Literature DB >> 27295577

Clinical progress and pharmacology of small molecule bromodomain inhibitors.

Natalie H Theodoulou1, Nicholas Co Tomkinson2, Rab K Prinjha3, Philip G Humphreys4.   

Abstract

Bromodomains have emerged as an exciting target class for drug discovery over the past decade. Research has primarily focused on the bromodomain and extra terminal (BET) family of bromodomains, which has led to the development of multiple small molecule inhibitors and an increasing number of clinical assets. The excitement centred on the clinical potential of BET inhibition has stimulated intense interest in the broader family and the growing number of non-BET bromodomain chemical probes has facilitated phenotypic investigations, implicating these targets in a variety of disease pathways including cancer, inflammation, embryonic development and neurological disorders.
Copyright © 2016 Elsevier Ltd. All rights reserved.

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Year:  2016        PMID: 27295577     DOI: 10.1016/j.cbpa.2016.05.028

Source DB:  PubMed          Journal:  Curr Opin Chem Biol        ISSN: 1367-5931            Impact factor:   8.822


  24 in total

1.  BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo.

Authors:  Mary A Morse; Karla K Balogh; Sarah A Brendle; Colin A Campbell; Mao X Chen; Rebecca C Furze; Isobel L Harada; Ian D Holyer; Umesh Kumar; Kevin Lee; Rab K Prinjha; Martin Rüdiger; Jonathan T Seal; Simon Taylor; Jason Witherington; Neil D Christensen
Journal:  Antiviral Res       Date:  2018-04-11       Impact factor: 5.970

Review 2.  Molecules targeting the androgen receptor (AR) signaling axis beyond the AR-Ligand binding domain.

Authors:  N G R Dayan Elshan; Matthew B Rettig; Michael E Jung
Journal:  Med Res Rev       Date:  2018-11-22       Impact factor: 12.944

Review 3.  Cancer therapies in HIV cure research.

Authors:  Thomas A Rasmussen; Jenny L Anderson; Fiona Wightman; Sharon R Lewin
Journal:  Curr Opin HIV AIDS       Date:  2017-01       Impact factor: 4.283

4.  Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.

Authors:  David Remillard; Dennis L Buckley; Hyuk-Soo Seo; Fleur M Ferguson; Sirano Dhe-Paganon; James E Bradner; Nathanael S Gray
Journal:  ACS Med Chem Lett       Date:  2019-09-13       Impact factor: 4.345

5.  Design and Optimization of Benzopiperazines as Potent Inhibitors of BET Bromodomains.

Authors:  David S Millan; Katherine J Kayser-Bricker; Matthew W Martin; Adam C Talbot; Shawn E R Schiller; Torsten Herbertz; Grace L Williams; George P Luke; Stephen Hubbs; Monica A Alvarez Morales; Daniel Cardillo; Paul Troccolo; Rachel L Mendes; Crystal McKinnon
Journal:  ACS Med Chem Lett       Date:  2017-07-14       Impact factor: 4.345

6.  Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands.

Authors:  David Remillard; Dennis L Buckley; Joshiawa Paulk; Gerard L Brien; Matthew Sonnett; Hyuk-Soo Seo; Shiva Dastjerdi; Martin Wühr; Sirano Dhe-Paganon; Scott A Armstrong; James E Bradner
Journal:  Angew Chem Int Ed Engl       Date:  2017-04-18       Impact factor: 15.336

7.  Data-Driven Construction of Antitumor Agents with Controlled Polypharmacology.

Authors:  Chenxiao Da; Dehui Zhang; Michael Stashko; Eleana Vasileiadi; Rebecca E Parker; Katherine A Minson; Madeline G Huey; Justus M Huelse; Debra Hunter; Thomas S K Gilbert; Jacqueline Norris-Drouin; Michael Miley; Laura E Herring; Lee M Graves; Deborah DeRyckere; H Shelton Earp; Douglas K Graham; Stephen V Frye; Xiaodong Wang; Dmitri Kireev
Journal:  J Am Chem Soc       Date:  2019-09-20       Impact factor: 15.419

8.  Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.

Authors:  Yujun Zhao; Bing Zhou; Longchuan Bai; Liu Liu; Chao-Yie Yang; Jennifer L Meagher; Jeanne A Stuckey; Donna McEachern; Sally Przybranowski; Mi Wang; Xu Ran; Angelo Aguilar; Yang Hu; Jeff W Kampf; Xiaoqin Li; Ting Zhao; Siwei Li; Bo Wen; Duxin Sun; Shaomeng Wang
Journal:  J Med Chem       Date:  2018-07-17       Impact factor: 7.446

9.  Development and Validation of 2D Difference Intensity Analysis for Chemical Library Screening by Protein-Detected NMR Spectroscopy.

Authors:  John M Egner; Davin R Jensen; Michael D Olp; Nolan W Kennedy; Brian F Volkman; Francis C Peterson; Brian C Smith; R Blake Hill
Journal:  Chembiochem       Date:  2018-01-25       Impact factor: 3.164

10.  Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 Inhibitors.

Authors:  Alex Muthengi; Virangika K Wimalasena; Hailemichael O Yosief; Melissa J Bikowitz; Logan H Sigua; Tingjian Wang; Deyao Li; Zied Gaieb; Gagan Dhawan; Shuai Liu; Jon Erickson; Rommie E Amaro; Ernst Schönbrunn; Jun Qi; Wei Zhang
Journal:  J Med Chem       Date:  2021-04-19       Impact factor: 7.446

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