V., & Rastinejad, F. (2010). Structural Overview of the Nuclear Receptor Superfamily: Insights into Physiology and Therapeutics. Annual Review of Physiology. https://doi.org/10.1146/annurev-physiol-021909-135917
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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