Literature DB >> 24107192

The making of I-BET762, a BET bromodomain inhibitor now in clinical development.

Yujun Zhao1, Chao-Yie Yang, Shaomeng Wang.   

Abstract

Bromodomain and extra-terminal (BET) proteins belong to a class of proteins collectively called epigenetic "readers". BET bromodomains have emerged as promising drug targets for treatment of cancers, inflammatory diseases, and other medical conditions. GlaxoSmithKline scientists have successfully optimized a class of benzodiazepines as inhibitors of BET bromodomains, without any prior knowledge of identified molecular targets. It thus is possible to hit a target without aiming at it. The optimized lead compound I-BET762 is currently being evaluated in a phase I clinical trial for treatment of human cancer.

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Year:  2013        PMID： 24107192     DOI： 10.1021/jm4014407

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


  29 in total

Review 1.  The MOZ histone acetyltransferase in epigenetic signaling and disease.

Authors:  Samuel Carlson; Karen C Glass
Journal:  J Cell Physiol       Date:  2014-11       Impact factor: 6.384

Review 2.  Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidence.

Authors:  Aristeidis Chaidos; Valentina Caputo; Anastasios Karadimitris
Journal:  Ther Adv Hematol       Date:  2015-06

Review 3.  Targeting Brd4 for cancer therapy: inhibitors and degraders.

Authors:  Yingchao Duan; Yuanyuan Guan; Wenping Qin; Xiaoyu Zhai; Bin Yu; Hongmin Liu
Journal:  Medchemcomm       Date:  2018-08-07       Impact factor: 3.597

4.  The bromodomain protein BRD4 positively regulates necroptosis via modulating MLKL expression.

Authors:  Yu Xiong; Linli Li; Liting Zhang; Yangyang Cui; Chengyong Wu; Hui Li; Kai Chen; Qiuyuan Yang; Rong Xiang; Yiguo Hu; Shile Huang; Yuquan Wei; Shengyong Yang
Journal:  Cell Death Differ       Date:  2019-01-15       Impact factor: 15.828

5.  A CK1α Activator Penetrates the Brain and Shows Efficacy Against Drug-resistant Metastatic Medulloblastoma.

Authors:  Jezabel Rodriguez-Blanco; Bin Li; Jun Long; Chen Shen; Fan Yang; Darren Orton; Sara Collins; Noriyuki Kasahara; Nagi G Ayad; Heather J McCrea; Martine F Roussel; William A Weiss; Anthony J Capobianco; David J Robbins
Journal:  Clin Cancer Res       Date:  2018-11-28       Impact factor: 12.531

Review 6.  BET-ting on Nrf2: How Nrf2 Signaling can Influence the Therapeutic Activities of BET Protein Inhibitors.

Authors:  Nirmalya Chatterjee; Dirk Bohmann
Journal:  Bioessays       Date:  2018-03-30       Impact factor: 4.345

7.  Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2.

Authors:  Tomoko Takimoto-Shimomura; Taku Tsukamoto; Saori Maegawa; Yuto Fujibayashi; Yayoi Matsumura-Kimoto; Yoshimi Mizuno; Yoshiaki Chinen; Yuji Shimura; Shinsuke Mizutani; Shigeo Horiike; Masafumi Taniwaki; Tsutomu Kobayashi; Junya Kuroda
Journal:  Invest New Drugs       Date:  2018-06-21       Impact factor: 3.850

8.  Discovery of a Positron Emission Tomography Radiotracer Selectively Targeting the BD1 Bromodomains of BET Proteins.

Authors:  Ping Bai; Xiaoxia Lu; Yan Liu; Yu Lan; Hao Wang; Stephanie Fiedler; Robin Striar; Changning Wang
Journal:  ACS Med Chem Lett       Date:  2021-01-08       Impact factor: 4.345

9.  BET bromodomain inhibitors regulate keratinocyte plasticity.

Authors:  Gabi Schutzius; Christian Kolter; Sebastian Bergling; Federico Tortelli; Florian Fuchs; Steffen Renner; Vito Guagnano; Simona Cotesta; Heinrich Rueeger; Michael Faller; Laure Bouchez; Adrian Salathe; Florian Nigsch; Shola M Richards; Malvina Louis; Viktoria Gruber; Alexandra Aebi; Jonathan Turner; Frederic Grandjean; Jun Li; Chris Dimitri; Jason R Thomas; Markus Schirle; Jutta Blank; Peter Drueckes; Andrea Vaupel; Ralph Tiedt; Paul W Manley; Julia Klopp; Rene Hemmig; Florence Zink; Nelly Leroy; Walter Carbone; Guglielmo Roma; Caroline Gubser Keller; Natalie Dales; Armin Beyerbach; Alfred Zimmerlin; Debora Bonenfant; Remi Terranova; Amy Berwick; Sukhdeep Sahambi; Aimee Reynolds; Lori L Jennings; Heinz Ruffner; Peter Tarsa; Tewis Bouwmeester; Vickie Driver; Mathias Frederiksen; Felix Lohmann; Susan Kirkland
Journal:  Nat Chem Biol       Date:  2021-01-18       Impact factor: 15.040

10.  Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer.

Authors:  P Jake Slavish; Liying Chi; Mi-Kyung Yun; Lyudmila Tsurkan; Nancy E Martinez; Barbara Jonchere; Sergio C Chai; Michele Connelly; M Brett Waddell; Sourav Das; Geoffrey Neale; Zhenmei Li; William R Shadrick; Rachelle R Olsen; Kevin W Freeman; Jonathan A Low; Jeanine E Price; Brandon M Young; Nagakumar Bharatham; Vincent A Boyd; Jun Yang; Richard E Lee; Marie Morfouace; Martine F Roussel; Taosheng Chen; Daniel Savic; R Kiplin Guy; Stephen W White; Anang A Shelat; Philip M Potter
Journal:  Cancer Res       Date:  2020-07-10       Impact factor: 12.701
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