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Title: Discovery of a novel B-cell lymphoma 6 (BCL6)–corepressor interaction inhibitor by utilizing structure-based drug design

Authors:
ORCiD logo; ; ; ; ORCiD logo; ORCiD logo; ; ; ; ; ; ; ; ; ; ; ; ;
Publication Date:
Sponsoring Org.:
USDOE Office of Science (SC), Basic Energy Sciences (BES)
OSTI Identifier:
1549649
Grant/Contract Number:  
AC02-05CH11231
Resource Type:
Publisher's Accepted Manuscript
Journal Name:
Bioorganic and Medicinal Chemistry
Additional Journal Information:
Journal Name: Bioorganic and Medicinal Chemistry Journal Volume: 25 Journal Issue: 17; Journal ID: ISSN 0968-0896
Publisher:
Elsevier
Country of Publication:
United Kingdom
Language:
English

Citation Formats

Yasui, Takeshi, Yamamoto, Takeshi, Sakai, Nozomu, Asano, Kouhei, Takai, Takafumi, Yoshitomi, Yayoi, Davis, Melinda, Takagi, Terufumi, Sakamoto, Kotaro, Sogabe, Satoshi, Kamada, Yusuke, Lane, Weston, Snell, Gyorgy, Iwata, Masashi, Goto, Masayuki, Inooka, Hiroshi, Sakamoto, Jun-ichi, Nakada, Yoshihisa, and Imaeda, Yasuhiro. Discovery of a novel B-cell lymphoma 6 (BCL6)–corepressor interaction inhibitor by utilizing structure-based drug design. United Kingdom: N. p., 2017. Web. https://doi.org/10.1016/j.bmc.2017.07.037.
Yasui, Takeshi, Yamamoto, Takeshi, Sakai, Nozomu, Asano, Kouhei, Takai, Takafumi, Yoshitomi, Yayoi, Davis, Melinda, Takagi, Terufumi, Sakamoto, Kotaro, Sogabe, Satoshi, Kamada, Yusuke, Lane, Weston, Snell, Gyorgy, Iwata, Masashi, Goto, Masayuki, Inooka, Hiroshi, Sakamoto, Jun-ichi, Nakada, Yoshihisa, & Imaeda, Yasuhiro. Discovery of a novel B-cell lymphoma 6 (BCL6)–corepressor interaction inhibitor by utilizing structure-based drug design. United Kingdom. https://doi.org/10.1016/j.bmc.2017.07.037
Yasui, Takeshi, Yamamoto, Takeshi, Sakai, Nozomu, Asano, Kouhei, Takai, Takafumi, Yoshitomi, Yayoi, Davis, Melinda, Takagi, Terufumi, Sakamoto, Kotaro, Sogabe, Satoshi, Kamada, Yusuke, Lane, Weston, Snell, Gyorgy, Iwata, Masashi, Goto, Masayuki, Inooka, Hiroshi, Sakamoto, Jun-ichi, Nakada, Yoshihisa, and Imaeda, Yasuhiro. Fri . "Discovery of a novel B-cell lymphoma 6 (BCL6)–corepressor interaction inhibitor by utilizing structure-based drug design". United Kingdom. https://doi.org/10.1016/j.bmc.2017.07.037.
@article{osti_1549649,
title = {Discovery of a novel B-cell lymphoma 6 (BCL6)–corepressor interaction inhibitor by utilizing structure-based drug design},
author = {Yasui, Takeshi and Yamamoto, Takeshi and Sakai, Nozomu and Asano, Kouhei and Takai, Takafumi and Yoshitomi, Yayoi and Davis, Melinda and Takagi, Terufumi and Sakamoto, Kotaro and Sogabe, Satoshi and Kamada, Yusuke and Lane, Weston and Snell, Gyorgy and Iwata, Masashi and Goto, Masayuki and Inooka, Hiroshi and Sakamoto, Jun-ichi and Nakada, Yoshihisa and Imaeda, Yasuhiro},
abstractNote = {},
doi = {10.1016/j.bmc.2017.07.037},
journal = {Bioorganic and Medicinal Chemistry},
number = 17,
volume = 25,
place = {United Kingdom},
year = {2017},
month = {9}
}

Journal Article:
Free Publicly Available Full Text
Publisher's Version of Record
https://doi.org/10.1016/j.bmc.2017.07.037

Citation Metrics:
Cited by: 9 works
Citation information provided by
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Works referenced in this record:

The Ansamycin Antibiotic, Rifamycin SV, Inhibits BCL6 Transcriptional Repression and Forms a Complex with the BCL6-BTB/POZ Domain
journal, March 2014


Roles of BCL6 in normal and transformed germinal center B cells: BCL6 role in GC B cells
journal, April 2012


Discovery of high-affinity BCL6-binding peptide and its structure-activity relationship
journal, January 2017

  • Sakamoto, Kotaro; Sogabe, Satoshi; Kamada, Yusuke
  • Biochemical and Biophysical Research Communications, Vol. 482, Issue 2
  • DOI: 10.1016/j.bbrc.2016.11.060

A peptomimetic inhibitor of BCL6 with potent antilymphoma effects in vitro and in vivo
journal, April 2009


Predicting druggable binding sites at the protein–protein interface
journal, February 2009

  • Fuller, Jonathan C.; Burgoyne, Nicholas J.; Jackson, Richard M.
  • Drug Discovery Today, Vol. 14, Issue 3-4
  • DOI: 10.1016/j.drudis.2008.10.009

Structure of a BCOR Corepressor Peptide in Complex with the BCL6 BTB Domain Dimer
journal, February 2008


The BCL-6 POZ domain and other POZ domains interact with the co-repressors N-CoR and SMRT
journal, October 1998


MolProbity : all-atom structure validation for macromolecular crystallography
journal, December 2009

  • Chen, Vincent B.; Arendall, W. Bryan; Headd, Jeffrey J.
  • Acta Crystallographica Section D Biological Crystallography, Vol. 66, Issue 1
  • DOI: 10.1107/S0907444909042073

Features and development of Coot
journal, March 2010

  • Emsley, P.; Lohkamp, B.; Scott, W. G.
  • Acta Crystallographica Section D Biological Crystallography, Vol. 66, Issue 4
  • DOI: 10.1107/S0907444910007493

Discovery of a B-Cell Lymphoma 6 Protein–Protein Interaction Inhibitor by a Biophysics-Driven Fragment-Based Approach
journal, May 2017


Discovery of Pyrazolo[1,5- a ]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors
journal, May 2017


REFMAC 5 for the refinement of macromolecular crystal structures
journal, March 2011

  • Murshudov, Garib N.; Skubák, Pavol; Lebedev, Andrey A.
  • Acta Crystallographica Section D Biological Crystallography, Vol. 67, Issue 4
  • DOI: 10.1107/S0907444911001314

Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma
journal, August 2016

  • Cardenas, Mariano G.; Yu, Wenbo; Beguelin, Wendy
  • Journal of Clinical Investigation, Vol. 126, Issue 9
  • DOI: 10.1172/JCI85795

Reaching for high-hanging fruit in drug discovery at protein–protein interfaces
journal, December 2007

  • Wells, James A.; McClendon, Christopher L.
  • Nature, Vol. 450, Issue 7172
  • DOI: 10.1038/nature06526

RNA interference targeting Bcl-6 ameliorates experimental autoimmune myasthenia gravis in mice
journal, January 2014


Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry
journal, March 2011

  • Ishikawa, Minoru; Hashimoto, Yuichi
  • Journal of Medicinal Chemistry, Vol. 54, Issue 6
  • DOI: 10.1021/jm101356p

A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo
journal, April 2010


BCL-6 protein is expressed in germinal-center B cells
journal, July 1995


Critical Residues within the BTB Domain of PLZF and Bcl-6 Modulate Interaction with Corepressors
journal, March 2002


The CCP4 suite programs for protein crystallography
journal, September 1994


BCL6 programs lymphoma cells for survival and differentiation through distinct biochemical mechanisms
journal, September 2007


Signals that influence T follicular helper cell differentiation and function
journal, January 2010


MOLREP an Automated Program for Molecular Replacement
journal, December 1997


The solvatochromic comparison method. 3. Hydrogen bonding by some 2-nitroaniline derivatives
journal, May 1976

  • Yokoyama, Tai; Taft, R. W.; Kamlet, Mortimer J.
  • Journal of the American Chemical Society, Vol. 98, Issue 11
  • DOI: 10.1021/ja00427a030

Therapeutic targeting of the BCL6 oncogene for diffuse large B-cell lymphomas
journal, January 2008


Mechanism of SMRT Corepressor Recruitment by the BCL6 BTB Domain
journal, December 2003