The DOI matches its Crossref record; 59 of the 59 references it cites were found in a registry or an index.
Regulation of the androgen receptor by SET9-mediated methylation.
Open accessAbstract
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.
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“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.”
From Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer (2011) · cites this paper as [65]
In the citing paper
“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.”
From Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer (2011) · cites this paper as [65]
In the citing paper
“The histone methyltransferase SET-domain containing protein-9 (SET9) was very recently identified as a novel coregulator of the AR (65).”
From Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer (2011) · cites this paper as [65]
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Cites
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Stapled histone H3 tails are super-substrates for lysine methyltransferase SETD7
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Metadata
- 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
- ORCID
- Venue
- Nucleic Acids Research
- Publisher
- Oxford University Press (OUP)
- Published
- 2010-10-19
- Volume
- 39
- Issue
- 4
- Pages
- 1266-1279
- ISSN
- 0305-1048 (ISSN-L)
- 1362-4962
- PMC
- PMC3045589
- 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
- gold
- doi.org
- Licence
- 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
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › 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
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