Bromodomains

Supporting information

Bromodomains (BRDs) are epigenetic "readers" that selectively recognize acetylated lysine (Kac) residues on histone protein tails, and are the only known protein modules that target Kac residues. There are approximately 62 unique human bromodomains, most of which can be classified according to sequence identity into nine groups.

Bromodomains are found in a wide range of proteins, from the histone acetyltransferase PCAF to the ATP-dependent helicase SNF2L2. This diversity makes it difficult to characterize the function of a given BRD-containing protein, particularly as some proteins may contain one or more additional epigenetic "reader" domains. However, some bromodomains have been implicated in diseases such as cancer and inflammation.

Of particular interest is the BET (bromodomain and extra-terminal) bromodomain family, which comprises the ubiquitously expressed proteins BRD2, BRD3, BRD4; and the testis-specific protein, BRDT. Due to the binding of BRD4 to transcriptional sites of genes expressed during the M/G1 cell cycle transition, BRD4 is currently under investigation as a therapeutic target for cancer. BRD4 has also been implicated in a rare but lethal form of cancer - NUT midline carcinoma (NUC) - which is caused by a rearrangement of the nuclear protein in testis gene (NUT), causing the formation of a BRD4-NUT fusion gene. In addition, BRD4 has been reported to function as a coactivator for the transcriptional activation of NFκB.

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
BRD2 Human BRD2 NM_001113182 P25440
Mouse Brd2 NM_001204973 Q7JJ13
Rat Brd2 NM_212495 Q6MGA9
BRD3 Human BRD3 NM_007371 Q15059
Mouse Brd3 NM_023336 Q8K2F0
Rat Brd3 NM_001108575 NP_001102045
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Literature for Bromodomains

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
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Cancer Research Product Guide
Epigenetics Scientific Review

This review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

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Epigenetics Scientific Review
Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
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Epigenetics Research Bulletin research bulletin

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Cancer Research Product Guide

Cancer Research Product Guide

Our Cancer Research Guide highlights over 750 products for cancer research. Request copy or view PDF today.

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Epigenetics Toolbox

80 Epigenetic modulators supplied pre-dissolved in DMSO

Tocriscreen Epigenetics Toolbox

Includes many of the latest compounds available for epigenetics research. Covers a wide range of targets, such as bromodomains, KMTs, PRMTs and HDACs.

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Epigenetics Review

Written by S. Müller-Knapp & P. Brown

Epigenetics Scientific Review

Our Epigenetics review gives an overview of the development of chemical probes for epigenetic targets, and discusses their biological effects. Request copy or view PDF today.

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Epigenetics Research Bulletin

The epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets. View PDF today.

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