ArticleMolecular cancer therapeutics2008
Structural basis for nuclear receptor corepressor recruitment by antagonist-liganded androgen receptor.
Article in Molecular cancer therapeutics, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
29 citing papers in PubMed, 58 citations in OpenAlex.
- A Spatiotemporal Atlas of the Androgen Receptor Proximal Interactome.bioRxiv : the preprint server for biology · 2026Article
- Limitations of Molecular Docking in Predicting the Selectivity of Selective Androgen Receptor Modulators (SARMs): A Comparative Study of YK11 and Ostarine Across Five Nuclear Receptors.International journal of molecular sciences · 2026Article
- Nuclear receptor coregulator interactions: beyond the switch.Genes & development · 2026Review
- Review
- Epigenetic Coregulation of Androgen Receptor Signaling.Advances in experimental medicine and biology · 2022Article
- PARP7 mono-ADP-ribosylates the agonist conformation of the androgen receptor in the nucleus.The Biochemical journal · 2021Article
- Molecular Dynamics of Cobalt Protoporphyrin Antagonism of the Cancer Suppressor REV-ERBβ.Molecules (Basel, Switzerland) · 2021Article
- Interaction between androgen receptor and coregulator SLIRP is regulated by Ack1 tyrosine kinase and androgen.Scientific reports · 2019Article
- Emerging therapeutic agents for genitourinary cancers.Journal of hematology & oncology · 2019Review
- Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models.International journal of cancer · 2019Article
- Selective modulation of the androgen receptor AF2 domain rescues degeneration in spinal bulbar muscular atrophy.Nature medicine · 2018Article
- Binding of bisphenol A, bisphenol AF, and bisphenol S on the androgen receptor: Coregulator recruitment and stimulation of potential interaction sites.Toxicology in vitro : an international journal published in association with BIBRA · 2017Article
- Thyroid hormone receptor sumoylation is required for preadipocyte differentiation and proliferation.The Journal of biological chemistry · 2015Article
- Switching and withdrawing hormonal agents for castration-resistant prostate cancer.Nature reviews. Urology · 2015Review
- Androgen receptor: structure, role in prostate cancer and drug discovery.Acta pharmacologica Sinica · 2015Review
- Review
- Article
- Mechanism of androgen receptor corepression by CKβBP2/CRIF1, a multifunctional transcription factor coregulator expressed in prostate cancer.Molecular and cellular endocrinology · 2014Article
- Androgen receptor epigenetics.Translational andrology and urology · 2013Article
- Bisphenol A affects androgen receptor function via multiple mechanisms.Chemico-biological interactions · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Androgen receptor (AR) recruitment of transcriptional corepressors NCoR and SMRT can be enhanced by antagonists such as mifepristone. This study shows that enhanced NCoR binding to the mifepristone-liganded AR is mediated by the NCoR COOH-terminal N1 CoRNR box and that this selectivity is due to charged residues unique to the COOH-terminal CoRNR boxes of NCoR and SMRT. Significantly, these residues are on a helical face adjacent to oppositely charged residues in helix 4 of the AR ligand-binding domain. Mutagenesis of these AR residues in helix 4, as well as mutation of lysine 720 in helix 3 (predicted to interact with the CoRNR box), markedly impaired AR recruitment of NCoR, indicating that N1 CoRNR box binding is being stabilized by these ionic interactions in the AR ligand-binding domain coactivator/corepressor binding site. Finally, results using a helix 12-deleted AR indicate that mifepristone induces allosteric changes in addition to helix 12 displacement that are critical for NCoR binding. These findings show that AR antagonists can enhance corepressor recruitment by stabilizing a distinct antagonist conformation of the AR coactivator/corepressor binding site and support the development of additional antagonists that may be able to further enhance AR recruitment of corepressors.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.