Cited by 128Prostate Cancer Treatment and ResearchCancer-related gene regulationEpigenetics and DNA Methylation

Regulation of the androgen receptor by SET9-mediated methylation.

Open access
Gaughan, Luke, Stockley, Jacqueline, Wang, Nan, McCracken, Stuart R.C., Treumann, Achim, Armstrong, Kelly, Shaheen, Fadhel, Watt, Kate +4 more·2011·Nucleic Acids Research

Abstract

The androgen receptor (AR) is a member of the nuclear hormone receptor family of transcription factors that plays a critical role in regulating expression of genes involved in prostate development and transformation. Upon hormone binding, the AR associates with numerous co-regulator proteins that regulate the activation status of target genes via flux to the post-translational modification status of histones and the receptor. Here we show that the AR interacts with and is directly methylated by the histone methyltransferase enzyme SET9. Methylation of the AR on lysine 632 is necessary for enhancing transcriptional activity of the receptor by facilitating both inter-domain communication between the N- and C-termini and recruitment to androgen-target genes. We also show that SET9 is pro-proliferative and anti-apoptotic in prostate cancer cells and demonstrates up-regulated nuclear expression in prostate cancer tissue. In all, our date indicate a new mechanism of AR regulation that may be therapeutically exploitable for prostate cancer treatment.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Integrity signals

Registry

Crossref · 10.1093/nar/gkq861

Cites

59 of 59 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

  • SET9 methylates the androgen receptor on Lys-632, a modification that facilitates N-C interaction of the receptor and promotes recruitment to AR-regulated genes.

    “SET9 is able to methylate the AR on Lys-632, a modification that facilitates N-C interaction of the receptor and promotes recruitment to AR-regulated genes.”
  • Expression of SET9 is increased in prostate cancer specimens compared with benign prostatic hyperplasia.

    “The expression of SET9 is increased in prostate cancer specimens compared with benign prostatic hyperplasia; however, more work is needed to determine whether increased ex-pression of SET9 is exhibited by CR tumors and whether SET9 can promote transactivation of the AR in the absence of DHT.”
  • SET9 was recently identified as a novel coregulator of the androgen receptor.

    “The histone methyltransferase SET-domain containing protein-9 (SET9) was very recently identified as a novel coregulator of the AR (65).”

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Cites

Flagged first, then by citations

Cited by

Sorted by citations

Authors
Gaughan, L., Stockley, J., Wang, N., McCracken, S. R. C., Treumann, A., Armstrong, K., Shaheen, F., Watt, K., McEwan, I. J., Wang, C., Pestell, R. G., & Robson, C. N.
Affiliations
Thomas Jefferson University (US)
Corresponding author
Gaughan, Luke
Venue
Nucleic Acids Research
Published
2010-10-19
Volume
39
Issue
4
Pages
1266-1279
ISSN
  • 0305-1048 (ISSN-L)
  • 1362-4962
OpenAlex
W2129651872
Cited by
127
References
59
Citations by year
2026: 3 · 2025: 3 · 2024: 3 · 2023: 11 · 2022: 12 · 2021: 6 · 2020: 4 · 2019: 5 · 2018: 10 · 2017: 12 · 2016: 8 · 2015: 7 · 2014: 8 · 2013: 15 · 2012: 10
FWCI
9.34
Type
journal article
Language
en
Open access
Locations
  • Nucleic Acids Research (publishedVersion, cc-by-nc)
  • PubMed Central (publishedVersion, cc-by-nc)
  • PubMed (publishedVersion)
  • The Medicine Forum (submittedVersion)
  • Newcastle University ePrints (Newcastle Univesity) (cc-by-nc)
Funders
  • Cancer Research UK
  • Academy of Medical Sciences (AMS-SGCL4-McCracken)
Topics
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cancer-related gene regulation
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
Keywords
androgen receptor, histone methyltransferase, lysine methylation, receptor regulation, transcriptional activation, prostate cancer, apoptosis, cell proliferation, nuclear receptors
MeSH terms
Cell Nucleus, Histones, Humans, Lysine, Male, Methylation, Prostatic Neoplasms, Histone-Lysine N-Methyltransferase, Receptors, Androgen, Transcriptional Activation, Prostate-Specific Antigen, Active Transport, Cell Nucleus, Cell Line, Tumor, Cell Proliferation

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review