Discovery and characterization of OKI-219, an orally bioavailable H1047R-mutant-selective inhibitor of PI3Kα

被引：0
|
作者：
Taylor, Molly A.
Zhao, Qian
Mareska, David
Hoh, Maria
Izrayelit, Yevgeniy
Litwiler, Kevin
Boys, Mark L.
Woessner, Rich
Walker, Duncan
Diamond, Jennifer
Winkler, James D.
机构：
来源：
MOLECULAR CANCER THERAPEUTICS | 2023年 / 22卷 / 12期
关键词：
D O I：
10.1158/1535-7163.TARG-23-B163
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
B163
引用
收藏
页数：2
相关论文
共 50 条
  • [1] OKI-219 is an inhibitor of PI3K α H1047R that has brain penetrance and anti-tumor activity in a preclinical intracranial model of metastatic breast cancer
    Strait, Alexander A.
    Taylor, Molly A.
    Litwiler, Kevin S.
    Zhao, Qian
    Mareska, David A.
    Boys, Mark L.
    Izrayelit, Yevgeniy
    Woessner, Richard
    Winkler, James D.
    [J]. CANCER RESEARCH, 2024, 84 (07)
  • [2] OKI-219, a PI3KaH1047R-mutant-selective inhibitor demonstrates efficacy as a single agent and drives combination responses with standard of care therapies in preclinical PI3KaH1047R mutant breast cancer models
    Taylor, Molly A.
    Zhao, Qian
    Mareska, David
    Hoh, Maria
    Izrayelit, Yevgeniy
    Litwiler, Kevin
    Boys, Mark L.
    Woessner, Rich
    Walker, Duncan
    Winkler, James D.
    Diamond, Jennifer
    [J]. CANCER RESEARCH, 2024, 84 (09)
  • [3] Discovery and characterization of a mutant selective PI3KαH1047Xinhibitor with a best-in-class profile
    Buckbinder, Leonard
    St Jean, David J.
    Tieu, Trang
    Wang, Weixue
    Kryukov, Gregory
    Jonsson, Philip
    Alltucker, Jacob
    Manimala, Samantha
    Ladd, Brendon
    Guzman-Perez, Angel
    Stuart, Darrin
    [J]. CANCER RESEARCH, 2022, 82 (12)
  • [4] Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein
    Ketcham, John M.
    Harwood, Stephen J.
    Aranda, Ruth
    Aloiau, Athenea N.
    Bobek, Briana M.
    Briere, David M.
    Burns, Aaron C.
    Haatveit, Kersti Caddell
    Calinisan, Andrew
    Clarine, Jeffery
    Elliott, Adam
    Engstrom, Lars D.
    Gunn, Robin J.
    Ivetac, Anthony
    Jones, Benjamin
    Kuehler, Jon
    Lawson, J. David
    Nguyen, Natalie
    Parker, Cody
    Pearson, Kelly E.
    Rahbaek, Lisa
    Saechao, Barbara
    Wang, Xiaolun
    Waters, Anna
    Waters, Laura
    Watkins, Ashlee H.
    Olson, Peter
    Smith, Christopher R.
    Christensen, James G.
    Marx, Matthew A.
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (06) : 4936 - 4949
  • [5] Discovery of a novel and potent mutant-selective inhibitor of PI3Kα
    Gao, Mingming
    Qi, Chao
    Li, Zhentian
    Fan, Qipeng
    Wang, Liyang
    Zhou, Fei
    You, Lin
    Zheng, Hewen
    Li, Yu
    Wu, Liangxing
    Yao, Wenqing
    Liu, Phillip C.
    [J]. CANCER RESEARCH, 2024, 84 (06)
  • [6] Targeting aberrant PI3K pathway signaling with XL147, a potent, selective and orally bioavailable PI3K inhibitor
    Shapiro, Geoffrey I.
    Edelman, Gerald
    Calvo, Emiliano
    Aggarwal, Sanjay K.
    Laird, A. Douglas
    [J]. MOLECULAR CANCER THERAPEUTICS, 2007, 6 (12) : 3594S - 3594S
  • [7] Colon Cancer Tumorigenesis Initiated by the H1047R Mutant PI3K
    Yueh, Alexander E.
    Payne, Susan N.
    Leystra, Alyssa A.
    Van De Hey, Dana R.
    Foley, Tyler M.
    Pasch, Cheri A.
    Clipson, Linda
    Matkowskyj, Kristina A.
    Deming, Dustin A.
    [J]. PLOS ONE, 2016, 11 (02):
  • [8] Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors
    Pemberton, Nils
    Mogemark, Mickael
    Arlbrandt, Susanne
    Bold, Peter
    Cox, Rhona J.
    Gardelli, Cristina
    Holden, Neil S.
    Karabelas, Kostas
    Karlsson, Johan
    Lever, Sarah
    Li, Xueshan
    Lindrnark, Helena
    Norberg, Monica
    Perry, Matthew W. D.
    Petersen, Jens
    Blomqvist, Sandra Rodrigo
    Thomas, Matthew
    Tyrchan, Christian
    Eriksson, Annika Westin
    Zlatoidsky, Pavol
    Osterg, Linda
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2018, 61 (12) : 5435 - 5441
  • [9] LOXO-783: A potent, highly mutant selective and brain-penetrant allosteric PI3Kα H1047R inhibitor in combination with standard of care (SOC) treatments in preclinical PI3Kα H1047R-mutant breast cancer models
    Puca, Loredana
    Dowless, Michele S.
    Perez-Ferreiro, Carmen M.
    Ortiz-Ruiz, Maria Jesus
    Donoho, Gregory P.
    Capen, Andrew
    Huber, Lysiane
    Bogner, Sarah M.
    Fei, Dongling
    Manro, Jason R.
    Yu, Chun Ping
    Xu, Wei Guo
    Wang, Rui
    Chen, Shuang
    Hicks, Mark A.
    Zolfaghari, Parisa
    Faber, Andrew
    Gilmour, Raymond
    Ramstetter, Monica D.
    Chang, Matthew T.
    Lallena, Maria Jose
    Gong, Xuequian
    Hyman, David M.
    Smyth, Lillian M.
    Brandhuber, Barbara J.
    Taylor, Barry S.
    Klippel, Anke
    [J]. CANCER RESEARCH, 2023, 83 (05)
  • [10] Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode
    Down, Kenneth
    Amour, Augustin
    Anderson, Niall A.
    Barton, Nick
    Campos, Sebastien
    Cannons, Edward P.
    Clissold, Cole
    Convery, Maire A.
    Coward, John J.
    Doyle, Kevin
    Duempelfeld, Birgit
    Edwards, Christopher D.
    Goldsmith, Michael D.
    Krause, Jana
    Mallett, David N.
    McGonagle, Grant A.
    Patel, Vipulkumar K.
    Rowedder, James
    Rowland, Paul
    Sharpe, Andrew
    Sriskantharajah, Srividya
    Thomas, Daniel A.
    Thomson, Douglas W.
    Uddin, Sorif
    Hamblin, J. Nicole
    Hessel, Edith M.
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2021, 64 (18) : 13780 - 13792
12345