Property guided design of a brain penetrant PI3K inhibitor

被引：0
|
作者：
Dotson, Jennafer [1 ]
Heffron, Timothy [1 ]
Pang, Jodie [2 ]
Salphati, Laurent [2 ]
机构：
[1] Genentech Inc, Discovery Chem, San Francisco, CA 94080 USA
[2] Genentech Inc, Drug Met & Pharm, San Francisco, CA 94002 USA
来源：
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY | 2011年 / 242卷
关键词：
D O I：
暂无
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
47-MEDI
引用
收藏
页数：1
相关论文
共 50 条
  • [1] Efficacy of a Brain-penetrant PI3K/mTOR Inhibitor in Orthotopic Models of Glioblastoma
    Salphati, L.
    Heffron, T. P.
    Alicke, B.
    Barck, K.
    Carano, R. A.
    Kharbanda, S.
    Lee, L. B.
    Nishimura, M.
    Olivero, A. G.
    Phillips, H. S.
    EUROPEAN JOURNAL OF CANCER, 2012, 48 : 110 - 110
  • [2] EFFICACY OF A BRAIN-PENETRANT PI3K/MTOR INHIBITOR IN ORTHOTOPIC MODELS OF GLIOBLASTOMA
    Salphati, Laurent
    Heffron, Timothy P.
    Alicke, Bruno
    Barck, Kai
    Carano, Richard A.
    Cheong, Jonathan
    Greve, Joan
    Lee, Leslie B.
    Nishimura, Merry
    Pang, Jodie
    Plise, Emile G.
    Reslan, Hani Bou
    Zhang, Xiaolin
    GOuld, Stephen G.
    Olivero, Alan G.
    Phillips, Heidi S.
    NEURO-ONCOLOGY, 2012, 14 : 35 - 36
  • [3] Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR
    Heffron, Timothy P.
    Ndubaku, Chudi O.
    Salphati, Laurent
    Alicke, Bruno
    Cheong, Jonathan
    Drobnick, Joy
    Edgar, Kyle
    Gould, Stephen E.
    Lee, Leslie B.
    Lesnick, John D.
    Lewis, Cristina
    Nonomiya, Jim
    Pang, Jodie
    Plise, Emile G.
    Sideris, Steve
    Wallin, Jeffrey
    Wang, Lan
    Zhang, Xiaolin
    Olivero, Alan G.
    ACS MEDICINAL CHEMISTRY LETTERS, 2016, 7 (04): : 351 - 356
  • [4] Designing brain-penetrant small molecule inhibitors of PI3K
    Heffron, Timothy P.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 247
  • [5] Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma
    Salphati, Laurent
    Alicke, Bruno
    Heffron, Timothy P.
    Shahidi-Latham, Sheerin
    Nishimura, Merry
    Cao, Tim
    Carano, Richard A.
    Cheong, Jonathan
    Greve, Joan
    Koeppen, Hartmut
    Lau, Shari
    Lee, Leslie B.
    Nannini-Pepe, Michelle
    Pang, Jodie
    Plise, Emile G.
    Quiason, Cristine
    Rangell, Linda
    Zhang, Xiaolin
    Gould, Stephen E.
    Phillips, Heidi S.
    Olivero, Alan G.
    DRUG METABOLISM AND DISPOSITION, 2016, 44 (12) : 1881 - 1889
  • [6] Preclinical therapeutic efficacy of a novel blood-brain barrier-penetrant dual PI3K/mTOR inhibitor with preferential response in PI3K/PTEN mutant glioma
    Koul, Dimpy
    Wang, Shuzhen
    Wu, Shaofang
    Saito, Norihiko
    Zheng, Siyuan
    Gao, Feng
    Kaul, Isha
    Setoguchi, Masaki
    Nakayama, Kiyoshi
    Koyama, Kumiko
    Shiose, Yoshinobu
    Sulman, Erik P.
    Hirota, Yasuhide
    Yung, W. K. Alfred
    ONCOTARGET, 2017, 8 (13) : 21741 - 21753
  • [7] Arsenic trioxide sensitizes glioma stem cells to brain penetrant PI3K and mTOR inhibitor GDC-0084
    Dong, Jianwen
    Martinez-Ledesma, Emmanuel
    Nghi Nguyen
    Carrillo, Caroline
    Piao, Yuji
    Henry, Verlene
    Park, Soon Young
    Tiao, Ningyi
    Stephan, Clifford
    Verhaak, Roel
    Sulman, Erik
    Balasubramaniyan, Veerakumar
    de Groot, John F.
    CANCER RESEARCH, 2018, 78 (13)
  • [8] Targeting the PI3K pathway in the brain - pharmacokinetics and efficacy of a PI3k inhibitor optimized to cross the blood-brain barrier
    Salphati, Laurent
    Pang, Jodie
    Cheong, Jonathan
    Plise, Emile G.
    Alicke, Bruno
    Ding, Xiao
    Dotson, Jennafer
    Feng, Dingzhou
    Heffron, Tim
    Joachico, Allan
    Lee, Leslie B.
    Ndubaku, Chudi
    Nishimura, Merry
    Nonomiya, Jim
    Olivero, Alan
    Phillips, Heidi
    Sideris, Setve
    Wang, Lan
    Zhang, Xiaolin
    DRUG METABOLISM REVIEWS, 2011, 43 : 183 - 183
  • [9] Targeting the PI3K Pathway in the Brain-Efficacy of a PI3K Inhibitor Optimized to Cross the Blood-Brain Barrier
    Salphati, Laurent
    Heffron, Timothy P.
    Alicke, Bruno
    Nishimura, Merry
    Barck, Kai
    Carano, Richard A.
    Cheong, Jonathan
    Edgar, Kyle A.
    Greve, Joan
    Kharbanda, Samir
    Koeppen, Hartmut
    Lau, Shari
    Lee, Leslie B.
    Pang, Jodie
    Plise, Emile G.
    Pokorny, Jenny L.
    Reslan, Hani Bou
    Sarkaria, Jann N.
    Wallin, Jeffrey J.
    Zhang, Xiaolin
    Gould, Stephen E.
    Olivero, Alan G.
    Phillips, Heidi S.
    CLINICAL CANCER RESEARCH, 2012, 18 (22) : 6239 - 6248
  • [10] Evaluation of a PI3K inhibitor by an orthotopic brain tumor model
    Yamori, Takao
    Okamura, Mutsumi
    Yoshimi, Hisashi
    Kawada, Manabu
    Fujimaki, Takamitsu
    CANCER RESEARCH, 2009, 69
12345