Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors

Hyperactivation of mTOR kinase by mutations in the PI3K/mTOR pathway or by crosstalk with other mutant cancer drivers, such as RAS, is a feature of many tumors. Multiple allosteric inhibitors of mTORC1 and orthosteric dual inhibitors of mTORC1 and mTORC2 have been developed as anticancer drugs, but...

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Veröffentlicht in:	Journal of medicinal chemistry 2023-01, Vol.66 (1), p.149-169
Hauptverfasser:	Burnett, G. Leslie, Yang, Yu C., Aggen, James B., Pitzen, Jennifer, Gliedt, Micah K., Semko, Chris M., Marquez, Abby, Evans, James W., Wang, Gang, Won, Walter S., Tomlinson, Aidan C. A., Kiss, Gert, Tzitzilonis, Christos, Thottumkara, Arun P., Cregg, James, Mellem, Kevin T., Choi, Jong S., Lee, Julie C., Zhao, Yongyuan, Lee, Bianca J., Meyerowitz, Justin G., Knox, John E., Jiang, Jingjing, Wang, Zhican, Wildes, David, Wang, Zhengping, Singh, Mallika, Smith, Jacqueline A. M., Gill, Adrian L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Carcinoma, Non-Small-Cell Lung - drug therapy Cell Line, Tumor Cell Proliferation Drug Annotation Humans Lung Neoplasms - drug therapy Mechanistic Target of Rapamycin Complex 1 Mechanistic Target of Rapamycin Complex 2 Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Proto-Oncogene Proteins p21(ras) - metabolism TOR Serine-Threonine Kinases
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