342 609

Cited 47 times in

Procyanidin B3, an inhibitor of histone acetyltransferase, enhances the action of antagonist for prostate cancer cells via inhibition of p300-dependent acetylation of androgen receptor

Authors
 Kyung-Chul CHOI  ;  SiYong PARK  ;  Beom Jin LIM  ;  Ah-Reum SUNG  ;  Yoo-Hyun LEE  ;  Masaki SHIOTA  ;  Akira YOKOMIZO  ;  Seiji NAITO  ;  Younghwa NA  ;  Ho-Geun YOON 
Citation
 BIOCHEMICAL JOURNAL, Vol.433(1) : 235-244, 2011 
Journal Title
BIOCHEMICAL JOURNAL
ISSN
 0264-6021 
Issue Date
2011
Keywords
acetylation ; androgen receptor ; histone acetyltransferase ; procyanidin b3 ; prostate cancer
Abstract
Increasing evidence suggests that AR (androgen receptor) acetylation is critical for prostate cancer cell growth. In the present study, we identified Pro-B3 (procyanidin B3) as a specific HAT (histone acetyltransferase) inhibitor. Pro-B3 selectively inhibited the activity of HATs, but not other epigenetic enzymes. Pro-B3 substantially inhibited the p300-mediated AR acetylation, both in vitro and in vivo. Pro-B3 inhibited both p300-dependent and agonist-induced AR transcription. We demonstrate that the p300-mediated AR acetylation is critical for the hormone responsiveness of AR. Interestingly, B3 treatment efficiently enhanced the antagonist activity of flutamide through suppression of p300 HAT activity, demonstrating that relative p300 activity is critical for the antagonist action. Finally, Pro-B3 treatment inhibited acetylation-dependent prostate cell proliferation and expression of cell-cycle control genes, subsequently increasing cell death, indicating the functional importance of AR acetylation for prostate cancer cell growth.
Files in This Item:
T201003794.pdf Download
DOI
10.1042/BJ20100980
Appears in Collections:
1. College of Medicine (의과대학) > BioMedical Science Institute (의생명과학부) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Biochemistry and Molecular Biology (생화학-분자생물학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Pathology (병리학교실) > 1. Journal Papers
Yonsei Authors
Yoon, Ho Geun(윤호근) ORCID logo https://orcid.org/0000-0003-2718-3372
Lim, Beom Jin(임범진) ORCID logo https://orcid.org/0000-0003-2856-0133
Choi, Kyung Chul(최경철)
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/92531
사서에게 알리기
  feedback

qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

Browse

Links