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Regulation of MYC expression and differential JQ1 sensitivity in cancer cells
Journal article   Open access   Peer reviewed

Regulation of MYC expression and differential JQ1 sensitivity in cancer cells

Trent Fowler, Payel Ghatak, David H Price, Ronald Conaway, Joan Conaway, Cheng-Ming Chiang, James E Bradner, Ali Shilatifard and Ananda L Roy
PloS one, Vol.9(1), pp.e87003-e87003
2014
DOI: 10.1371/journal.pone.0087003
PMCID: PMC3900694
PMID: 24466310
url
https://doi.org/10.1371/journal.pone.0087003View
Published (Version of record) Open Access

Abstract

High level MYC expression is associated with almost all human cancers. JQ1, a chemical compound that inhibits MYC expression is therapeutically effective in preclinical animal models in midline carcinoma, and Burkitt's lymphoma (BL). Here we show that JQ1 does not inhibit MYC expression to a similar extent in all tumor cells. The BL cells showed a ∼90% decrease in MYC transcription upon treatment with JQ1, however, no corresponding reduction was seen in several non-BL cells. Molecularly, these differences appear due to requirements of Brd4, the most active version of the Positive Transcription Elongation Factor B (P-TEFb) within the Super Elongation Complex (SEC), and transcription factors such as Gdown1, and MED26 and also other unknown cell specific factors. Our study demonstrates that the regulation of high levels of MYC expression in different cancer cells is driven by unique regulatory mechanisms and that such exclusive regulatory signatures in each cancer cells could be employed for targeted therapeutics.
Neoplasms - metabolism Mediator Complex - metabolism Humans RNA Polymerase II - metabolism Promoter Regions, Genetic - genetics Burkitt Lymphoma - pathology Chromatin Immunoprecipitation Gene Expression Regulation, Neoplastic - drug effects Tumor Cells, Cultured Nuclear Proteins - genetics Real-Time Polymerase Chain Reaction Burkitt Lymphoma - drug therapy RNA, Messenger - genetics Burkitt Lymphoma - metabolism Mediator Complex - genetics Nuclear Proteins - metabolism Transcription Factors - genetics Reverse Transcriptase Polymerase Chain Reaction Blotting, Western Neoplasms - drug therapy Azepines - pharmacology Transcription Factors - metabolism Triazoles - pharmacology Proto-Oncogene Proteins c-myc - antagonists & inhibitors RNA Polymerase II - genetics Neoplasms - pathology

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