Phosphatidylinositide-3-Kinase Inhibitors: Addressing Questions of Isoform Selectivity and Pharmacodynamic/Predictive Biomarkers in Early Clinical Trials

被引:24
作者
Clarke, Paul A. [1 ]
Workman, Paul [1 ]
机构
[1] Inst Canc Res, Haddow Labs, Sutton, Surrey, England
关键词
CLASS-I; HUMAN CANCER; POTENT; DISCOVERY; MUTATIONS; PATHWAY;
D O I
10.1200/JCO.2011.38.7167
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
引用
收藏
页码:331 / 333
页数:3
相关论文
共 14 条
  • [1] WORTMANNIN IS A POTENT PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR - THE ROLE OF PHOSPHATIDYLINOSITOL 3,4,5-TRISPHOSPHATE IN NEUTROPHIL RESPONSES
    ARCARO, A
    WYMANN, MP
    [J]. BIOCHEMICAL JOURNAL, 1993, 296 : 297 - 301
  • [2] Phase I, Dose-Escalation Study of BKM120, an Oral Pan-Class I PI3K Inhibitor, in Patients With Advanced Solid Tumors
    Bendell, Johanna C.
    Rodon, Jordi
    Burris, Howard A.
    de Jonge, Maja
    Verweij, Jaap
    Birle, Diana
    Demanse, David
    De Buck, Stefan S.
    Ru, Qinhua C.
    Peters, Malte
    Goldbrunner, Michael
    Baselga, Jose
    [J]. JOURNAL OF CLINICAL ONCOLOGY, 2012, 30 (03) : 282 - 290
  • [3] Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer
    Burger, Matthew T.
    Pecchi, Sabina
    Wagman, Allan
    Ni, Zhi-Jie
    Knapp, Mark
    Hendrickson, Thomas
    Atallah, Gordana
    Pfister, Keith
    Zhang, Yanchen
    Bartulis, Sarah
    Frazier, Kelly
    Ng, Simon
    Smith, Aaron
    Verhagen, Joelle
    Haznedar, Joshua
    Huh, Kay
    Iwanowicz, Ed
    Xin, Xiaohua
    Menezes, Daniel
    Merritt, Hanne
    Lee, Isabelle
    Wiesmann, Marion
    Kaufman, Susan
    Crawford, Kenneth
    Chin, Michael
    Bussiere, Dirksen
    Shoemaker, Kevin
    Zaror, Isabel
    Maira, Sauveur-Michel
    Voliva, Charles F.
    [J]. ACS MEDICINAL CHEMISTRY LETTERS, 2011, 2 (10): : 774 - 779
  • [4] COSMIC (the Catalogue of Somatic Mutations in Cancer): a resource to investigate acquired mutations in human cancer
    Forbes, Simon A.
    Tang, Gurpreet
    Bindal, Nidhi
    Bamford, Sally
    Dawson, Elisabeth
    Cole, Charlotte
    Kok, Chai Yin
    Jia, Mingming
    Ewing, Rebecca
    Menzies, Andrew
    Teague, Jon W.
    Stratton, Michael R.
    Futreal, P. Andrew
    [J]. NUCLEIC ACIDS RESEARCH, 2010, 38 : D652 - D657
  • [5] Targeting the phosphoinositide 3-kinase pathway in cancer
    Liu, Pixu
    Cheng, Hailing
    Roberts, Thomas M.
    Zhao, Jean J.
    [J]. NATURE REVIEWS DRUG DISCOVERY, 2009, 8 (08) : 627 - 644
  • [6] Maira M, 2010, AM ASS CANC RES ANN
  • [7] Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
    Raynaud, Florence I.
    Eccles, Suzanne A.
    Patel, Sonal
    Alix, Sonia
    Box, Gary
    Chuckowree, Irina
    Folkes, Adrian
    Gowan, Sharon
    Brandon, Alexis De Haven
    Di Stefano, Francesca
    Hayes, Angela
    Henley, Alan T.
    Lensun, Letitia
    Pergl-Wilson, Giles
    Robson, Anthony
    Saghir, Nahid
    Zhyvoloup, Alexander
    McDonald, Edward
    Sheldrake, Peter
    Shuttleworth, Stephen
    Valenti, Melanie
    Wan, Nan Chi
    Clarke, Paul A.
    Workman, Paul
    [J]. MOLECULAR CANCER THERAPEUTICS, 2009, 8 (07) : 1725 - 1738
  • [8] Shuttleworth SJ, 2011, CURR MED CHEM, V18, P2686
  • [9] The emerging mechanisms of isoform-specific PI3K signalling
    Vanhaesebroeck, Bart
    Guillermet-Guibert, Julie
    Graupera, Mariona
    Bilanges, Benoit
    [J]. NATURE REVIEWS MOLECULAR CELL BIOLOGY, 2010, 11 (05) : 329 - 341
  • [10] AKT-Independent Signaling Downstream of Oncogenic PIK3CA Mutations in Human Cancer
    Vasudevan, Krishna M.
    Barbie, David A.
    Davies, Michael A.
    Rabinovsky, Rosalia
    McNear, Chontelle J.
    Kim, Jessica J.
    Hennessy, Bryan T.
    Tseng, Hsiuyi
    Pochanard, Panisa
    Kim, So Young
    Dunn, Ian F.
    Schinzel, Anna C.
    Sandy, Peter
    Hoersch, Sebastian
    Sheng, Qing
    Gupta, Piyush B.
    Boehm, Jesse S.
    Reiling, Jan H.
    Silver, Serena
    Lu, Yiling
    Stemke-Hale, Katherine
    Dutta, Bhaskar
    Joy, Corwin
    Sahin, Aysegul A.
    Gonzalez-Angulo, Ana Maria
    Lluch, Ana
    Rameh, Lucia E.
    Jacks, Tyler
    Root, David E.
    Lander, Eric S.
    Mills, Gordon B.
    Hahn, William C.
    Sellers, William R.
    Garraway, Levi A.
    [J]. CANCER CELL, 2009, 16 (01) : 21 - 32