Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620

被引：0
|
作者：
Beaufils, Florent
Rageot, Denise
Melone, Anna
Sele, Alexander
Lang, Marc
Mestan, Juergen
Ettlin, Robert A.
Hillmann, Petra
Cmiljanovic, Vladimir
Walter, Carolin
Singer, Elisabeth
Nguyen, Hoa H. P.
Hebeisen, Paul
Fabbro, Dorian
Wymann, Matthias P.
机构：
来源：
CANCER RESEARCH | 2016年 / 76卷
关键词：
D O I：
10.1158/1538-7445.AM2016-393A
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
393A
引用
收藏
页数：4
相关论文
共 50 条
  • [1] Pharmacological characterization of the selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor PQR530
    Hillmann, Petra
    Rageot, Denise
    Beaufils, Florent
    Melone, Anna
    Sele, Alexander
    Ettlin, Robert A.
    Mestan, Juergen
    Cmiljanovic, Vladimir
    Lang, Marc
    Singer, Elisabeth
    Walter, Carolin
    Nguyen, Hoa H. P.
    Hebeisen, Paul
    Wymann, Matthias P.
    Fabbro, Doriano
    CANCER RESEARCH, 2017, 77
  • [2] Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor
    Beaufils, Florent
    Rageot, Denise
    Melone, Anna
    Lang, Marc
    Mestan, Jurgen
    Cmiljanovic, Vladimir
    Hillmann, Petra
    Hebeisen, Paul
    Fabbro, Doriano
    Wymann, Matthias P.
    CANCER RESEARCH, 2016, 76
  • [3] The novel mTORC1/2 inhibitor PQR620 has in vitro and in vivo activity in lymphomas
    Tarantelli, C.
    Gaudio, E.
    Hillmann, P.
    Spriano, F.
    Rinaldi, A.
    Kwee, I.
    Cascione, L.
    Fabbro, D.
    Stathis, A.
    Zucca, E.
    Cmiljanovic, V.
    Bertoni, F.
    EUROPEAN JOURNAL OF CANCER, 2016, 69 : S38 - S38
  • [4] The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy
    Brandt, Claudia
    Hillmann, Petra
    Noack, Andreas
    Roemermann, Kerstin
    Oehler, Leon A.
    Rageot, Denise
    Beaufils, Florent
    Melone, Anna
    Sele, Alexander M.
    Wymann, Matthias P.
    Fabbro, Doriano
    Loescher, Wolfgang
    NEUROPHARMACOLOGY, 2018, 140 : 107 - 120
  • [5] Characterization of AZD8055, a potent selective inhibitor of mTORC1 and mTORC2 kinase
    Chresta, Christine
    Davies, Barry
    Harding, Tom
    Hickson, Ian
    Cosulich, Sabina
    Critchlow, Susan
    Sini, Patrizia
    James, Dominic
    Malagu, Karine
    Hummersone, Marc
    Smith, Graeme
    Pass, Martin
    Guichard, Sylvie
    CANCER RESEARCH, 2009, 69
  • [6] Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1
    Blackaby, Wesley P.
    Lewis, Richard T.
    Thomson, Joanne L.
    Jennings, Andrew S. R.
    Goodacre, Simon C.
    Street, Leslie J.
    MacLeod, Angus M.
    Pike, Andrew
    Wood, Suzanne
    Thomas, Steve
    Brown, Terry A.
    Smith, Alison
    Pillai, Gopalan
    Almond, Sarah
    Guscott, Martin R.
    Burns, H. Donald
    Eng, Waisi
    Ryan, Christine
    Cook, Jacquelynn
    Hamill, Terence G.
    ACS MEDICINAL CHEMISTRY LETTERS, 2010, 1 (07): : 350 - 354
  • [7] Preclinical Characterization of OSI-027, a Potent and Selective Inhibitor of mTORC1 and mTORC2: Distinct from Rapamycin
    Bhagwat, Shripad V.
    Gokhale, Prafulla C.
    Crew, Andrew P.
    Cooke, Andy
    Yao, Yan
    Mantis, Christine
    Kahler, Jennifer
    Workman, Jennifer
    Bittner, Mark
    Dudkin, Lorina
    Epstein, David M.
    Gibson, Neil W.
    Wild, Robert
    Arnold, Lee D.
    Houghton, Peter J.
    Pachter, Jonathan A.
    MOLECULAR CANCER THERAPEUTICS, 2011, 10 (08) : 1394 - 1406
  • [8] Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2
    Pike, Kurt G.
    Morris, Jeff
    Ruston, Linette
    Pass, Sarah L.
    Greenwood, Ryan
    Williams, Emma J.
    Demeritt, Julie
    Culshaw, Janet D.
    Gill, Kristy
    Pass, Martin
    Finlay, M. Raymond V.
    Good, Catherine J.
    Roberts, Craig A.
    Currie, Gordon S.
    Blades, Kevin
    Eden, Jonathan M.
    Pearson, Stuart E.
    JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (05) : 2326 - 2349
  • [9] Characterization of AZD4547: An orally bioavailable, potent and selective inhibitor of FGFR tyrosine kinases 1, 2 and 3
    Gayine, Paul R.
    Mooney, Lorraine
    Kilgour, Elaine
    Thomas, Andrew P.
    Al-Kadhimi, Katherine
    Beck, Sarah
    Coleman, Tanya
    Baker, Dawn
    Mellor, Martine J.
    Brooks, Nigel A. N.
    Klinowska, Teresa
    CANCER RESEARCH, 2011, 71
  • [10] The Antipancreatic Cancer Activity of OSI-027, a Potent and Selective Inhibitor of mTORC1 and mTORC2
    Chen, Bo
    Xu, Ming
    Zhang, Hui
    Xu, Ming-zheng
    Wang, Xu-jing
    Tang, Qing-he
    Tang, Jian-ying
    DNA AND CELL BIOLOGY, 2015, 34 (10) : 610 - 617
12345