The discovery and preclinical characterization of the MTA cooperative PRMT5 inhibitor AM-9747

被引:0
|
作者
Belmontes, Brian [1 ]
Policheni, Antonia [1 ]
Liu, Siyuan [1 ]
Slemmons, Katherine [1 ]
Moriguchi, Jodi [1 ]
Ma, Hayley [1 ]
Aiello, Daniel [1 ]
Yang, Yajing [1 ]
Vestergaard, Mikkel [2 ]
Cowland, Sanne [2 ]
Anderson, Jan [2 ]
Sarvary, Ian [2 ]
Tamayo, Nuria [1 ]
Pettus, Liping [1 ]
Mukund, Susmith [3 ]
Pope, Leszek [1 ]
Allen, Jennifer R. [1 ]
Glad, Sanne [2 ]
Bourbeau, Matthew [1 ]
Hughes, Paul E. [1 ]
机构
[1] Amgen Inc, Thousand Oaks, CA USA
[2] Amgen Inc, Copenhagen, Denmark
[3] Amgen Inc, San Francisco, 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
1807
引用
收藏
页数:2
相关论文
共 50 条
  • [1] From DNA-Encoded Library Screening to AM-9747: An MTA-Cooperative PRMT5 Inhibitor with Potent Oral In Vivo Efficacy
    Sarvary, Ian
    Vestergaard, Mikkel
    Moretti, Loris
    Andersson, Jan
    Cadahia, Jorge Peiro
    Cowland, Sanne
    Flagstad, Thomas
    Franch, Thomas
    Gouliaev, Alex
    Husemoen, Gitte
    Jacso, Tomas
    Kronborg, Titi
    Kuropatnicka, Aleksandra
    Nadali, Anna
    Madsen, Mads
    Nielsen, Soren
    Pii, David
    Ryborg, Soren
    Soede, Camillia
    Allen, Jennifer R.
    Bourbeau, Matthew
    Li, Kexue
    Liu, Qingyian
    Lo, Mei-Chu
    Madoux, Franck
    Mardirossian, Narbe
    Moriguchi, Jodi
    Ngo, Rachel
    Peng, Chi-Chi
    Pettus, Liping
    Tamayo, Nuria
    Wang, Paul
    Kapoor, Rajiv
    Belmontes, Brian
    Caenepeel, Sean
    Hughes, Paul
    Liu, Siyuan
    Slemmons, Katherine K.
    Yang, Yajing
    Xie, Fang
    Ghimire-Rijal, Sudipa
    Mukund, Susmith
    Glad, Sanne
    JOURNAL OF MEDICINAL CHEMISTRY, 2025, 68 (06) : 6534 - 6557
  • [2] iscovery and characterization of an MTA-cooperative and brain-penetrant PRMT5 inhibitor
    Pan, Welling
    Wang, Hui
    Qi, Fangfei
    Deng, Haibing
    Yang, Fei
    Yu, Hongping
    Xu, Yao-Chang
    Chen, Zhui
    Ying, Haiyan
    MOLECULAR CANCER THERAPEUTICS, 2023, 22 (12)
  • [3] Preclinical characterization of ABSK131, a potential best-in-class MTA-cooperative PRMT5 inhibitor
    Pan, W.
    Wang, H.
    Qi, F.
    Deng, H.
    Yu, H.
    Xu, Y. C.
    Chen, Z.
    Ying, H.
    EUROPEAN JOURNAL OF CANCER, 2024, 211 : S17 - S18
  • [4] Discovery of AMG 193, an MTA-Cooperative PRMT5 Inhibitor for the Treatment of MTAP-Deleted Cancers
    Pettus, Liping H.
    Bourbeau, Matthew
    Tamayo, Nuria A.
    Amegadzie, Albert
    Beylkin, Diane
    Booker, Shon K.
    Butler, John
    Frohn, Michael J.
    Kaller, Matthew R.
    Kohn, Todd
    Lanman, Brian A.
    Li, Kexue
    Liu, Qingyian
    Ma, Vu
    Medina, Jose
    Minatti, Ana E.
    Lopez, Patricia
    Manoni, Francesco
    Pickrell, Alex
    Weires, Nicholas
    Andersson, Jan
    Cowland, Sanne
    Glad, Sanne
    Sarvary, Ian
    Vestergaard, Mikkel
    Li, Weikun
    Ghimire-Rijal, Sudipa
    Mardirossian, Narbe
    Mukund, Susmith
    Chen, Qing
    Lo, Mei-Chu
    Ngo, Rachel
    Khetan, Jawahar
    Madoux, Franck
    Sanders, Christiana
    Sharma, Pooja
    Wang, Paul
    Bruenner, Bernd
    Mccloud, Stuart
    Ponce, Manuel
    Soto, Marcus
    Wahlstrom, Jan
    Xie, Fang
    Yang, Yajing
    Liu, Siyuan
    Tan, Hong
    Policheni, Antonia
    Caenepeel, Sean
    Slemmons, Katherine K.
    Belmontes, Brian
    JOURNAL OF MEDICINAL CHEMISTRY, 2025,
  • [5] The discovery and preclinical characterization of AMG 193, a first-in-class MTA-cooperative PRMT5 inhibitor with broad activity against MTAP-null cancers
    Bojko-Matuszek, Agnieszka
    Kolakowski, Damian
    Bojko, Magdalena
    Sowinska, Aleksandra
    Mitula, Filip
    Lacek, Krzysztof
    Popiel, Delfina
    Kwiatkowski, Sebastian
    Kornatowski, Tomasz
    Kliszcz, Beata
    Jablonska, Anna
    Flis, Krzysztof
    Wiernicki, Bartosz
    Wieczorek, Maciej
    Pieczykolan, Jerzy
    Abramczyk, Olga
    MOLECULAR CANCER THERAPEUTICS, 2023, 22 (12)
  • [6] The discovery and preclinical characterization of the SAM-competitive PRMT5 inhibitor UCT-000445
    McDermott, Martina S.
    O'Brien, Neil A.
    O'Boyle, Brendan
    Bartberger, Michael
    Loson, Oliver C.
    Chau, Kevin
    Schwab, Ella
    Hong, Jenny
    Zhou, Jiaying
    Hu, Chuhong
    Luo, Tong
    Ayala, Raul
    Glasby, John
    Stoltz, Brian M.
    Slamon, Dennis J.
    CANCER RESEARCH, 2023, 83 (07)
  • [7] A review of the known MTA-cooperative PRMT5 inhibitors
    Hu, Mei
    Chen, Xiang
    RSC Advances, 2024, 14 (53) : 39653 - 39691
  • [8] Discovery of highly selective novel MTA-cooperative PRMT5 inhibitors for the treatment of cancers
    Wu, Wen-Lian
    Hu, Taishan
    Deng, Zhilin
    Li, Honghai
    Shen, Quanrong
    Zhang, Lei
    Ma, Xiaochu
    Sun, Peihua
    Cheng, Cindy
    Liu, Fang
    Chen, Xin
    Hua, Ye
    Huang, Bryan
    CANCER RESEARCH, 2024, 84 (06)
  • [9] TNG908, a brain-penetrant MTA-cooperative PRMT5 inhibitor, is efficacious in preclinical glioblastoma models
    Zhang, Minjie
    Tsai, Alice
    Cottrell, Kevin M.
    Haines, Brian B.
    Wilker, Erik
    DiBenedetto, Heather
    Weitzman, Ron
    Huang, Alan
    Davis, Charles B.
    Maxwell, John P.
    Briggs, Kimberly J.
    CANCER RESEARCH, 2023, 83 (07)
  • [10] Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity
    Smith, James M.
    Barlaam, Bernard
    Beattie, David
    Bradshaw, Lauren
    Chan, Ho Man
    Chiarparin, Elisabetta
    Collingwood, Olga
    Cooke, Sophie L.
    Cronin, Anna
    Cumming, Iain
    Dean, Emma
    Debreczeni, Judit E.
    del Barco Barrantes, Ivan
    Diene, Coura
    Gianni, Davide
    Guerot, Carine
    Guo, Xiaoxiao
    Guven, Sinem
    Hayhow, Thomas G.
    Hong, Ted
    Kemmitt, Paul D.
    Lamont, Gillian M.
    Lamont, Scott
    Lynch, James T.
    McWilliams, Lisa
    Moore, Shaun
    Raubo, Piotr
    Robb, Graeme R.
    Robinson, James
    Scott, James S.
    Srinivasan, Bharath
    Steward, Oliver
    Stubbs, Christopher J.
    Syson, Karl
    Tan, Lixiang
    Turner, Oliver
    Underwood, Elizabeth
    Urosevic, Jelena
    Vazquez-Chantada, Mercedes
    Whittaker, Amy L.
    Wilson, David M.
    Winter-Holt, Jon J.
    JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (16) : 13604 - 13638