Pharmacological inhibition of bromodomain-containing proteins in inflammation.

Abstract

Inflammation is associated with the activation of genes that contribute to immune defense and tissue repair. The bromodomain-containing proteins of the BET family, which recognize histone lysine acetylation, play a key role in the transcriptional control of inflammatory genes. Inhibition of BET proteins by the small-molecule inhibitor I-BET affects the expression of a particular subset of inflammatory genes-namely, ones that follow an "analog-like," but not "digital-like" activation pattern. This ability of I-BET to target genes based on the dynamic pattern of their activation may facilitate the further development of anti-inflammatory treatment protocols that are tuned to the individual or to disease-specific patterns of gene expression.

• Authors: Uwe Schaefer
• Journal: Cold Spring Harbor perspectives in biology (Cold Spring Harb Perspect Biol) Vol. 6 Issue 6 (Jun 02 2014) ISSN: 1943-0264 [Electronic] United States
• PMID: 24890512 (Publication Type: Journal Article)
• Copyright: Copyright © 2014 Cold Spring Harbor Laboratory Press; all rights reserved.

Chemical References

• Anti-Inflammatory Agents
• Proteins

Topics

• Anti-Inflammatory Agents (pharmacology)
• Inflammation (drug therapy)
• Proteins (antagonists & inhibitors, chemistry)