BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure
Priti Anand,Jonathan D. Brown,Charles Y. Lin,Jun Qi,Rongli Zhang,Pedro Calderon Artero,Amer Alaiti,Jace Bullard,Kareem Alazem,Kenneth B. Margulies,Thomas P. Cappola,Madeleine E. Lemieux,Jorge Plutzky,James E. Bradner,Saptarsi M. Haldar +14 more
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TLDR
Integrative transcriptional and epigenomic analyses reveal that BET proteins function mechanistically as pause-release factors critical to expression of genes that are central to HF pathogenesis and relevant to the pathobiology of failing human hearts.About:
This article is published in Cell.The article was published on 2013-08-01 and is currently open access. It has received 347 citations till now. The article focuses on the topics: Bromodomain & Epigenomics.read more
Citations
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Phthalimide conjugation as a strategy for in vivo target protein degradation
Georg E. Winter,Dennis L. Buckley,Joshiawa Paulk,Justin M. Roberts,Amanda Souza,Sirano Dhe-Paganon,James E. Bradner +6 more
TL;DR: In this paper, a chemical strategy that promotes ligand-dependent target protein degradation using as an example the transcriptional coactivator BRD4, a protein critical for cancer cell growth and survival, was devised.
Journal ArticleDOI
Targeting bromodomains: epigenetic readers of lysine acetylation
TL;DR: Recent progress in the development of bromodomain inhibitors is highlighted, and their potential applications in drug discovery are highlighted.
Journal ArticleDOI
The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition
Junwei Shi,Christopher R. Vakoc +1 more
TL;DR: The current understanding of molecular mechanisms that underlie the promising therapeutic effects of BET bromodomain inhibition are reviewed.
Journal ArticleDOI
The dTAG system for immediate and target-specific protein degradation
Behnam Nabet,Justin M. Roberts,Dennis L. Buckley,Dennis L. Buckley,Joshiawa Paulk,Joshiawa Paulk,Shiva Dastjerdi,Annan Yang,Alan L. Leggett,Michael A. Erb,Matthew A. Lawlor,Amanda Souza,Amanda Souza,Thomas G. Scott,Sarah Vittori,Jennifer A. Perry,Jun Qi,Georg E. Winter,Georg E. Winter,Kwok-Kin Wong,Nathanael S. Gray,James E. Bradner,James E. Bradner +22 more
TL;DR: The dTAG system pairs potent heterobifunctional degraders and extensible tagging strategies to achieve immediate and reversible degradation of divergent proteins, facilitating biological investigation and drug target validation in cells and in mice.
Journal ArticleDOI
NF-κB Directs Dynamic Super Enhancer Formation in Inflammation and Atherogenesis
Jonathan D. Brown,Charles Y. Lin,Qiong Duan,Qiong Duan,Gabriel K. Griffin,Alexander J. Federation,Ronald M. Paranal,Steven M. Bair,Gail Newton,Andrew H. Lichtman,Andrew L. Kung,Andrew L. Kung,Tianlun Yang,Hong Wang,Francis W. Luscinskas,Kevin Croce,James E. Bradner,Jorge Plutzky +17 more
TL;DR: A chemical genetic approach reveals a requirement for BET bromodomains in communicating enhancer remodeling to RNA Polymerase II and orchestrating the transition to the inflammatory cell state, demonstrated in activated endothelium and macrophages.
References
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Aravind Subramanian,Pablo Tamayo,Vamsi K. Mootha,Sayan Mukherjee,Benjamin L. Ebert,Michael A. Gillette,Amanda G. Paulovich,Scott L. Pomeroy,Todd R. Golub,Eric S. Lander,Jill P. Mesirov +10 more
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TL;DR: The statistical update brings together the most up-to-date statistics on heart disease, stroke, other vascular diseases, and their risk factors and presents them in its Heart Disease and Stroke Statistical Update.
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