DEVELOPMENT OF BRAIN-PENETRANT EGFR INHIBITORS FOR CNS MALIGNANCIES

被引:0
|
作者
Tsang, Jonathan [1 ]
Urner, Lorenz [1 ]
Tse, Christopher [1 ]
Baufeld, Lynn [1 ]
Faull, Kym [1 ]
Clark, Peter [1 ]
Cloughesy, Timothy [1 ]
Jung, Michael [1 ]
Nathanson, David [1 ]
机构
[1] Univ Calif Los Angeles, Los Angeles, CA USA
关键词
D O I
暂无
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
DDIS-17
引用
收藏
页码:66 / 66
页数:1
相关论文
共 50 条
  • [31] Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors
    Keylor, Mitchell H.
    Gulati, Anmol
    Kattar, Solomon D.
    Johnson, Rebecca E.
    Chau, Ryan W.
    Margrey, Kaila A.
    Ardolino, Michael J.
    Zarate, Cayetana
    Poremba, Kelsey E.
    Simov, Vladimir
    Morriello, Gregori J.
    Acton, John J.
    Pio, Barbara
    Yan, Xin
    Palte, Rachel L.
    McMinn, Spencer E.
    Nogle, Lisa
    Lesburg, Charles A.
    Adpressa, Donovon
    Lin, Shishi
    Neelamkavil, Santhosh
    Liu, Ping
    Su, Jing
    Hegde, Laxminarayan G.
    Woodhouse, Janice D.
    Faltus, Robert
    Xiong, Tina
    Ciaccio, Paul J.
    Piesvaux, Jennifer
    Otte, Karin M.
    Wood, Harold B.
    Kennedy, Matthew E.
    Bennett, David Jonathan
    DiMauro, Erin F.
    Fell, Matthew J.
    Fuller, Peter H.
    JOURNAL OF MEDICINAL CHEMISTRY, 2022, 65 (01) : 838 - 856
  • [32] Development of Novel Brain-Penetrant Radioligands for PET Imaging of GABA Transporter-1
    Wang, Chao
    Gravel, Paul
    Zheng, Ming-Qiang
    Kapinos, Michael
    Emery, Paul
    Holden, Daniel
    Ropchan, Jim
    Borroni, Edilio
    Honer, Michael
    Gobbi, Luca
    Tamagnan, Gilles
    Carson, Richard
    Huang, Henry
    JOURNAL OF NUCLEAR MEDICINE, 2021, 62
  • [33] ERAS-801 IS A SELECTIVE BRAIN-PENETRANT EGFR INHIBITOR WITH IMPROVED ACTIVITY AGAINST EGFR EXTRACELLULAR DOMAIN-MUTANT GLIOBLASTOMA
    Okobi, Quincy
    Cadet, Dimitri
    Urner, Lorenz
    Jung, Michael
    Cloughesy, Timothy
    Nathanson, David
    NEURO-ONCOLOGY, 2024, 26
  • [34] ERAS-801: a selective brain-penetrant EGFR inhibitor with improved activity against EGFR extracellular domain-mutant glioblastoma
    Nathanson, D.
    Cadet, D.
    Okobi, Q.
    Urner, L.
    Jung, M.
    Cloughesy, T.
    EUROPEAN JOURNAL OF CANCER, 2024, 211 : S55 - S56
  • [35] Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei
    Cleghorn, Laura A. T.
    Albrecht, Sebastien
    Stojanovski, Laste
    Simeons, Frederick R. J.
    Norval, Suzanne
    Kime, Robert
    Collie, Iain T.
    De Rycker, Manu
    Campbell, Lorna
    Hallyburton, Irene
    Frearson, Julie A.
    Wyatt, Paul G.
    Read, Kevin D.
    Gilbert, Ian H.
    JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (19) : 7695 - 7706
  • [36] DEVELOPMENT OF HIGHLY POTENT, SELECTIVE BET BROMODOMAIN INHIBITORS THAT ARE CNS PENETRANT AND EFFECTIVE IN RODENT MODELS OF BRAIN CANCER
    Johnstone, Shawn
    Johhnsone, Andrea
    Penas, Clara
    Stathias, Vasileios
    Brothers, Shaun
    Ayad, Nagi
    Wahlestedt, Claes
    Albert, Jeffrey
    NEURO-ONCOLOGY, 2014, 16
  • [37] Development of highly potent, selective BET bromodomain inhibitors that are CNS penetrant and effective in rodent models of brain cancer
    Albert, Jeffrey
    Johnstone, Shawn
    Bayrakdarian, Malken
    Johnstone, Andrea
    Penas, Clara
    Stathias, Vasileios
    Brothers, Shaun
    Ayad, Nagi
    Wahlestedt, Claes
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2015, 250
  • [38] Brain-penetrant cyanoindane and cyanotetralin inhibitors of G2019S-LRRK2 kinase activity
    Garofalo, Albert W.
    Schwarz, Jacob
    Zobel, Kerry
    Beato, Claudia
    Bernardi, Silvia
    Budassi, Federica
    Caberlotto, Laura
    Gao, Peng
    Griffante, Cristiana
    Liu, Xinying
    Migliore, Marco
    Qiao, Feifei
    Sabbatini, Fabio Maria
    Sava, Anna
    Zhang, Mingliang
    Carlisle, Holly J.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2023, 95
  • [39] A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors
    Harrison, Justin R.
    Brand, Stephen
    Smith, Victoria
    Robinson, David A.
    Thompson, Stephen
    Smith, Alasdair
    Davies, Kenneth
    Mok, Ngai
    Torrie, Leah S.
    Collie, Iain
    Hallyburton, Irene
    Norval, Suzanne
    Simeons, Frederick R. C.
    Stojanovski, Laste
    Frearson, Julie A.
    Brenk, Ruth
    Wyatt, Paul G.
    Gilbert, Ian H.
    Read, Kevin D.
    JOURNAL OF MEDICINAL CHEMISTRY, 2018, 61 (18) : 8374 - 8389
  • [40] Discovery of Potent and Brain-Penetrant Bicyclic NLRP3 Inhibitors with Peripheral and Central In Vivo Activity
    Mammoliti, Oscar
    Carbajo, Rodrigo
    Perez-Benito, Laura
    Yu, Xiaodi
    Prieri, Marion L. C.
    Bontempi, Leonardo
    Embrechts, Sofie
    Paesmans, Ine
    Bassi, Michela
    Bhattacharya, Anindya
    Canellas, Santiago
    De Hoog, Saskia
    Demin, Samuel
    Gijsen, Harrie J. M.
    Hache, Geerwin
    Jacobs, Tom
    Jerhaoui, Soufyan
    Leenaerts, Joseph
    Lutter, Ferdinand H.
    Mahieu, Michel
    Matico, Rosalie
    Miller, Robyn
    Oehlrich, Daniel
    Perrier, Mathieu
    Ryabchuk, Pavel
    Schepens, Wim
    Sharma, Sujata
    Somers, Marijke
    Suarez, Javier
    Surkyn, Michel
    Van Opdenbosch, Nina
    Verhulst, Tinne
    Bottelbergs, Astrid
    JOURNAL OF MEDICINAL CHEMISTRY, 2025, 68 (04) : 4848 - 4887