Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

KRASG12C was recently identified to be potentially druggable by allele-specific covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP). Success of this approach requires active cycling of KRASG12C between its active-GTP and inactive-GDP conformations as accessib...

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Veröffentlicht in:	Cell 2018-01, Vol.172 (3), p.578-589.e17
Hauptverfasser:	Janes, Matthew R., Zhang, Jingchuan, Li, Lian-Sheng, Hansen, Rasmus, Peters, Ulf, Guo, Xin, Chen, Yuching, Babbar, Anjali, Firdaus, Sarah J., Darjania, Levan, Feng, Jun, Chen, Jeffrey H., Li, Shuangwei, Li, Shisheng, Long, Yun O., Thach, Carol, Liu, Yuan, Zarieh, Ata, Ely, Tess, Kucharski, Jeff M., Kessler, Linda V., Wu, Tao, Yu, Ke, Wang, Yi, Yao, Yvonne, Deng, Xiaohu, Zarrinkar, Patrick P., Brehmer, Dirk, Dhanak, Dashyant, Lorenzi, Matthew V., Hu-Lowe, Dana, Patricelli, Matthew P., Ren, Pingda, Liu, Yi
Format:	Artikel
Sprache:	eng
Schlagworte:	3D culture addiction Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use ARS-1620 Cell Proliferation - drug effects Cells, Cultured dependence Female G12C HCT116 Cells HEK293 Cells Humans KRAS Male Mice Mice, Inbred BALB C Mice, Nude Molecular Docking Simulation Mutation Neoplasms, Experimental - drug therapy NSCLC oncogene Piperazines - chemistry Piperazines - pharmacology Piperazines - therapeutic use Protein Binding Proto-Oncogene Proteins p21(ras) - antagonists & inhibitors Proto-Oncogene Proteins p21(ras) - genetics Proto-Oncogene Proteins p21(ras) - metabolism Quinazolines - chemistry Quinazolines - pharmacology Quinazolines - therapeutic use RAS
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