Literature DB >> 17552510

Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.

Guozhi Tang1, Ke Ding, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Su Qiu, Sanjeev Shangary, Renxiao Wang, Jie Guo, Wei Gao, Jennifer Meagher, Jeanne Stuckey, Krzysztof Krajewski, Sheng Jiang, Peter P Roller, Shaomeng Wang.   

Abstract

Structure-based strategy was employed to design flavonoid compounds to mimic the Bim BH3 peptide as a new class of inhibitors of the anti-apoptotic Bcl-2 proteins. The most potent compound, 4 (BI-33), binds to Bcl-2 and Mcl-1 with Ki values of 17 and 18 nM, respectively. Compound 4 inhibits cell growth in the MDA-MB-231 breast cancer cell line with an IC50 value of 110 nM and effectively induces apoptosis.

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Year:  2007        PMID： 17552510      PMCID： PMC2527594          DOI： 10.1021/jm070383c

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  20 in total

1.  Hierarchical regulation of mitochondrion-dependent apoptosis by BCL-2 subfamilies.

Authors:  Hyungjin Kim; Mubina Rafiuddin-Shah; Ho-Chou Tu; John R Jeffers; Gerard P Zambetti; James J-D Hsieh; Emily H-Y Cheng
Journal:  Nat Cell Biol       Date:  2006-11-19       Impact factor: 28.824

2.  Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.

Authors:  Guoping Wang; Zaneta Nikolovska-Coleska; Chao-Yie Yang; Renxiao Wang; Guozhi Tang; Jie Guo; Sanjeev Shangary; Su Qiu; Wei Gao; Dajun Yang; Jennifer Meagher; Jeanne Stuckey; Krzysztof Krajewski; Sheng Jiang; Peter P Roller; Hatice Ozel Abaan; York Tomita; Shaomeng Wang
Journal:  J Med Chem       Date:  2006-10-19       Impact factor: 7.446

3.  The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized.

Authors:  Mark F van Delft; Andrew H Wei; Kylie D Mason; Cassandra J Vandenberg; Lin Chen; Peter E Czabotar; Simon N Willis; Clare L Scott; Catherine L Day; Suzanne Cory; Jerry M Adams; Andrew W Roberts; David C S Huang
Journal:  Cancer Cell       Date:  2006-11       Impact factor: 31.743

4.  Structural insights into the degradation of Mcl-1 induced by BH3 domains.

Authors:  Peter E Czabotar; Erinna F Lee; Mark F van Delft; Catherine L Day; Brian J Smith; David C S Huang; W Douglas Fairlie; Mark G Hinds; Peter M Colman
Journal:  Proc Natl Acad Sci U S A       Date:  2007-03-27       Impact factor: 11.205

5.  Apoptosis initiated when BH3 ligands engage multiple Bcl-2 homologs, not Bax or Bak.

Authors:  Simon N Willis; Jamie I Fletcher; Thomas Kaufmann; Mark F van Delft; Lin Chen; Peter E Czabotar; Helen Ierino; Erinna F Lee; W Douglas Fairlie; Philippe Bouillet; Andreas Strasser; Ruth M Kluck; Jerry M Adams; David C S Huang
Journal:  Science       Date:  2007-02-09       Impact factor: 47.728

Review 6.  Recent progress on the regulation of apoptosis by Bcl-2 family members.

Authors:  A J Minn; R E Swain; A Ma; C B Thompson
Journal:  Adv Immunol       Date:  1998       Impact factor: 3.543

Review 7.  BCL-2 family: regulators of cell death.

Authors:  D T Chao; S J Korsmeyer
Journal:  Annu Rev Immunol       Date:  1998       Impact factor: 28.527

Review 8.  Bcl-2 family proteins: strategies for overcoming chemoresistance in cancer.

Authors:  J C Reed
Journal:  Adv Pharmacol       Date:  1997

9.  An inhibitor of Bcl-2 family proteins induces regression of solid tumours.

Authors:  Tilman Oltersdorf; Steven W Elmore; Alexander R Shoemaker; Robert C Armstrong; David J Augeri; Barbara A Belli; Milan Bruncko; Thomas L Deckwerth; Jurgen Dinges; Philip J Hajduk; Mary K Joseph; Shinichi Kitada; Stanley J Korsmeyer; Aaron R Kunzer; Anthony Letai; Chi Li; Michael J Mitten; David G Nettesheim; ShiChung Ng; Paul M Nimmer; Jacqueline M O'Connor; Anatol Oleksijew; Andrew M Petros; John C Reed; Wang Shen; Stephen K Tahir; Craig B Thompson; Kevin J Tomaselli; Baole Wang; Michael D Wendt; Haichao Zhang; Stephen W Fesik; Saul H Rosenberg
Journal:  Nature       Date:  2005-05-15       Impact factor: 49.962

10.  Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis.

Authors:  Andrew M Petros; Jurgen Dinges; David J Augeri; Steven A Baumeister; David A Betebenner; Mark G Bures; Steven W Elmore; Philip J Hajduk; Mary K Joseph; Shelley K Landis; David G Nettesheim; Saul H Rosenberg; Wang Shen; Sheela Thomas; Xilu Wang; Irini Zanze; Haichao Zhang; Stephen W Fesik
Journal:  J Med Chem       Date:  2006-01-26       Impact factor: 7.446
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  11 in total

1.  Anti-AIDS agents 79. Design, synthesis, molecular modeling and structure-activity relationships of novel dicamphanoyl-2',2'-dimethyldihydropyranochromone (DCP) analogs as potent anti-HIV agents.

Authors:  Ting Zhou; Qian Shi; Chin-Ho Chen; Hao Zhu; Li Huang; Phong Ho; Kuo-Hsiung Lee
Journal:  Bioorg Med Chem       Date:  2010-08-02       Impact factor: 3.641

2.  Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.

Authors:  Jun Wei; Shinichi Kitada; John L Stebbins; William Placzek; Dayong Zhai; Bainan Wu; Michele F Rega; Ziming Zhang; Jason Cellitti; Li Yang; Russell Dahl; John C Reed; Maurizio Pellecchia
Journal:  J Med Chem       Date:  2010-10-29       Impact factor: 7.446

3.  Development of dimeric modulators for anti-apoptotic Bcl-2 proteins.

Authors:  Liangyou Wang; Fansen Kong; Candis L Kokoski; David W Andrews; Chengguo Xing
Journal:  Bioorg Med Chem Lett       Date:  2007-10-30       Impact factor: 2.823

4.  A dual-readout F2 assay that combines fluorescence resonance energy transfer and fluorescence polarization for monitoring bimolecular interactions.

Authors:  Yuhong Du; Zaneta Nikolovska-Coleska; Min Qui; Lian Li; Iestyn Lewis; Raymond Dingledine; Jeanne A Stuckey; Krzysztof Krajewski; Peter P Roller; Shaomeng Wang; Haian Fu
Journal:  Assay Drug Dev Technol       Date:  2011-03-11       Impact factor: 1.738

5.  Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins.

Authors:  Yuzhi Lu; Shuangchan Wu; Yuan Yue; Si He; Jun Li; Jun Tang; Wei Wang; Hai-Bing Zhou
Journal:  ACS Med Chem Lett       Date:  2016-10-19       Impact factor: 4.345

6.  Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression.

Authors:  Jianfang Chen; Haibin Zhou; Angelo Aguilar; Liu Liu; Longchuan Bai; Donna McEachern; Chao-Yie Yang; Jennifer L Meagher; Jeanne A Stuckey; Shaomeng Wang
Journal:  J Med Chem       Date:  2012-10-02       Impact factor: 7.446

7.  4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors.

Authors:  Patrick T Weiser; Ching-Yi Chang; Donald P McDonnell; Robert N Hanson
Journal:  Bioorg Med Chem       Date:  2013-11-08       Impact factor: 3.641

Review 8.  BH3-only proteins in apoptosis and beyond: an overview.

Authors:  E Lomonosova; G Chinnadurai
Journal:  Oncogene       Date:  2008-12       Impact factor: 9.867

9.  WL-276, an antagonist against Bcl-2 proteins, overcomes drug resistance and suppresses prostate tumor growth.

Authors:  Liangyou Wang; Daniel T Sloper; Sadiya N Addo; Defeng Tian; Joel W Slaton; Chengguo Xing
Journal:  Cancer Res       Date:  2008-06-01       Impact factor: 12.701

10.  Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.

Authors:  Jun Wei; Shinichi Kitada; Michele F Rega; John L Stebbins; Dayong Zhai; Jason Cellitti; Hongbin Yuan; Aras Emdadi; Russell Dahl; Ziming Zhang; Li Yang; John C Reed; Maurizio Pellecchia
Journal:  J Med Chem       Date:  2009-07-23       Impact factor: 7.446
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