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

被引:25
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 [J].
ARCARO, A ;
WYMANN, MP .
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 [J].
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 .
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 [J].
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. .
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 [J].
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 .
NUCLEIC ACIDS RESEARCH, 2010, 38 :D652-D657
[5]   Targeting the phosphoinositide 3-kinase pathway in cancer [J].
Liu, Pixu ;
Cheng, Hailing ;
Roberts, Thomas M. ;
Zhao, Jean 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 [J].
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 .
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 [J].
Vanhaesebroeck, Bart ;
Guillermet-Guibert, Julie ;
Graupera, Mariona ;
Bilanges, Benoit .
NATURE REVIEWS MOLECULAR CELL BIOLOGY, 2010, 11 (05) :329-341
[10]   AKT-Independent Signaling Downstream of Oncogenic PIK3CA Mutations in Human Cancer [J].
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. .
CANCER CELL, 2009, 16 (01) :21-32