Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

被引：0
|
作者：
Pietro Ciceri
Susanne Müller
Alison O'Mahony
Oleg Fedorov
Panagis Filippakopoulos
Jeremy P Hunt
Elisabeth A Lasater
Gabriel Pallares
Sarah Picaud
Christopher Wells
Sarah Martin
Lisa M Wodicka
Neil P Shah
Daniel K Treiber
Stefan Knapp
机构：
[1] KINOMEscan Division of DiscoveRx Corporation,Nuffield Department of Clinical Medicine
[2] University of Oxford,Nuffield Department of Clinical Medicine
[3] Structural Genomics Consortium,Nuffield Department of Clinical Medicine
[4] University of Oxford,Division of Hematology/Oncology
[5] Target Discovery Institute (TDI),undefined
[6] BioSeek Division of DiscoveRx Corporation,undefined
[7] University of Oxford,undefined
[8] Ludwig Institute for Cancer Research (LICR),undefined
[9] University of California–San Francisco,undefined
来源：
Nature Chemical Biology | 2014年 / 10卷
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摘要：
Kinases are a widely targeted enzyme class in cancer chemotherapy. Several clinically used kinase inhibitors also inhibit bromodomains, epigenetic ‘readers’ of acetylated lysine residues, suggesting that kinase-bromodomain polypharmacology may offer benefits in therapeutic settings.[graphic not available: see fulltext]
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页码：305 / 312
页数：7
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