The ansamycin antibiotic, rifamycin SV, inhibits BCL6 transcriptional repression and forms a complex with the BCL6-BTB/POZ domain

BCL6 is a transcriptional repressor that is over-expressed due to chromosomal translocations, or other abnormalities, in ∼40% of diffuse large B-cell lymphoma. BCL6 interacts with co-repressor, SMRT, and this is essential for its role in lymphomas. Peptide or small molecule inhibitors, which prevent...

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Veröffentlicht in:	PloS one 2014-03, Vol.9 (3), p.e90889
Hauptverfasser:	Evans, Sian E, Goult, Benjamin T, Fairall, Louise, Jamieson, Andrew G, Ko Ferrigno, Paul, Ford, Robert, Schwabe, John W R, Wagner, Simon D
Format:	Artikel
Sprache:	eng
Schlagworte:	Abnormalities Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics Apoptosis B-cell lymphoma Bcl-6 protein Binding sites Biochemistry Biology Cancer Chemistry Chromosome translocations Crystal structure Crystallography, X-Ray DNA-Binding Proteins - antagonists & inhibitors DNA-Binding Proteins - chemistry DNA-Binding Proteins - metabolism Gene expression Gene silencing Genetic aspects HEK293 Cells Humans Inhibitors Life sciences Lymphocytes B Lymphoma Lymphomas Magnetic resonance spectroscopy Materials Science Medical prognosis Medical screening Medicine Models, Molecular Mutation Natural products NMR NMR spectroscopy Nuclear magnetic resonance Nuclear magnetic resonance spectroscopy Nuclear Receptor Co-Repressor 2 - chemistry Nuclear Receptor Co-Repressor 2 - metabolism Peptides Protein Interaction Maps - drug effects Protein Structure, Tertiary Proteins Proto-Oncogene Proteins c-bcl-6 Recruitment Repressor Proteins - antagonists & inhibitors Repressor Proteins - chemistry Repressor Proteins - metabolism Rifabutin Rifabutin - chemistry Rifabutin - pharmacology Rifamycins Rifamycins - chemistry Rifamycins - pharmacology RNA polymerase Spectroscopy Toxicology Transcription (Genetics) Transcription, Genetic - drug effects
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