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  A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo

Cerchietti, L. C., Ghetu, A. F., Zhu, X., Da Silva, G. F., Zhong, S., Matthews, M., et al. (2010). A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo. Cancer Cell, 17(4), 400-411. doi:10.1016/j.ccr.2009.12.050.

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 Creators:
Cerchietti , Leandro C.1, 2, Author
Ghetu , Alexandru F.3, Author
Zhu, Xiao4, Author
Da Silva , Gustavo F.5, Author
Zhong, Shijun4, Author
Matthews , Marylin4, Author
Bunting , Karen L.1, 2, Author
Polo, Jose M.5, Author
Farès, Christophe3, Author           
Arrowsmith, Cheryl H.3, 6, Author
Ning Yang, Shao1, 2, Author
Garcia, Monica1, 2, Author
Coop, Andrew4, Author
MacKerell Jr. , Alexander D.4, Author
Privé , Gilbert G.3, 6, 7, Author
Melnick, Ari1, 2, Author
Affiliations:
1Division of Hematology and Medical Oncology, Department of Medicine, Weill Cornell Medical College, Cornell University, New York, NY 10065, USA, ou_persistent22              
2Department of Pharmacology, Weill Cornell Medical College, Cornell University, New York, NY 10065, USA, ou_persistent22              
3Ontario Cancer Institute and Campbell Family Institute for Cancer Research, Toronto, ON M5G 1L7, Canada, ou_persistent22              
4Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USA, ou_persistent22              
5Department of Developmental and Molecular Biology, Albert Einstein College of Medicine, Bronx, NY 10461, USA, ou_persistent22              
6Department of Medical Biophysics, University of Toronto, Toronto, ON M5G 2N9, Canada, ou_persistent22              
7Department of Biochemistry, University of Toronto, Toronto, ON M5S 1A8, Canada, ou_persistent22              

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Free keywords: Cellcycle; Chembio
 Abstract: The BCL6 transcriptional repressor is the most frequently involved oncogene in diffuse large B cell lymphoma (DLBCL). We combined computer-aided drug design with functional assays to identify low-molecular-weight compounds that bind to the corepressor binding groove of the BCL6 BTB domain. One such compound disrupted BCL6/corepressor complexes in vitro and in vivo, and was observed by X-ray crystallography and NMR to bind the critical site within the BTB groove. This compound could induce expression of BCL6 target genes and kill BCL6-positive DLBCL cell lines. In xenotransplantation experiments, the compound was nontoxic and potently suppressed DLBCL tumors in vivo. The compound also killed primary DLBCLs from human patients.

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Language(s): eng - English
 Dates: 2009-03-062010-02-052010-04-122010-04-13
 Publication Status: Published in print
 Pages: 12
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1016/j.ccr.2009.12.050
 Degree: -

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Title: Cancer Cell
  Other : Cancer Cell
Source Genre: Journal
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Publ. Info: Cambridge, Mass. : Cell Press
Pages: - Volume / Issue: 17 (4) Sequence Number: - Start / End Page: 400 - 411 Identifier: ISSN: 1535-6108
CoNE: https://pure.mpg.de/cone/journals/resource/111025129473004