Next Article in Journal
Social Demography of Transitional Dietary Patterns in Thailand: Prospective Evidence from the Thai Cohort Study
Previous Article in Journal
Performance and Health Benefits of Dietary Nitrate Supplementation in Older Adults: A Systematic Review
Article Menu
Issue 11 (November) cover image

Export Article

Open AccessCommunication
Nutrients 2017, 9(11), 1172; doi:10.3390/nu9111172

Dietary Compound Resveratrol Is a Pan-BET Bromodomain Inhibitor

1
School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara 14800903, Brazil
2
Institute for Pharmaceutical Chemistry and Buchmann Institute for Life Sciences, Goethe-University, D-60438 Frankfurt am Main, Germany
*
Authors to whom correspondence should be addressed.
Received: 14 August 2017 / Revised: 17 October 2017 / Accepted: 20 October 2017 / Published: 27 October 2017
View Full-Text   |   Download PDF [1821 KB, uploaded 27 October 2017]   |  

Abstract

The chemopreventive and anticancer effects of resveratrol (RSV) are widely reported in the literature. Specifically, mechanisms involving epigenetic regulation are promising targets to regulate tumor development. Bromodomains act as epigenetic readers by recognizing lysine acetylation on histone tails and boosting gene expression in order to regulate tissue-specific transcription. In this work, we showed that RSV is a pan-BET inhibitor. Using Differential Scanning Fluorimetry (DSF), we showed that RSV at 100 µM increased the melting temperature (∆Tm) of BET bromodomains by around 2.0 °C. The micromolar dissociation constant (Kd) range was characterized using Isothermal Titration Calorimetry (ITC). The RSV Kd value accounted to 6.6 µM in case of BRD4(1). Molecular docking proposed the binding mode of RSV against BRD4(1) mimicking the acetyl-lysine interactions. All these results suggest that RSV can also recognize epigenetic readers domains by interacting with BET bromodomains. View Full-Text
Keywords: resveratrol; bromodomains; epigenetic; Differential Scanning Calorimetry (DSF); Isothermal Titration Calorimetry (ITC) resveratrol; bromodomains; epigenetic; Differential Scanning Calorimetry (DSF); Isothermal Titration Calorimetry (ITC)
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Dutra, L.A.; Heidenreich, D.; Silva, G.D.B.; Man Chin, C.; Knapp, S.; Santos, J.L. Dietary Compound Resveratrol Is a Pan-BET Bromodomain Inhibitor. Nutrients 2017, 9, 1172.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Nutrients EISSN 2072-6643 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top