Structure- based drug discovery of a selective, covalent KRas G12C inhibitor with oral activity in animal models of cancer

被引：0

作者：

Fischer, John ^{[1
]}

Baer, Brian ^{[1
]}

Ballard, Joshua ^{[1
]}

Blake, James ^{[1
]}

Bouhana, Karyn ^{[1
]}

Brandhuber, Barbara ^{[1
]}

Briere, David ^{[2
]}

Burgess, Laurence ^{[1
]}

Burkard, Michael ^{[1
]}

Chiang, Harrah ^{[2
]}

Chicarelli, Mark ^{[1
]}

Christensen, James ^{[2
]}

Davidson, Kevin ^{[1
]}

Gaudino, John ^{[1
]}

Hallin, Jill ^{[2
]}

Hanson, Lauren ^{[1
]}

Hee, Kenneth ^{[1
]}

Hicken, Erik ^{[1
]}

Hinklin, Ronald ^{[1
]}

Marx, Matthew ^{[2
]}

Mejia, Macedonio ^{[1
]}

Olson, Peter ^{[2
]}

Savechenkov, Pavel ^{[1
]}

Sudhakar, Niranjan ^{[2
]}

Tang, Tony ^{[1
]}

Vigers, Guy ^{[1
]}

Zecca, Henry ^{[1
]}

Fell, Jay ^{[1
]}

机构：

[1] Array Biopharma Inc, Boulder, CO USA

[2] Mirati Therapeut, San Diego, CA USA

来源：

ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY | 2018年 / 256卷

关键词：

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

144

引用

页数：1

共 50 条

[41] Developing KRAS G12C inhibitor-resistant tumor models for efficacy evaluation of next-generation anticancer therapies
Zhou, Jun
Ye, Zi
Bo, Ning
Zhang, Dan
Hua, Li
Nie, Chenpan
Wang, Jingjing
Kumari, Rajendra
Price, Leo
Xu, Xiaoxi
CANCER RESEARCH, 2023, 83 (07)
[42] Epithelial-to-Mesenchymal Transition is a Cause of Both Intrinsic and Acquired Resistance to KRAS G12C Inhibitor in KRAS G12C-Mutant Non-Small Cell Lung Cancer
Adachi, Yuta
Ito, Kentaro
Hayashi, Yuko
Kimura, Ryo
Tan, Tuan Zea
Yamaguchi, Rui
Ebi, Hiromichi
CLINICAL CANCER RESEARCH, 2020, 26 (22) : 5962 - 5973
[43] Preclinical studies of ZG19018, a novel irreversible covalent inhibitor of KRAS G12C, for the treatment of advanced nonsmall cell lung cancer and other solid tumors
Zhu, Bing
Cui, Dawei
Liu, Ruifeng
Feng, Weidong
Sheng, Zelin
Lv, Binhua
CANCER RESEARCH, 2023, 83 (07)
[44] CDX model based genome-scale CRISPR KO screens for modulators of KRAS (G12C) inhibitor sensitivity
Zhao, Haixin
Zhai, Fangzheng
Li, Bin
Fan, Qiangqiang
Peng, Zhengang
CANCER RESEARCH, 2023, 83 (07)
[45] Insight towards therapeutic susceptibility of KRAS mutant cancers from MRTX1257, a novel KRAS G12C mutant selective small molecule inhibitor
Christensen, James G.
Fell, Jay B.
Marx, Matthew A.
Fischer, John
Hallin, Jill
Calinisan, Andrew
Baer, Brian
Burkhard, Michael
Blake, James
Vigers, Guy
Aranda, Ruth
Hargis, Lauren
Briere, David
Engstrom, Lars
Olson, Peter
CANCER RESEARCH, 2019, 79 (13)
[46] Preliminary activity and safety results of KRAS G12C inhibitor glecirasib (JAB-21822) in patients with pancreatic cancer and other solid tumors.
Li, Jian
Shen, Lin
Gu, Yanhong
Calles, Antonio
Wu, Lin
Ba, Yi
Li, Zhi-hua
Bai, Chunmei
Yao, Yu
Hubert, Ayala
Perez, Julia Martinez
Zugazagoitia, Jon
Ding, Yuli
Liu, Sumei
Rao, Zhiyue
He, Zhiwen
JOURNAL OF CLINICAL ONCOLOGY, 2024, 42 (3_SUPPL) : 604 - 604
[47] Development of Patient-Derived Colorectal Cancer Xenograft and Organoid Models with Acquired Resistance to KRAS G12C Inhibitors
Hua, L.
Zheng, J.
Wang, J.
Shang, L.
Qian, W.
Sun, Y.
Bourre, L.
Wang, J.
EUROPEAN JOURNAL OF CANCER, 2024, 211 : S104 - S105
[48] Pan-tumor activity of olomorasib (LY3537982), a second-generation KRAS G12C inhibitor (G12Ci), in patients with KRAS G12C-mutant advanced solid tumors.
Heist, Rebecca Suk
Koyama, Takafumi
Murciano-Goroff, Yonina R.
Hollebecque, Antoine
Cassier, Philippe Alexandre
Han, Ji-Youn
Tosi, Diego
Sacher, Adrian G.
Burns, Timothy F.
Spira, Alexander I.
Gomez-Roca, Carlos A.
Shimizu, Toshio
Ammakkanavar, Natraj Reddy
Sabari, Joshua K.
Nagasaka, Misako
Fink, Aaron Alan
Chen, Aaron
Willard, Melinda D.
Oxnard, Geoffrey R.
Kuboki, Yasutoshi
JOURNAL OF CLINICAL ONCOLOGY, 2024, 42 (16)
[49] Discovery and characterization of ABSK071, a novel and potent small-molecule covalent inhibitor for KRAS-G12C
Guo, F.
Zhao, Y.
Yu, H.
Xu, Y.
Chen, Z.
Yang, S.
EUROPEAN JOURNAL OF CANCER, 2022, 174 : S22 - S23
[50] Discovery of novel Quinazoline-based KRAS G12C inhibitors as potential anticancer agents (vol 71, 116962, 2022)
Li, Ling
Zhao, Huiting
Peng, Xiaopeng
Liu, Jin
Mai, Ruiyao
Chen, Jingxuan
Lin, Lin
Chen, Ting
Yan, Jun
Shi, Jiaolong
Chen, Jianjun
BIOORGANIC & MEDICINAL CHEMISTRY, 2024, 111

← 1 2 3 4 5 →