The transcriptional modulator BCL6 as a molecular target for breast cancer therapy.

TitleThe transcriptional modulator BCL6 as a molecular target for breast cancer therapy.
Publication TypeJournal Article
Year of Publication2015
AuthorsWalker SR, Liu S, Xiang M, Nicolais M, Hatzi K, Giannopoulou E, Elemento O, Cerchietti L, Melnick A, Frank DA
JournalOncogene
Volume34
Issue9
Pagination1073-82
Date Published2015 Feb 26
ISSN1476-5594
KeywordsBinding Sites, Cell Line, Tumor, Cell Survival, Chromatin Immunoprecipitation, DNA-Binding Proteins, Drug Synergism, Female, Gene Amplification, High-Throughput Nucleotide Sequencing, Humans, MCF-7 Cells, Molecular Targeted Therapy, Peptidomimetics, Pyrrolidines, RNA, Small Interfering, Signal Transduction, Sulfonamides, Triple Negative Breast Neoplasms
Abstract

Inappropriate expression or activation of transcription factors can drive patterns of gene expression, leading to the malignant behavior of breast cancer cells. We have found that the transcriptional repressor BCL6 is highly expressed in breast cancer cell lines, and its locus is amplified in about half of primary breast cancers. To understand how BCL6 regulates gene expression in breast cancer cells, we used chromatin immunoprecipitation followed by deep sequencing to identify the BCL6 binding sites on a genomic scale. This revealed that BCL6 regulates a unique cohort of genes in breast cancer cell lines compared with B-cell lymphomas. Furthermore, BCL6 expression promotes the survival of breast cancer cells, and targeting BCL6 with a peptidomimetic inhibitor leads to apoptosis of these cells. Finally, combining a BCL6 inhibitor and a signal transducer and activator of transcription3 inhibitor provided enhanced cell killing in triple-negative breast cancer cell lines, suggesting that combination therapy may be particularly useful. Thus, targeting BCL6 alone or in conjunction with other signaling pathways may be a useful therapeutic strategy for treating breast cancer.

DOI10.1038/onc.2014.61
Alternate JournalOncogene
PubMed ID24662818
PubMed Central IDPMC4175367
Grant ListR01 CA104348 / CA / NCI NIH HHS / United States
R01 CA160979 / CA / NCI NIH HHS / United States
R01-CA160979 / CA / NCI NIH HHS / United States
T32 GM007753 / GM / NIGMS NIH HHS / United States