Targeting MYC dependence in cancer by inhibiting BET bromodomains

The MYC transcription factor is a master regulator of diverse cellular functions and has been long considered a compelling therapeutic target because of its role in a range of human malignancies. However, pharmacologic inhibition of MYC function has proven challenging because of both the diverse mec...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 2011-10, Vol.108 (40), p.16669-16674
Hauptverfasser:	Mertz, Jennifer A, Conery, Andrew R, Bryant, Barbara M, Sandy, Peter, Balasubramanian, Srividya, Mele, Deanna A, Bergeron, Louise, Sims, Robert J., III
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals anticarcinogenic activity Apoptosis Apoptosis - genetics Apoptosis - physiology Azepines - pharmacology Betting Biological Sciences Blotting, Western Burkitt Lymphoma - drug therapy Cancer Cell cycle Cell Cycle - physiology Cell Line, Tumor Cell lines Cell Proliferation - drug effects Chromatin Chromatin Immunoprecipitation chromosome translocation DNA-Binding Proteins - antagonists & inhibitors DNA-Binding Proteins - genetics DNA-Binding Proteins - metabolism Dose-Response Relationship, Drug Flow Cytometry Gene expression Gene Expression Profiling Gene Expression Regulation, Neoplastic - drug effects Gene Expression Regulation, Neoplastic - physiology Genes Genetic loci HeLa cells Humans Leukemia, Myeloid, Acute - drug therapy loci lymphoma Messenger RNA Mice Mice, Inbred NOD Mice, SCID myeloid leukemia Polymerase Chain Reaction Protein Structure, Tertiary - genetics Proteins RNA, Small Interfering - genetics transcription (genetics) transcription factors Transcription Factors - antagonists & inhibitors Transcription Factors - genetics Transcription Factors - metabolism transcriptome Triazoles - pharmacology Tumors Viability
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