DRUG DISCOVERY Inhibitors that activate

被引：65
作者：
Cichowski, Karen [1 ]
Jaenne, Pasi A. [2 ]
机构：
[1] Brigham & Womens Hosp, Div Genet, Boston, MA 02115 USA
[2] Dana Farber Canc Inst, Dept Med Oncol, Boston, MA 02115 USA
来源：
NATURE | 2010年 / 464卷 / 7287期
关键词：
SQUAMOUS-CELL CARCINOMAS; BRAF;
D O I：
10.1038/464358a
中图分类号：
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号：
07 ; 0710 ; 09 ;
摘要：
Inhibitors of RAF enzymes can suppress or activate the same signalling pathway. The details of how this happens provide a cautionary note for those targeting the pathway for anticancer drug discovery.
引用
收藏
页码：358 / 359
页数：2
相关论文
共 9 条
  • [1] Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers
    Adjei, Alex A.
    Cohen, Roger B.
    Franklin, Wilbur
    Morris, Clive
    Wilson, David
    Molina, Julian R.
    Hanson, Lorelei J.
    Gore, Lia
    Chow, Laura
    Leong, Stephen
    Maloney, Lara
    Gordon, Gilad
    Simmons, Heidi
    Marlow, Allison
    Litwiler, Kevin
    Brown, Suzy
    Poch, Gregory
    Kane, Katie
    Haney, Jerry
    Eckhardt, S. Gail
    [J]. JOURNAL OF CLINICAL ONCOLOGY, 2008, 26 (13) : 2139 - 2146
  • [2] Keratoacanthomas and Squamous Cell Carcinomas in Patients Receiving Sorafenib
    Arnault, Jean Philippe
    Wechsler, Janine
    [J]. JOURNAL OF CLINICAL ONCOLOGY, 2009, 27 (23) : E59 - E61
  • [3] Flaherty K, 2009, J CLIN ONCOL, V27
  • [4] RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
    Hatzivassiliou, Georgia
    Song, Kyung
    Yen, Ivana
    Brandhuber, Barbara J.
    Anderson, Daniel J.
    Alvarado, Ryan
    Ludlam, Mary J. C.
    Stokoe, David
    Gloor, Susan L.
    Vigers, Guy
    Morales, Tony
    Aliagas, Ignacio
    Liu, Bonnie
    Sideris, Steve
    Hoeflich, Klaus P.
    Jaiswal, Bijay S.
    Seshagiri, Somasekar
    Koeppen, Hartmut
    Belvin, Marcia
    Friedman, Lori S.
    Malek, Shiva
    [J]. NATURE, 2010, 464 (7287) : 431 - U132
  • [5] Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF
    Heidorn, Sonja J.
    Milagre, Carla
    Whittaker, Steven
    Nourry, Arnaud
    Niculescu-Duvas, Ion
    Dhomen, Nathalie
    Hussain, Jahan
    Reis-Filho, Jorge S.
    Springer, Caroline J.
    Pritchard, Catrin
    Marais, Richard
    [J]. CELL, 2010, 140 (02) : 209 - 221
  • [6] Ikenoue T, 2003, CANCER RES, V63, P8132
  • [7] RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF
    Poulikakos, Poulikos I.
    Zhang, Chao
    Bollag, Gideon
    Shokat, Kevan M.
    Rosen, Neal
    [J]. NATURE, 2010, 464 (7287) : 427 - U126
  • [8] BRAF mutation predicts sensitivity to MEK inhibition
    Solit, DB
    Garraway, LA
    Pratilas, CA
    Sawai, A
    Getz, G
    Basso, A
    Ye, Q
    Lobo, JM
    She, YH
    Osman, I
    Golub, TR
    Sebolt-Leopold, J
    Sellers, WR
    Rosen, N
    [J]. NATURE, 2006, 439 (7074) : 358 - 362
  • [9] ACTIVATED RAS GENES OCCUR IN HUMAN ACTINIC KERATOSES, PREMALIGNANT PRECURSORS TO SQUAMOUS-CELL CARCINOMAS
    SPENCER, JM
    KAHN, SM
    JIANG, W
    DELEO, VA
    WEINSTEIN, IB
    [J]. ARCHIVES OF DERMATOLOGY, 1995, 131 (07) : 796 - 800
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