Discovery and characterization of AZ6197, a potent and selective ERK1/2 inhibitor

被引:0
|
作者
Flemington, Vikki [1 ]
Simpson, Iain [1 ]
Davies, Emma [1 ]
Robinson, David [1 ]
Lindsay, Nicola [1 ]
Hanson, Lyndsey [1 ]
Hopcroft, Philip [1 ]
Tonge, Michael [1 ]
Roberts, Karen [1 ]
Ward, Richard [1 ]
机构
[1] AstraZeneca, Cambridge, England
关键词
D O I
10.1158/1535-7163.TARG-17-B156
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
B156
引用
收藏
页数:2
相关论文
共 50 条
  • [1] Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development
    Robarge, Kirk
    Schwarz, Jacob
    Blake, Jim
    Burkard, Michael
    Chan, Jocelyn
    Chen, Huifen
    Chou, Kang-Jye
    Diaz, Dolores
    Gaudino, John
    Gould, Stephen
    Grina, Jonas
    Xin Linghu
    Liu, Lichuan
    Martinson, Matthew
    Moreno, David A.
    Orr, Christine
    Pacheco, Patricia
    Qin, Ann
    Rasor, Kevin
    Ren, Li
    Shahidi-Latham, Sheerin
    Stults, Jeffrey
    Sullivan, Francis
    Wang, Weiru
    Yin, Peter
    Zhou, Aihe
    Belvin, Marcia
    Merchant, Mark
    Moffat, John G.
    [J]. CANCER RESEARCH, 2014, 74 (19)
  • [2] Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development
    Schwarz, Jacob
    Blake, James
    Burkard, Michael
    Chan, Jocelyn
    Chen, Huifen
    Chou, Kang-Jye
    Diaz, Dolores
    Dudley, Danette
    Gaudino, John
    Gould, Stephen
    Grina, Jonas
    Hunsaker, Thomas
    Liu, Lichuan
    Martinson, Matthew
    Moreno, David
    Orr, Christine
    Pacheco, Patricia
    Qin, Ann
    Rasor, Kevin
    Ren, Li
    Robarge, Kirk
    Shahidi-Latham, Sheerin
    Stults, Jeffrey
    Sullivan, Francis
    Wang, Weiru
    Yin, Jianping
    Zhou, Aihe
    Belvin, Marcia
    Merchant, Mark
    Moffat, John
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2016, 252
  • [3] Discovery of potent and selective inhibitors of ERK1/2 with a unique mechanism of action
    Deng, Yongqi
    Samatar, Ahmed
    Shipps, Gerald
    Cooper, Alan
    Long, Brian
    Carr, Donnar
    Xiao, Li
    Hruza, Alan
    Wang, Tong
    Zhu, Liang
    Nan, Yang
    Patel, Mehul
    Muppalla, Kiran
    Zhu, Hugh
    Boga, Babu Sobhana
    Gao, Xiaolei
    [J]. CANCER RESEARCH, 2016, 76
  • [4] Discovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2
    Ren, Li
    Grina, Jonas
    Moreno, David
    Blake, James F.
    Gaudino, John J.
    Garrey, Rustam
    Metcalf, Andrew T.
    Burkard, Michael
    Martinson, Matthew
    Rasor, Kevin
    Chen, Huifen
    Dean, Brian
    Gould, Stephen E.
    Pacheco, Patricia
    Shahidi-Latham, Sheerin
    Yin, Jianping
    West, Kristina
    Wang, Weiru
    Moffat, John G.
    Schwarz, Jacob B.
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (04) : 1976 - 1991
  • [5] Discovery and characterization of AZ285 as a potent and selective inhibitor of CK2 kinase
    Dowling, James E.
    Alimzhanov, Marat
    Bao, Larry
    Brassil, Patrick
    Cooke, Emma L.
    Denz, Christopher R.
    Liu, Zhong-Ying
    Ye, Qing
    Lyne, Paul D.
    [J]. CANCER RESEARCH, 2012, 72
  • [6] Fragment-based discovery of a highly potent, orally bioavailable ERK1/2 inhibitor that modulates the phosphorylation and catalytic activity of ERK1/2
    Heightman, Tom D.
    Berdini, Valerio
    Braithwaite, Hannah
    Buck, Ildiko
    Cassidy, Megan
    Castro, Juan
    Courtin, Aurelie
    Day, James
    East, Charlotte
    Fazal, Lynsey
    Graham, Brent
    Griffiths-Jones, Charlotte
    Lyons, John
    Martins, Vanessa
    Muench, Sandra
    Munck, Joanne
    Norton, David
    O'Reilly, Marc
    Palmer, Nick
    Pathuri, Puja
    Reader, Mike
    Rees, David
    Rich, Sharna
    Richardson, Caroline
    Saini, Harpreet
    Thompson, Neil
    Wallis, Nicola
    Walton, Hugh
    Wilsher, Nicola
    Woolford, Alison
    Murray, Chris
    [J]. MOLECULAR CANCER THERAPEUTICS, 2018, 17 (01)
  • [7] Preclinical characterization of HMPL-295, a potent and selective ERK 1/2 inhibitor
    Hu, Jia
    Ni, Jun
    Lv, Yuanzhi
    Li, Wenjun
    Zhang, Hui
    Li, Xin
    Yu, Ying
    Zhong, Zeyu
    Wang, Jian
    Sai, Yang
    Qing, Weiguo
    Ren, Yongxin
    Shi, Michael
    Su, Weiguo
    [J]. CANCER RESEARCH, 2024, 84 (06)
  • [8] Discovery of AZD0364, a potent and selective oral inhibitor of ERK1/2 that is efficacious in both monotherapy and combination therapy in models of NSCLC
    Simpson, Iain
    Anderton, Mark J.
    Andrews, David M.
    Breed, Jason
    Davies, Emma
    Debreczeni, Judit E.
    Flemington, Vikki
    Gibbons, Francis D.
    Graham, Mark A.
    Hopcroft, Philip
    Howard, Tina
    Hudson, Julian
    Jones, Clifford D.
    Jones, Christopher
    Lindsay, Nicola
    Pease, J. Elizabeth
    Rawlins, Philip
    Roberts, Karen
    Swallow, Steve
    St-Gallay, Steve
    Tonge, Michael E.
    Ward, Richard A.
    [J]. CANCER RESEARCH, 2018, 78 (13)
  • [9] Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations
    Bhagwat, Shripad V.
    McMillen, William T.
    Cai, Shufen
    Zhao, Baohui
    Whitesell, Matthew
    Kindler, Lisa
    Flack, Robert S.
    Wu, Wenjuan
    Huss, Karen
    Anderson, Bryan
    Yuan, Xiu-Juan
    Jaken, Susan
    McCann, Denis
    Mathes, Brian
    Dropsey, Andrew J.
    Manro, Jason
    Walgren, Jennie
    Yuen, Eunice
    Gong, Xueqian
    Rodriguez, Michael J.
    Huang, Jianping
    Tiu, Ramon V.
    Joseph, Sajan
    Peng, Sheng-Bin
    [J]. CANCER RESEARCH, 2017, 77
  • [10] Characterization of a novel ERK1/2 inhibitor, which modulates the phosphorylation and catalytic activity of ERK1/2
    Munck, Joanne M.
    Berdini, Valerio
    Bevan, Luke D.
    Braithwaite, Hannah
    Buck, Ildiko M.
    Cassidy, Megan
    Castro, Juan
    Courtin, Aurelie
    Day, James E.
    East, Charlotte
    Fazal, Lynsey
    Graham, Brent
    Griffiths-Jones, Charlotte M.
    Heightman, Tom D.
    Hindley, Chris J.
    Kidane, Birikiti
    Kucia-Tran, Justyna
    Lyons, John F.
    Martins, Vanessa
    Muench, Sandra
    Murray, Chris W.
    Norton, David
    O'Reilly, Marc
    Palmer, Nick
    Pathuri, Puja
    Reader, Mike
    Rees, David C.
    Rich, Sharna J.
    Richardson, Caroline J.
    Saini, Harpreet K.
    Shah, Alpesh
    Stanczuk, Lukas
    Thompson, Neil T.
    Walton, Hugh
    Wilsher, Nicola E.
    Woolford, Alison J.
    Wallis, Nicola G.
    [J]. MOLECULAR CANCER THERAPEUTICS, 2018, 17 (01)