Taking Aim at Glycolysis with CDK8 Inhibitors

被引:4
作者
Fisher, Robert P. [1 ]
机构
[1] Icahn Sch Med Mt Sinai, Dept Oncol Sci, New York, NY 10029 USA
关键词
KINASE; TRANSCRIPTION; ACTIVATION; CANCER; CELLS;
D O I
10.1016/j.tem.2018.02.005
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Dependence on glycolysis under aerobic conditions, a frequent metabolic derangement in cancer cells, suggests a therapeutic opportunity. Now, through chemical genetics, CDK8, a kinase associated with the Mediator transcriptional coactivator complex, has emerged as an upstream inducer of glycolysis and a possible target for anticancer drug discovery.
引用
收藏
页码:281 / 282
页数:2
相关论文
共 12 条
  • [1] The Mediator complex: a central integrator of transcription
    Allen, Benjamin L.
    Taatjes, Dylan J.
    [J]. NATURE REVIEWS MOLECULAR CELL BIOLOGY, 2015, 16 (03) : 155 - 166
  • [2] Engineering an analog-sensitive CDK12 cell line using CRISPR/Cas
    Bartkowiak, Bartlomiej
    Yan, Christopher
    Greenleaf, Arno L.
    [J]. BIOCHIMICA ET BIOPHYSICA ACTA-GENE REGULATORY MECHANISMS, 2015, 1849 (09): : 1179 - 1187
  • [3] A chemical switch for inhibitor-sensitive alleles of any protein kinase
    Bishop, AC
    Ubersax, JA
    Petsch, DT
    Matheos, DP
    Gray, NS
    Blethrow, J
    Shimizu, E
    Tsien, JZ
    Schultz, PG
    Rose, MD
    Wood, JL
    Morgan, DO
    Shokat, KM
    [J]. NATURE, 2000, 407 (6802) : 395 - 401
  • [4] CDK8 Kinase Activity Promotes Glycolysis
    Galbraith, Matthew D.
    Andrysik, Zdenek
    Pandey, Ahwan
    Hoh, Maria
    Bonner, Elizabeth A.
    Hill, Amanda A.
    Sullivan, Kelly D.
    Espinosa, Joaquin M.
    [J]. CELL REPORTS, 2017, 21 (06): : 1495 - 1506
  • [5] HIF1A Employs CDK8-Mediator to Stimulate RNAPII Elongation in Response to Hypoxia
    Galbraith, Matthew D.
    Allen, Mary A.
    Bensard, Claire L.
    Wang, Xiaoxing
    Schwinn, Marie K.
    Qin, Bo
    Long, Henry W.
    Daniels, Danette L.
    Hahn, William C.
    Dowell, Robin D.
    Espinosa, Joaquin M.
    [J]. CELL, 2013, 153 (06) : 1327 - 1339
  • [6] CDK9-dependent RNA polymerase II pausing controls transcription initiation
    Gressel, Saskia
    Schwalb, Bjorn
    Decker, Tim Michael
    Qin, Weihua
    Leonhardt, Heinrich
    Eick, Dirk
    Cramer, Patrick
    [J]. ELIFE, 2017, 6
  • [7] Reprogramming glucose metabolism in cancer: can it be exploited for cancer therapy?
    Hay, Nissim
    [J]. NATURE REVIEWS CANCER, 2016, 16 (10) : 635 - 649
  • [8] Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors
    Kalan, Sampada
    Amat, Ramon
    Schachter, Miriam Merzel
    Kwiatkowski, Nicholas
    Abraham, Brian J.
    Liang, Yanke
    Zhang, Tinghu
    Olson, Calla M.
    Larochelle, Stephane
    Young, Richard A.
    Gray, Nathanael S.
    Fisher, Robert P.
    [J]. CELL REPORTS, 2017, 21 (02): : 467 - 481
  • [9] HIF1α and HIF2α: sibling rivalry in hypoxic tumour growth and progression
    Keith, Brian
    Johnson, Randall S.
    Simon, M. Celeste
    [J]. NATURE REVIEWS CANCER, 2012, 12 (01) : 9 - 22
  • [10] Targeting transcription regulation in cancer with a covalent CDK7 inhibitor
    Kwiatkowski, Nicholas
    Zhang, Tinghu
    Rahl, Peter B.
    Abraham, Brian J.
    Reddy, Jessica
    Ficarro, Scott B.
    Dastur, Anahita
    Amzallag, Arnaud
    Ramaswamy, Sridhar
    Tesar, Bethany
    Jenkins, Catherine E.
    Hannett, Nancy M.
    McMillin, Douglas
    Sanda, Takaomi
    Sim, Taebo
    Kim, Nam Doo
    Look, Thomas
    Mitsiades, Constantine S.
    Weng, Andrew P.
    Brown, Jennifer R.
    Benes, Cyril H.
    Marto, Jarrod A.
    Young, Richard A.
    Gray, Nathanael S.
    [J]. NATURE, 2014, 511 (7511) : 616 - +