Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762-Reference-Cited by-同舟云学术

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

Published:2014-01-30 Issue:5 Volume:123 Page:697-705
ISSN:0006-4971
Container-title:Blood
language:en
Short-container-title:

Author:

Chaidos Aristeidis¹,Caputo Valentina¹,Gouvedenou Katerina¹,Liu Binbin¹,Marigo Ilaria¹,Chaudhry Mohammed Suhail¹,Rotolo Antonia¹,Tough David F.²,Smithers Nicholas N.²,Bassil Anna K.²,Chapman Trevor D.²,Harker Nicola R.²,Barbash Olena³,Tummino Peter³,Al-Mahdi Niam²,Haynes Andrea C.²,Cutler Leanne²,Le BaoChau²,Rahemtulla Amin¹,Roberts Irene¹,Kleijnen Maurits¹,Witherington Jason J.²,Parr Nigel J.²,Prinjha Rab K.²,Karadimitris Anastasios¹

Affiliation:

1. Centre for Haematology, Department of Medicine, Hammersmith Hospital, Imperial College London, London, United Kingdom;

2. Epinova Drug Performance Unit, Immuno-Inflammation Therapeutic Area and Quantitative Sciences Computational Biology, GlaxoSmithKline, Stevenage, United Kingdom; and

3. Cancer Epigenetics Epinova Drug Performance Unit, GlaxoSmithKline, Collegeville, PA

Abstract

Key Points I-BET151 and I-BET-762 induce cell cycle arrest and apoptosis in myeloma cells associated with MYC downregulation and HEXIM1 upregulation. Preclinical functional and pharmacologic profiling of I-BET762 supports its use in phase 1 clinical studies.

Publisher

American Society of Hematology

Subject

Cell Biology,Hematology,Immunology,Biochemistry

Link

http://ashpublications.org/blood/article-pdf/123/5/697/1379356/697.pdf

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