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
关键词
D O I
暂无
中图分类号
学科分类号
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]
引用
收藏
页码:305 / 312
页数:7
相关论文
共 50 条
  • [41] Large-Scale Evaluation of CavBase for Analyzing the Polypharmacology of Kinase Inhibitors
    Kalliokoski, Tuomo
    Vulpetti, Anna
    MOLECULAR INFORMATICS, 2011, 30 (11-12) : 923 - 925
  • [42] Targeting JAK3 tyrosine kinase-linked signal transduction pathways with rationally-designed inhibitors
    Uckun, Fatih M.
    Vassilev, Alexei
    Dibirdik, Ilker
    Tibbles, Heather
    ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2007, 7 (06) : 612 - 623
  • [43] Hsp90 Inhibitors from rationally designed chimeric compounds
    Shen, Gang
    Blagg, Brian S. J.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2006, 231
  • [44] Rationally designed TNF-α inhibitors: Identification of promising cytotoxic agents
    Kaur, Baljit
    Mishra, Sahil
    Kaur, Ramandeep
    Kalotra, Shikha
    Singh, Palwinder
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021, 41
  • [45] Dual targeting of Bruton's tyrosine kinase and Janus kinase 3 with rationally designed inhibitors prevents graft-versus-host disease (GVHD) in a murine allogeneic bone marrow transplantation model
    Cetkovic-Cvrlje, M
    Uckun, FM
    BRITISH JOURNAL OF HAEMATOLOGY, 2004, 126 (06) : 821 - 827
  • [46] Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors
    Karim, Rezaul Md
    Bikowitz, Melissa J.
    Chan, Alice
    Zhu, Jin-Yi
    Grassie, Dylan
    Becker, Andreas
    Berndt, Norbert
    Gunawan, Steven
    Lawrence, Nicholas J.
    Schonbrunn, Ernst
    JOURNAL OF MEDICINAL CHEMISTRY, 2021, 64 (21) : 15772 - 15786
  • [47] X-Ray crystallographic studies of rationally designed dihydroorotate dehydrogenase inhibitors
    Acklam, Paul
    Bedingfield, Paul
    Cunningham, Fraser
    Cowen, Deborah
    McConkey, Glenn
    Fishwick, Colin
    Johnson, Peter
    Parsons, Mark
    ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES, 2011, 67 : C312 - C312
  • [48] Development of rationally designed DNA N6 adenine methyltransferase inhibitors
    Hobley, Gerard
    McKelvie, Jennifer C.
    Harmer, Jenny E.
    Howe, Jason
    Oyston, Petra C. F.
    Roach, Peter L.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 22 (09) : 3079 - 3082
  • [49] Potent Dual BET Bromodomain-Kinase Inhibitors as Value-Added Multitargeted Chemical Probes and Cancer Therapeutics
    Ember, Stuart W.
    Lambert, Que T.
    Berndt, Norbert
    Gunawan, Steven
    Ayaz, Muhammad
    Tauro, Marilena
    Zhu, Jin-Yi
    Cranfill, Paula J.
    Greninger, Patricia
    Lynch, Conor C.
    Benes, Cyril H.
    Lawrence, Harshani R.
    Reuther, Gary W.
    Lawrence, Nicholas J.
    Schonbrunn, Ernst
    MOLECULAR CANCER THERAPEUTICS, 2017, 16 (06) : 1054 - 1067
  • [50] Rationally designed amyloid inhibitors based on amyloid-related structural studies
    Hu, Jinjian
    Zhao, Yufen
    Li, Yanmei
    CHINESE CHEMICAL LETTERS, 2023, 34 (02)