A novel PRMT5 inhibitor with potent in vitro and in vivo activity in preclinical lung cancer models

被引:15
|
作者
Brehmer, Dirk
Wu, Tongfei
Mannens, Geert
Beke, Lijs
Vinken, Petra
Gaffney, Dana
Sun, Weimei
Pande, Vineet
Thuring, Jan-Willem
Millar, Hillary
Poggesi, Italo
Somers, Ivan
Boeckx, An
Parade, Marc
van Heerde, Erika
Nys, Thomas
Yanovich, Carol
Herkert, Barbara
Verhulst, Tinne
Du Jardin, Marc
Meerpoel, Lieven
Moy, Christopher
Diels, Gaston
Viellevoye, Marcel
Schepens, Wim
Poncelet, Alain
Linders, Joannes T.
Lawson, Edward C.
Edwards, James P.
Chetty, Dushen
Laquerre, Sylvie
Lorenzi, Matthew V.
机构
关键词
D O I
10.1158/1538-7445.AM2017-DDT02-04
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
DDT02-04
引用
收藏
页数:2
相关论文
共 50 条
  • [1] Identification of a First-in-Class PRMT5 Inhibitor with Potent in Vitro and in Vivo Activity in Preclinical Models of Mantle Cell Lymphoma
    Penebre, Elayne
    Kuplast, Kristy G.
    Majer, Christina R.
    Johnston, L. Danielle
    Rioux, Nathalie
    Munchhof, Michael
    Jin, Lei
    Boriak-Sjodin, P. Ann
    Wigle, Tim J.
    Jacques, Suzanne L.
    West, Kip A.
    Lingaraj, Trupti
    Stickland, Kimberly
    Ribich, Scott A.
    Raimondi, Alejandra
    Porter-Scott, Margaret
    Waters, Nigel J.
    Pollock, Roy M.
    Smith, Jesse J.
    Barbash, Olena
    Kruger, Ryan G.
    Copeland, Robert A.
    Moyer, Mikel P.
    Chesworth, Richard
    Duncan, Kenneth W.
    [J]. BLOOD, 2014, 124 (21)
  • [2] JNJ-64619178, a selective and pseudo-irreversible PRMT5 inhibitor with potent in vitro and in vivo activity, demonstrated in several lung cancer models
    Wu, Tongfei
    Millar, Hillary
    Gaffney, Dana
    Beke, Lijs
    Mannens, Geert
    Vinken, Petra
    Sommers, Ivan
    Thuring, Jan-Willem
    Sun, Weimei
    Moy, Christopher
    Pande, Vineet
    Zhou, Junguo
    Haddish-Berhane, Nahor
    Salvati, Mark
    Laquerre, Sylvie
    Lorenzi, Matthew V.
    Brehmer, Dirk
    [J]. CANCER RESEARCH, 2018, 78 (13)
  • [3] Preclinical characterization of PRT543, a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5), with broad antitumor activity in in vitro and in vivo models
    Bhagwat, Neha
    Zhang, Yang
    Lin, Hong
    Wang, Min
    Rominger, Dave
    Emm, Tom
    Chugani-Mahtani, Divya
    Angelis, Dimitrios
    Shetty, Rupa
    Leal, Raul
    Gowen-MacDonald, William
    Grego, Alexander
    Luengo, Juan
    Manshouri, Taghi
    Pastore, Friederike
    Levine, Ross L.
    Verstovsek, Srdan
    Ruggeri, Bruce
    Scherle, Peggy
    Vaddi, Kris
    [J]. CANCER RESEARCH, 2020, 80 (16)
  • [4] A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
    Chan-Penebre, Elayne
    Kuplast, Kristy G.
    Majer, Christina R.
    Boriack-Sjodin, P. Ann
    Wigle, Tim J.
    Johnston, L. Danielle
    Rioux, Nathalie
    Munchhof, Michael J.
    Jin, Lei
    Jacques, Suzanne L.
    West, Kip A.
    Lingaraj, Trupti
    Stickland, Kimberly
    Ribich, Scott A.
    Raimondi, Alejandra
    Scott, Margaret Porter
    Waters, Nigel J.
    Pollock, Roy M.
    Smith, Jesse J.
    Barbash, Olena
    Pappalardi, Melissa
    Ho, Thau F.
    Nurse, Kelvin
    Oza, Khyati P.
    Gallagher, Kathleen T.
    Kruger, Ryan
    Moyer, Mikel P.
    Copeland, Robert A.
    Chesworth, Richard
    Duncan, Kenneth W.
    [J]. NATURE CHEMICAL BIOLOGY, 2015, 11 (06) : 432 - +
  • [5] A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
    Chan-Penebre E.
    Kuplast K.G.
    Majer C.R.
    Boriack-Sjodin P.A.
    Wigle T.J.
    Johnston L.D.
    Rioux N.
    Munchhof M.J.
    Jin L.
    Jacques S.L.
    West K.A.
    Lingaraj T.
    Stickland K.
    Ribich S.A.
    Raimondi A.
    Scott M.P.
    Waters N.J.
    Pollock R.M.
    Smith J.J.
    Barbash O.
    Pappalardi M.
    Ho T.F.
    Nurse K.
    Oza K.P.
    Gallagher K.T.
    Kruger R.
    Moyer M.P.
    Copeland R.A.
    Chesworth R.
    Duncan K.W.
    [J]. Nature Chemical Biology, 2015, 11 (6) : 432 - 437
  • [6] In vivo efficacy and pharmacodynamic modulation of JNJ-64619178, a selective PRMT5 inhibitor, in human lung and hematologic preclinical models
    Millar, Hillary J.
    Brehmer, Dirk
    Verhulst, Tinne
    Haddish-Berhane, Nahor
    Greway, Tony
    Gaffney, Dana
    Boeckx, An
    Van Heerde, Erika
    Nys, Thomas
    Portale, Joseph
    Philippar, Ulrike
    Wu, Tongfei
    Laquerre, Sylvie
    Packman, Kathryn
    [J]. CANCER RESEARCH, 2019, 79 (13)
  • [7] Preclinical In vivo evaluation of efficacy, pharmacokinetics and pharmacodynamics of novel PRMT5 inhibitors in multiple tumor models
    Chikkanna, Dinesh
    Panigrahi, Sunil Kumar
    Rajagopalan, Sujatha
    Sammeta, Srinivasa Raju
    Chawla, Darshan
    Pavithra, S.
    Samiulla, D. S.
    Prasanna, Angelene
    Chand, Priyabrata
    Aithal, Kiran
    Marri, Sai Sudheer
    Kumar, Naveen
    Ganipisetty, Srinivasa Rao
    Mutyala, Raju
    Rao, Kasieswara
    Antony, Thomas
    Daginakatte, Girish
    Lakshminarasimhan, Anirudha
    Mohan, R.
    Narasihmarao, K.
    Chelur, Shekar
    Pandit, Chetan
    Samajdar, Susanta
    Ramachandra, Murali
    [J]. CANCER RESEARCH, 2018, 78 (13)
  • [8] LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity
    Bonday, Zahid Q.
    Cortez, Guillermo S.
    Grogan, Michael J.
    Antonysamy, Stephen
    Weichert, Ken
    Bocchinfuso, Wayne P.
    Li, Fengling
    Kennedy, Steven
    Li, Binghui
    Mader, Mary M.
    Arrowsmith, Cheryl H.
    Brown, Peter J.
    Eram, Mohammad S.
    Szewczyk, Magdalena M.
    Barsyte-Lovejoy, Dalia
    Vedadi, Masoud
    Guccione, Ernesto
    Campbell, Robert M.
    [J]. ACS MEDICINAL CHEMISTRY LETTERS, 2018, 9 (07): : 612 - 617
  • [9] Flavokawain A is a natural inhibitor of PRMT5 in bladder cancer
    Liu, Shuangjie
    Liu, Zhuonan
    Piao, Chiyuan
    Zhang, Zhe
    Kong, Chuize
    Yin, Lei
    Liu, Xi
    [J]. JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH, 2022, 41 (01)
  • [10] Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity
    Mcalpine, Indrawan J.
    Tatlock, John
    Billitti, Joseph
    Braganza, John
    Brooun, Alexei
    Deng Ya-Li
    Hirakawa, Brad
    Jensen-Pergakes, Kristen
    Kumpf, Robert
    Liu, Wei
    Maegley, Karen
    McTigue, Michele
    Patman, Ryan
    Rui, Eugene
    Scales, Stephanie
    Spiegel, Noah
    Tran-Dube, Michelle
    Wang, Fen
    Wang, Zhenxiong
    Yamazaki, Shinji
    Zhang, Tao
    Wythes, Martin
    [J]. CANCER RESEARCH, 2018, 78 (13)