Literature DB >> 17034116

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

Guoping Wang1, 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.   

Abstract

A structure-based approach was employed to design a new class of small-molecule inhibitors of Bcl-2. The most potent compound 5 (TW-37) binds to Bcl-2 with a K(i) value of 290 nM and also to Bcl-xL and Mcl-1 with high affinities. Compound 5 potently inhibits cell growth in PC-3 prostate cancer cells with an IC(50) value of 200 nM and effectively induces apoptosis in a dose-dependent manner.

Entities:  

Mesh：

Substances：

Year:  2006        PMID： 17034116     DOI： 10.1021/jm060460o

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


  111 in total

Review 1.  PAR-4 as a possible new target for pancreatic cancer therapy.

Authors:  Asfar S Azmi; Philip A Philip; Syed F Zafar; Fazlul H Sarkar; Ramzi M Mohammad
Journal:  Expert Opin Ther Targets       Date:  2010-06       Impact factor: 6.902

2.  BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.

Authors:  Jun Wei; John L Stebbins; Shinichi Kitada; Rupesh Dash; William Placzek; Michele F Rega; Bainan Wu; Jason Cellitti; Dayong Zhai; Li Yang; Russell Dahl; Paul B Fisher; John C Reed; Maurizio Pellecchia
Journal:  J Med Chem       Date:  2010-05-27       Impact factor: 7.446

3.  Amphipathic tail-anchoring peptide and Bcl-2 homology domain-3 (BH3) peptides from Bcl-2 family proteins induce apoptosis through different mechanisms.

Authors:  Jae-Kyun Ko; Kyoung-Han Choi; Jun Peng; Feng He; Zhi Zhang; Noah Weisleder; Jialing Lin; Jianjie Ma
Journal:  J Biol Chem       Date:  2010-12-28       Impact factor: 5.157

4.  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

5.  Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.

Authors:  Guozhi Tang; Chao-Yie Yang; Zaneta Nikolovska-Coleska; Jie Guo; Su Qiu; Renxiao Wang; Wei Gao; Guoping Wang; Jeanne Stuckey; Krzysztof Krajewski; Sheng Jiang; Peter P Roller; Shaomeng Wang
Journal:  J Med Chem       Date:  2007-03-23       Impact factor: 7.446

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.  Inhibition of proliferation of prostate cancer cell line, PC-3, in vitro and in vivo using (-)-gossypol.

Authors:  Xian-Qing Zhang; Xiao-Feng Huang; Shi-Jie Mu; Qun-Xing An; Ai-Jun Xia; Rui Chen; Dao-Cheng Wu
Journal:  Asian J Androl       Date:  2010-01-18       Impact factor: 3.285

8.  Intracellular delivery of a proapoptotic peptide via conjugation to a RAFT synthesized endosomolytic polymer.

Authors:  Craig L Duvall; Anthony J Convertine; Danielle S W Benoit; Allan S Hoffman; Patrick S Stayton
Journal:  Mol Pharm       Date:  2010-04-05       Impact factor: 4.939

9.  Sabutoclax, a Mcl-1 antagonist, inhibits tumorigenesis in transgenic mouse and human xenograft models of prostate cancer.

Authors:  Roger S Jackson; William Placzek; Ana Fernandez; Shabnam Ziaee; Chia-Yi Chu; Jun Wei; John Stebbins; Shinichi Kitada; Gloria Fritz; John C Reed; Leland W Chung; Maurizio Pellecchia; Neil A Bhowmick
Journal:  Neoplasia       Date:  2012-07       Impact factor: 5.715

10.  B cell lymphoma-2 (BCL-2) homology domain 3 (BH3) mimetics demonstrate differential activities dependent upon the functional repertoire of pro- and anti-apoptotic BCL-2 family proteins.

Authors:  Thibaud T Renault; Rana Elkholi; Archana Bharti; Jerry E Chipuk
Journal:  J Biol Chem       Date:  2014-08-05       Impact factor: 5.157
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.