BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc
Jake Delmore,Ghayas C Issa,Madeleine E. Lemieux,Peter B. Rahl,Junwei Shi,Hannah M. Jacobs,Efstathios Kastritis,Timothy Gilpatrick,Ronald M. Paranal,Jun Qi,Marta Chesi,Anna C. Schinzel,Michael R. McKeown,Timothy P. Heffernan,Christopher R. Vakoc,P. Leif Bergsagel,Irene M. Ghobrial,Paul G. Richardson,Richard A. Young,William C. Hahn,William C. Hahn,Kenneth C. Anderson,Andrew L. Kung,James E. Bradner,Constantine S. Mitsiades +24 more
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TLDR
In this paper, a small-molecule bromodomain inhibitor, JQ1, was used to identify BET proteins as regulatory factors for c-Myc oncoprotein.About:
This article is published in Cell.The article was published on 2011-09-16 and is currently open access. It has received 2500 citations till now. The article focuses on the topics: BET inhibitor & Bromodomain.read more
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MYC on the Path to Cancer
TL;DR: The richness of the understanding of MYC is reviewed, highlighting new biological insights and opportunities for cancer therapies.
Journal ArticleDOI
Cancer epigenetics: from mechanism to therapy.
Mark A. Dawson,Tony Kouzarides +1 more
TL;DR: The basic principles behind DNA methylation, histone modification, nucleosome remodeling, and RNA-mediated targeting are presented and the evidence suggesting that their misregulation can culminate in cancer is highlighted.
Journal ArticleDOI
Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers
Jakob Lovén,Heather A. Hoke,Charles Y. Lin,Charles Y. Lin,Ashley Lau,David A. Orlando,Christopher R. Vakoc,James E. Bradner,Tong Ihn Lee,Richard A. Young +9 more
TL;DR: This work investigates how inhibition of the widely expressed transcriptional coactivator BRD4 leads to selective inhibition ofThe MYC oncogene in multiple myeloma (MM), and finds that super-enhancers were found at key oncogenic drivers in many other tumor cells.
Journal ArticleDOI
The PI3K pathway in human disease
David A. Fruman,Honyin Chiu,Benjamin D. Hopkins,Shubha Bagrodia,Lewis C. Cantley,Robert T. Abraham +5 more
TL;DR: A perspective on the roles of class I PI3Ks in the regulation of cellular metabolism and in immune system functions is provided, two topics closely intertwined with cancer biology.
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PI3K and cancer: lessons, challenges and opportunities
David A. Fruman,Christian Rommel +1 more
TL;DR: Through a greater focus on patient selection, increased understanding of immune modulation and strategic application of rational combinations, it should be possible to realize the potential of this promising class of targeted anticancer agents.
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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Conducting Meta-Analyses in R with the metafor Package
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Exploration, normalization, and summaries of high density oligonucleotide array probe level data
Rafael A. Irizarry,Bridget G. Hobbs,Francois Collin,Yasmin Beazer-Barclay,Kristen J. Antonellis,Uwe Scherf,Terence P. Speed +6 more
TL;DR: There is no obvious downside to using RMA and attaching a standard error (SE) to this quantity using a linear model which removes probe-specific affinities, and the exploratory data analyses of the probe level data motivate a new summary measure that is a robust multi-array average (RMA) of background-adjusted, normalized, and log-transformed PM values.
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A comparison of normalization methods for high density oligonucleotide array data based on variance and bias
TL;DR: Three methods of performing normalization at the probe intensity level are presented: a one number scaling based algorithm and a method that uses a non-linear normalizing relation by comparing the variability and bias of an expression measure and the simplest and quickest complete data method is found to perform favorably.
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Adjusting batch effects in microarray expression data using empirical Bayes methods
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