ArticleMethods in molecular biology (Clifton, N.J.)2011
Analysis of interdomain interactions of the androgen receptor.
Article in Methods in molecular biology (Clifton, N.J.), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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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.
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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.
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Who cites it
18 citing papers in PubMed, 35 citations in OpenAlex.
- Endocrine nuclear receptors and long non‑coding RNAs reciprocal regulation in cancer (Review).International journal of oncology · 2024Review
- Characterization of allosteric modulators that disrupt androgen receptor co-activator protein-protein interactions to alter transactivation-Drug leads for metastatic castration resistant prostate cancer.SLAS discovery : advancing life sciences R & D · 2023Article
- N/C Interactions Are Dispensable for Normal In Vivo Functioning of the Androgen Receptor in Male Mice.Endocrinology · 2022Article
- Targeting Nuclear Receptors in Lung Cancer-Novel Therapeutic Prospects.Pharmaceuticals (Basel, Switzerland) · 2022Review
- MAGE-A11 Expression Predicts Patient Prognosis in Head and Neck Squamous Cell Carcinoma.Cancer management and research · 2020Article
- Androgen Receptor Dependence.Advances in experimental medicine and biology · 2019Review
- Current status of androgen receptor-splice variant 7 inhibitor niclosamide in castrate-resistant prostate-cancer.Investigational new drugs · 2018Review
- Inhibition of androgen receptor transactivation function by adenovirus type 12 E1A undermines prostate cancer cell survival.The Prostate · 2018Article
- Androgen Receptor Structure, Function and Biology: From Bench to Bedside.The Clinical biochemist. Reviews · 2016Review
- Androgen receptor: structure, role in prostate cancer and drug discovery.Acta pharmacologica Sinica · 2015Review
- Reporter cell lines to evaluate the selectivity of chemicals for human and zebrafish estrogen and peroxysome proliferator activated γ receptors.Frontiers in neuroscience · 2015Review
- Reporter Cell Lines for the Characterization of the Interactions between Human Nuclear Receptors and Endocrine Disruptors.Frontiers in endocrinology · 2015Review
- Targeting alternative sites on the androgen receptor to treat castration-resistant prostate cancer.International journal of molecular sciences · 2013Review
- A competitive inhibitor that reduces recruitment of androgen receptor to androgen-responsive genes.The Journal of biological chemistry · 2012Article
- Androgen receptor exon 1 mutation causes androgen insensitivity by creating phosphorylation site and inhibiting melanoma antigen-A11 activation of NH2- and carboxyl-terminal interaction-dependent transactivation.The Journal of biological chemistry · 2012Article
- Structural features discriminate androgen receptor N/C terminal and coactivator interactions.Molecular and cellular endocrinology · 2012Review
- Article
- Assays to Interrogate the Ability of Compounds to Inhibit the AF-2 or AF-1 Transactivation Domains of the Androgen Receptor.Assay and drug development technologiesArticle
Corrections and comments
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Authors and funding
1 author at 1 institution in 1 country.
Funding
Abstract
High-affinity binding of testosterone or dihydrotestosterone to the androgen receptor (AR) triggers the androgen-dependent AR NH2- and carboxyl-terminal (N/C) interaction between the AR NH2-terminal FXXLF motif and the activation function 2 (AF2) hydrophobic binding surface in the ligand-binding domain. The functional importance of the AR N/C interaction is supported by naturally occurring loss-of-function AR AF2 mutations where AR retains high-affinity androgen binding but is defective in AR FXXLF motif binding. Ligands with agonist activity in vivo such as testosterone, dihydrotestosterone, and the synthetic anabolic steroids induce the AR N/C interaction and increase AR transcriptional activity in part by slowing the dissociation rate of bound ligand and stabilizing AR against degradation. AR ligand-binding domain competitive antagonists inhibit the agonist-dependent AR N/C interaction. Although the human AR N/C interaction is important for transcriptional activity, it has an inhibitory effect on transcriptional activity from AF2 by competing for p160 coactivator LXXLL motif binding. The primate-specific AR coregulatory protein, melanoma antigen gene protein-A11 (MAGE-A11), modulates the AR N/C interaction through a direct interaction with the AR FXXLF motif. Inhibition of AF2 transcriptional activity by the AR N/C interaction is relieved by AR FXXLF motif binding to the F-box region of MAGE-11. Described here are methods to measure the androgen-dependent AR N/C interdomain interaction and the influence of transcriptional coregulators.
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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.