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

[31] Remodeling of the tumor/tumor microenvironment ecosystem during KRAS G12C inhibitor clinical resistance in lung cancer
Manabe, Tadashi
Bivona, Trever G.
JOURNAL OF CLINICAL INVESTIGATION, 2022, 132 (04):
[32] Real-time monitoring of the reaction of KRAS G12C mutant specific covalent inhibitor by in vitro and in-cell NMR spectroscopy
Zhao, Qingci
Haga, Ryoka
Tamura, Satoko
Shimada, Ichio
Nishida, Noritaka
SCIENTIFIC REPORTS, 2023, 13 (01)
[33] Efficacy and safety of LY3537982, a potent and highly selective KRAS G12C inhibitor in KRAS G12C-mutant GI cancers: Results from a phase 1 study
Kuboki, Yasutoshi
Murciano-Goroff, Yonina R.
Yaeger, Rona
Cassier, Philippe Alexandre
Heist, Rebecca Suk
Fujiwara, Yutaka
Deming, Dustin A.
Ammakkanavar, Natraj
Patnaik, Amita
Shimizu, Toshio
Call, Justin
Han, Sae-Won
Fink, Aaron Alan
Chen, Aaron
Willard, Melinda D.
Balar, Arjun Vasant
Koyama, Takafumi
JOURNAL OF CLINICAL ONCOLOGY, 2024, 42 (3_SUPPL) : 94 - 94
[34] Real-time monitoring of the reaction of KRAS G12C mutant specific covalent inhibitor by in vitro and in-cell NMR spectroscopy
Qingci Zhao
Ryoka Haga
Satoko Tamura
Ichio Shimada
Noritaka Nishida
Scientific Reports, 13
[35] JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic properties in preclinical models
Brachmann, Saskia M.
Weiss, Andreas
Guthy, Daniel A.
Beyer, Kim
Voshol, Johannes
Maira, Michel
Prahallad, Anirudh
Porta, Diana Graus
Schnell, Christian
Ostermann, Nils
Vaupel, Andrea
Gerspacher, Marc
Leblanc, Catherine
Erdmann, Dirk
Sterker, Dario
Kerr, Grainne
Jerome, Giovannoni
Head, Victoria
Stringer, Rowan
De Kanter, Ruben
Jeff, Kearns
Roman, Danielle
Widmer, Toni
Wessels, Peter
Nunez, Eloisa Jimenez
Sedrani, Richard
Zecri, Frederic
Hofmann, Francesco
Engleman, Jeff
Lorthiois, Edwige
Cotesta, Simona
MOLECULAR CANCER THERAPEUTICS, 2021, 20 (12)
[36] GTPase KRAS (G12C mutant) inhibitor Treatment of non-small cell lung cancer Treatment of colorectal cancer
Shao, Shi-yun
Rong, Wen-qing
Talukder, Salehikram
Jia, Ru
Chen, Zhe-Sheng
DRUGS OF THE FUTURE, 2022, 47 (11) : 783 - 795
[37] Elucidating the mechanisms of acquired resistance to AMG510 in cancer models harboring KRAS G12C mutations
Ni, Ting
Huo, Tongxin
Zhang, Yawen
Wang, Jingjing
Liu, Gaoxiang
Shi, Wenting
Gu, Qingyang
CANCER RESEARCH, 2024, 84 (06)
[38] Secondary KRAS G12C Mutation and Acquired BRAF Inhibitor Resistance in a Patient with Papillary Thyroid Cancer: A Case Report
Sham, S.
Bendari, A.
Seetharamu, N.
Vele, O.
JOURNAL OF MOLECULAR DIAGNOSTICS, 2023, 25 (11): : S136 - S136
[39] Investigation of KRAS G12C inhibitor JAB-21822 as a single agent and in combination with SHP2 inhibitor JAB-3312 in preclinical cancer models
Wang, P.
Zheng, Q.
Kang, D.
Sun, X.
Zhu, S.
Wang, Y.
Long, W.
Lin, Y.
ANNALS OF ONCOLOGY, 2022, 33 : S1441 - S1441
[40] A first-in-human phase 1 study of LY3537982, a highly selective and potent KRAS G12C inhibitor in patients with KRAS G12C-mutant advanced solid tumors
Murciano-Goroff, Yonina R.
Heist, Rebecca S.
Kuboki, Yasutoshi
Koyama, Takafumi
Ammakkanavar, Natraj Reddy
Hollebecque, Antoine
Patnaik, Amita
Shimizu, Toshio
Spira, Alexander I.
Nagasaka, Misako
Han, Ji-Youn
Iams, Wade Thomas
Deming, Dustin
Call, Justin
Cassier, Philippe
Han, Sae-Won
Chu, Quincy Siu-Chung
Cosman, Rasha
Durm, Gregory
Burns, Timothy
Willard, Melinda D.
Liu, Shiyao
Callies, Sophie
Balar, Arjun V.
Sabari, Joshua K.
CANCER RESEARCH, 2023, 83 (08)

← 1 2 3 4 5 →