Ligand Binding to the Androgen Receptor Induces Conformational Changes That Regulate Phosphatase Interactions

Yang, Chun-Song; Xin, Hong-Wu; Kelley, Joshua B.; Spencer, Adam; Brautigan, David L.; Paschal, Bryce M.

doi:10.1128/mcb.02411-06

Cited by 55Prostate Cancer Treatment and ResearchEstrogen and related hormone effectsSperm and Testicular Function

Ligand Binding to the Androgen Receptor Induces Conformational Changes That Regulate Phosphatase Interactions

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Yang, Chun-Song, Xin, Hong-Wu, Kelley, Joshua B., Spencer, Adam, Brautigan, David L., Paschal, Bryce M.·2007·Molecular and Cellular Biology

DOI 10.1128/mcb.02411-06PMC PMC1899975

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Abstract

We describe a mechanism for protein phosphatase 2A (PP2A) targeting to the androgen receptor (AR) and provide insight into the more general issue of kinase and phosphatase interactions with AR. Simian virus 40 (SV40) small t antigen (ST) binding to N-terminal HEAT repeats in the PP2A A subunit induces structural changes transduced to C-terminal HEAT repeats. This enables the C-terminal HEAT repeats in the PP2A A subunit, including HEAT repeat 13, to discriminate between androgen- and androgen antagonist-induced AR conformations. The PP2A-AR interaction was used to show that an AR mutant in prostate cancer cells (T877A) is activated by multiple ligands without acquiring the same conformation as that induced by androgen. The correlation between androgen binding to AR and increased phosphorylation of the activation function 1 (AF-1) region implies that changes in AR conformation or chaperone composition are causal to kinase access to phosphorylation sites. However, AF-1 phosphorylation sites are kinase accessible prior to androgen binding. This suggests that androgens can enhance the phosphorylation state of AR either by negatively regulating the ability of the ligand-binding domain to bind phosphatases or by inducing an AR conformation that is resistant to phosphatase action. SV40 ST subverts this mechanism by promoting the direct transfer of PP2A onto androgen-bound AR, resulting in multisite dephosphorylation.

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The AR-PP2A interaction is strictly dependent on the agonist conformation of AR.
“the AR-PP2A interaction, which is strictly dependent on the agonist conformation of AR (35).”
From FKBP51 Promotes Assembly of the Hsp90 Chaperone Complex and Regulates Androgen Receptor Signaling in Prostate Cancer Cells (2010) · cites this paper as [35]
In the presence of SV40 small t antigen, PP2A undergoes highly selective loading onto androgen-bound AR.
“In the presence of SV40 small t antigen, protein phosphatase 2A (PP2A) undergoes highly selective loading onto androgen-bound AR (35).”
From FKBP51 Promotes Assembly of the Hsp90 Chaperone Complex and Regulates Androgen Receptor Signaling in Prostate Cancer Cells (2010) · cites this paper as [35]
The PP2A-AR interaction assay discriminates between androgen-free and androgen-bound forms of AR.
“a quantitative coimmunoprecipitation assay developed in our laboratory (35) that discriminates between androgen-free and androgen-bound forms of AR”
From FKBP51 Promotes Assembly of the Hsp90 Chaperone Complex and Regulates Androgen Receptor Signaling in Prostate Cancer Cells (2010) · cites this paper as [35]

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Authors: Yang, C.-S., Xin, H.-W., Kelley, J. B., Spencer, A., Brautigan, D. L., & Paschal, B. M.
Affiliations: Center for Cell Signaling
University of Virginia (US)
ORCID: Xin, Hong-Wu
Kelley, Joshua B.
Spencer, Adam
Brautigan, David L.
Paschal, Bryce M.
Venue: Molecular and Cellular Biology
Publisher: Informa UK Limited
Published: 2007-05-01
Volume: 27
Issue: 9
Pages: 3390-3404
ISSN: 0270-7306 (ISSN-L)
1098-5549
DOI: 10.1128/mcb.02411-06
PMC: PMC1899975
OpenAlex: W2134011929
Cited by: 55
References: 54
Citations by year: 2024: 3 · 2023: 3 · 2022: 3 · 2021: 1 · 2020: 3 · 2019: 2 · 2018: 1 · 2017: 4 · 2016: 2 · 2015: 5 · 2014: 3 · 2013: 3 · 2012: 3
FWCI: 4.63
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: journals.asm.org/non-commercial-tdm-license (tdm)
Locations: Molecular and Cellular Biology (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: Northwestern University
National Institutes of Health
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Health Sciences › Medicine › Reproductive Medicine › Sperm and Testicular Function
Keywords: androgen receptor, protein phosphatase 2A, ligand binding, receptor conformation, HEAT repeats, SV40 small t antigen, androgen antagonists, dephosphorylation, prostate cancer
MeSH terms: Androgens, Animals, Cell Line, Chlorocebus aethiops, Humans, Ligands, Male, Phosphoprotein Phosphatases, Phosphorylation, Prostatic Neoplasms, Protein Binding, Receptors, Androgen, Transcription, Genetic, Transplantation, Heterologous, Response Elements, Amino Acid Motifs, Protein Subunits, Mice, Protein Phosphatase 2

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Ligand Binding to the Androgen Receptor Induces Conformational Changes That Regulate Phosphatase Interactions

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