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Cited by 310

The DOI matches its Crossref record; 40 of the 40 references it cites were found in a registry or an index.

Tip60 and Histone Deacetylase 1 Regulate Androgen Receptor Activity through Changes to the Acetylation Status of the Receptor

Open access
Gaughan, Luke, Logan, Ian R., Cook, Susan, Neal, David E., Robson, Craig N.·2002·Journal of Biological Chemistry

Abstract

The androgen receptor (AR), a member of the nuclear hormone receptor superfamily, is thought to play an important role in the development of prostate cancer. The AR is a hormone-dependent transcription factor that activates expression of numerous androgen-responsive genes. Histone acetyltransferase-containing proteins have been shown to increase activity of several transcription factors, including nuclear hormone receptors, by eliciting histone acetylation, which facilitates promoter access to the transcriptional machinery. Conversely, histone deacetylases (HDACs) have been identified which reduce levels of histone acetylation and are associated with transcriptional repression by various transcription factors. We have previously shown that Tip60 (Tat-interactive protein, 60 kDa) is a bona fide co-activator protein for the AR. Here we show that Tip60 directly acetylates the AR, which we demonstrate is a requisite for Tip60-mediated transcription. To define a mechanism for repression of AR function, we demonstrate that AR activity is specifically down-regulated by the histone deacetylase activity of HDAC1. Furthermore, using both mammalian two-hybrid and immunoprecipitation experiments, we show that AR and HDAC1 interact, suggestive of a direct role for down-regulation of AR activity by HDAC1. In chromatin immunoprecipitation assays, we provide evidence that AR, Tip60, and HDAC1 form a trimeric complex upon the endogenous AR-responsive PSA promoter, suggesting that acetylation and deacetylation of the AR is an important mechanism for regulating transcriptional activity.

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Metadata

Authors
Gaughan, L., Logan, I. R., Cook, S., Neal, D. E., & Robson, C. N.
Venue
Journal of Biological Chemistry
Publisher
Elsevier BV
Published
2002-07
Volume
277
Issue
29
Pages
25904-25913
ISSN
0021-9258 (ISSN-L)
OpenAlex
W1991995900
Cited by
310
References
40
FWCI
4.75
Type
journal article
Language
en
Open access
hybrid

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CoChat. (2026). Citation check: Tip60 and Histone Deacetylase 1 Regulate Androgen Receptor Activity through Changes to the Acetylation Status of the Receptor. https://app.cochat.ai/papers/10.1074/jbc.m203423200
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Gaughan, L., Logan, I. R., Cook, S., Neal, D. E., & Robson, C. N. (2002). Tip60 and Histone Deacetylase 1 Regulate Androgen Receptor Activity through Changes to the Acetylation Status of the Receptor. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m203423200

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