Evaluation of the impact of homozygous MTAP truncations on the activity and selectivity of MTA-cooperative PRMT5 inhibitors

被引：0
|
作者：
Tonini, Matthew R.
Mignault, Andre A.
Whittington, Douglas A.
Lombardo, Steven A.
Shen, Binzhang
Stowe, Hannah
Yoda, Satoshi
Liu, Shangtao
Zhang, Minjie
Cottrell, Kevin M.
Meier, Samuel R.
Rego, Heidi
Morawiak, Jennifer
Hooper, Ellen
Yu, Yi
DiBenedetto, Heather
Crystal, Adam S.
Teng
Briggs, Kimberly
机构：
来源：
CANCER RESEARCH | 2024年 / 84卷 / 06期
关键词：
D O I：
10.1158/1538-7445.AM2024-4631
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
4631
引用
收藏
页数：2
相关论文
共 50 条
  • [31] TNG462 is a potential best-in-class MTA-cooperative PRMT5 inhibitor for the treatment of peripheral MTAP-deleted solid tumors
    Briggs, K.
    Tsai, A.
    Zhang, M.
    Tonini, M.
    Haines, B.
    Huang, A.
    Cottrell, K.
    EUROPEAN JOURNAL OF CANCER, 2022, 174 : S84 - S84
  • [32] TNG908, A BRAIN-PENETRANT MTA-COOPERATIVE PRMT5 INHIBITOR, IS EFFICACIOUS IN PRECLINICAL MTAP-DELETED MODELS INCLUDING GLIOBLASTOMA
    Zhang, Minjie
    Tsai, Alice
    Cottrell, Kevin
    Wilker, Erik
    Davis, Charles
    DiBenedetto, Heather
    Weitzman, Ron
    Huang, Alan
    Maxwell, John
    Briggs, Kimberly
    NEURO-ONCOLOGY, 2023, 25
  • [33] MRTX1719: A first-in-class MTA-cooperative PRMT5 inhibitor that selectively elicits antitumor activity in MTAP/CDKN2A deleted cancer models
    Smith, Christopher R.
    Engstrom, Lars D.
    Kulyk, Svitlana
    Aranda, Ruth
    Waters, Laura
    Moya, Krystal
    Bowcut, Victoria
    Hebbert, Allan
    Trinh, David
    Briere, David M.
    Lawson, J. David
    Clarine, Jeff
    Rahbaek, Lisa
    Christensen, James G.
    Marx, Matthew A.
    Olson, Peter
    MOLECULAR CANCER THERAPEUTICS, 2021, 20 (12)
  • [34] 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
  • [35] PRIMROSE: A modular phase 1/2a study of AZD3470, an MTA-cooperative PRMT5 inhibitor, in patients with MTAP deficient advanced solid tumors.
    Spira, Alexander I.
    Lau, James
    Hattersley, Maureen M.
    Aronson, Boaz E.
    Peters, Jane
    Soo-Hoo, Yee
    Sawant, Aarti
    Loizou, Joanna
    Smith, Claire
    Dean, Emma
    Postel-Vinay, Sophie
    Solomon, Benjamin J.
    JOURNAL OF CLINICAL ONCOLOGY, 2024, 42 (16)
  • [36] Phase I dose escalation and initial dose expansion results of AMG 193: A MTA-cooperative PRMT5 inhibitor, in patients (pts) with MTAP-deleted solid tumors
    Sacher, A. G.
    Villalona-Calero, M.
    O'Neil, B. H.
    Rodon, J.
    Doi, T.
    Postel-Vinay, S.
    Ghiringhelli, F.
    Yamamoto, N.
    Wahlroos, S.
    Villaruz, L.
    El-Helali, A.
    Fujiwara, Y.
    Addeo, A.
    Lin, C-C.
    Fontana, E.
    Chuang, C-H.
    Liu, C.
    Eggert, T.
    Penel, N.
    Prenen, H.
    ANNALS OF ONCOLOGY, 2024, 35 : S484 - S485
  • [37] 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)
  • [38] First disclosure of AZD3470, a highly potent MTA-cooperative PRMT5 inhibitor in PRIMROSE and PRIMAVERA clinical studies
    Smith, J.
    Urosevic, J.
    Moore, S.
    Magiera, L.
    Bradshaw, L.
    Gianni, D.
    Srinivasan, B.
    Debreczeni, J.
    Stubbs, C.
    Vazquez-Chantada, M.
    Hong, T.
    Cronin, A.
    Khan, K.
    Wiseman, E.
    Ferguson, D.
    Lynch, J.
    Chan, H. M.
    Critchlow, S.
    Fawell, S.
    Dean, E.
    EUROPEAN JOURNAL OF CANCER, 2024, 211 : S59 - S60
  • [39] Discovery of Potent, Highly Selective, and Orally Bioavailable MTA Cooperative PRMT5 Inhibitors with Robust In Vivo Antitumor Activity
    Zhang, Meng
    Ding, Xiaoyu
    Cao, Zhongying
    Yang, Yilin
    Ding, Xiao
    Cai, Xin
    Zhang, Man
    Aliper, Alex
    Ren, Feng
    Lu, Hongfu
    Zhavoronkov, Alex
    JOURNAL OF MEDICINAL CHEMISTRY, 2025, 68 (02) : 1940 - 1955
  • [40] First-in-human study of AMG 193, an MTA-cooperative PRMT5 inhibitor, in patients with MTAP-deleted solid tumors: results from phase I dose exploration5
    Rodon, J.
    Prenen, H.
    Sacher, A.
    Villalona-Calero, M.
    Penel, N.
    El Helali, A.
    Rottey, S.
    Yamamoto, N.
    Ghiringhelli, F.
    Goebeler, M. E.
    Doi, T.
    Postel-Vinay, S.
    Lin, C. -c.
    Liu, C.
    Chuang, C. -h.
    Keyvanjah, K.
    Eggert, T.
    Neil, B. h. o '
    ANNALS OF ONCOLOGY, 2024, 35 (12) : 1138 - 1147
12345