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Cited by 533

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 access
Huang, Pengxiang, Chandra, Vikas, Rastinejad, Fraydoon·2010·Annual Review of Physiology

Abstract

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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Registry

Crossref · 10.1146/annurev-physiol-021909-135917

Cites

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Citations

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Metadata

Authors
Huang, P., Chandra, V., & Rastinejad, F.
Venue
Annual Review of Physiology
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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CoChat. (2026). Citation check: Structural Overview of the Nuclear Receptor Superfamily: Insights into Physiology and Therapeutics. https://app.cochat.ai/papers/10.1146/annurev-physiol-021909-135917
The paper
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

Data sources

Bibliographic data: Semantic Scholar, OpenAlex, Crossref.

Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.