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Discovery of Daraxonrasib (RMC-6236), a Potent and Orally Bioavailable RAS(ON) Multi-selective, Noncovalent Tri-complex Inhibitor for the Treatment of Patients with Multiple RAS-Addicted Cancers 发现Daraxonrasib (RMC-6236)，一种强效且口服生物利用度高的RAS(ON)多选择性、非共价三复合物抑制剂，用于治疗多种RAS成瘾性癌症患者。 Cregg, James; Edwards, Anne V.; Chang, Stephanie; Lee, Bianca J.; Knox, John E.; Tomlinson, Aidan C. A.; Marquez, Abby; Liu, Yang; Freilich, Rebecca; Aay, Naing; Wang, Yingyun; Jiang, Lingyan; Jiang, Jingjing; Wang, Zhican; Flagella, Michael; Wildes, David; Smith, Jacqueline A. M.; Singh, Mallika; Wang, Zhengping; Gill, Adrian L.; Koltun, Elena S. 分享 收藏
Translational Target Engagement Modeling of RMC-6291, a RAS(ON) G12C-selective, Covalent, Tri-Complex Inhibitor RMC-6291的转化靶点结合建模，RMC-6291是一种RAS(ON) G12C选择性、共价、三复合物抑制剂 Al-Radhawi, Muhammad Ali; Bao, Lei; Maldonato, Ben; Huang, Yue; Ly, Neang; Weller, Caroline; Yang, Yu chi; Jiang, Jingjing; Wildes, David; Wang, Zhican; Singh, Mallika; Wang, Zhengping 分享 收藏
Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers 在RAS驱动的癌症中通过RMC-6236抑制RAS-GTP的翻译和治疗评估 Jiang, Jingjing; Jiang, Lingyan; Maldonato, Benjamin J.; Wang, Yingyun; Holderfield, Matthew; Aronchik, Ida; Winters, Ian P.; Salman, Zeena; Blaj, Cristina; Menard, Marie; Brodbeck, Jens; Chen, Zhe; Wei, Xing; Rosen, Michael J.; Gindin, Yevgeniy; Lee, Bianca J.; Evans, James W.; Chang, Stephanie; Wang, Zhican; Seamon, Kyle J.; Parsons, Dylan; Cregg, James; Marquez, Abby; Tomlinson, Aidan C. A.; Yano, Jason K.; Knox, John E.; Quintana, Elsa; Aguirre, Andrew J.; Arbour, Kathryn C.; Reed, Abby; Gustafson, W. Clay; Gill, Adrian L.; Koltun, Elena S.; Wildes, David; Smith, Jacqueline A. M.; Wang, Zhengping; Singh, Mallika 分享 收藏
Discovery of RMC-9805, an oral, covalent tri-complex KRASG12D(ON) inhibitor Knox, John E.; Burnett, G. Leslie; Weller, Caroline; Jiang, Lingyan; Zhang, Dongyu; Vita, Nicole; Marquez, Abby; Seamon, Kyle J.; Gould, Andrea; Menard, Marie; Quintana, Elsa; Chen, Zhe; Wang, Zhican; Wang, Zhengping; Koltun, Elena S.; Singh, Malika; Jiang, Jingjing; Wildes, David; Smith, Jacqueline A. M.; Gill, Adrian L. 分享 收藏
RMC-5127, a first-in-class, orally bioavailable mutant- selective RASG12V( ON) inhibitor is central nervous system (CNS)-penetrant and demonstrates antitumor activity in a preclinical intracranial xenograft model Chen, Zhe; Eriksson, Andre; Lee, Bianca; Dinglasan, Jay; Montazer, Nilufar; Cregg, Jim; Edwards, Anne; Sanders, Kate; Smith, Jacqueline A.; Wildes, David; Singh, Mallika; Wang, Zhican; Jiang, Jingjing 分享 收藏
Combination RASG12C(ON) and RASMULTI(ON) inhibition overcomes resistance and prolongs durability in preclinical models of mutant KRASG12C-driven cancers Wei, Xing; Holderfield, Matthew; Yang, Yu Chi; Seamon, Kyle; Dinglasan, Jay; Montazar, Nilufar; Lee, Bianca; Cai, Shurui; Lai, Lick; Aronchik, Ida; Chang, Stephanie; Wang, Zhican; Wildes, Pete; Smith, Jacqueline A.; Jiang, Jingjing; Singh, Mallika 分享 收藏
Selective inhibition of the active state of KRASG12V with the non-covalent, tri-complex inhibitor RM-048 Lee, Bianca J.; Cregg, Jim; Edwards, Anne; Chen, Jerry; Eriksson, Andre; Tonogai, Emily; Tomlinson, Aidan; Seamon, Kyle; Ayala, Mariela Moreno; Shifrin, Nataliya Tovbis; Montazer, Nilufar; Sanders, Kate; Huang, Jun; Chou, Kang-Jye; Madej, Benjamin; Liu, Yang; Wang, Zhican; Wang, Zhengping; Knox, John; Koltun, Elena; Jiang, Jingjing; Gill, Adrian; Smith, Jacqueline A. M. 分享 收藏
First-in-human phase 1/1b trial of the first-in-class bi-steric mTORC1-selective inhibitor RMC-5552 in patients with advanced solid tumors Schram, Alison M.; Nagash, Abdul Rafeh; Haura, Eric B.; Riess, Jonathan W.; Ulahannan, Susanna V.; Ou, Sai-Hong I.; Capasso, Anna; Munster, Pamela N.; Cheng, Michael L.; Gustafson, W. Clay; Bitman, Bojena; Kar, Sumit; Wang, Zhican; Tao, Lin; Meyerowitz, Justin G.; Burns, Howard A. 分享 收藏
RM-046, a first-in-class, mutant-selective, and oral KRASQ61H(ON) inhibitor that drives tumor regression in preclinical models and validates KRASQ61H as a therapeutic target Yang, Yu C.; Thompson, Severin; Montgomery, David; Quinones, Antonio J.; Wei, Xing; Madej, Benjamin; Tomlinson, Aidan; Shifrin, Nataliya T.; McNamara, Alexander; Ahler, Ethan; McDowell, Laura L.; Flagella, Michael; Setser, John; Chang, Stephanie; Wang, Zhican; Wang, Zhengping; Huang, Jun; Ballmer, Steve; Li, Shaong; Buckl, Andreas; Koltun, Elena; Gill, Adrian; Jiang, Jingjing; Singh, Mallika; Smith, Jacqueline A. 分享 收藏
RMC-9805, a first-in-class, mutant-selective, covalent and oral KRASG12D(ON) inhibitor that induces apoptosis and drives tumor regression in preclinical models of KRASG12D cancers Jiang, Lingyan; Menard, Marie; Weller, Caroline; Wang, Zhican; Burnett, Les; Aronchik, Ida; Steele, Shelby; Flagella, Mike; Zhao, Ruiping; Evans, James W. W.; Chin, Shook; Chou, Kang-Jye; Mu, Yunming; Longhi, Michael; McDowell, Laura; Knox, John E.; Gill, Adrian; Smith, Jacqueline A.; Singh, Mallika; Quintana, Elsa; Jiang, Jingjing 分享 收藏
Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors mTORC1的选择性双空间抑制剂RMC-5552的发现，用于治疗mTORC1-Activated肿瘤 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. 分享 收藏
Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth (vol 17, pg 1065, 2021) Lee, Bianca J.; Boyer, Jacob A.; Burnett, G. Leslie; Thottumkara, Arun P.; Tibrewal, Nidhi; Wilson, Stacy L.; Hsieh, Tientien; Marquez, Abby; Lorenzana, Edward G.; Evans, James W.; Hulea, Laura; Kiss, Gert; Liu, Hui; Lee, Dong; Larsson, Ola; McLaughlan, Shannon; Topisirovic, Ivan; Wang, Zhengping; Wang, Zhican; Zhao, Yongyuan; Wildes, David; Aggen, James B.; Singh, Mallika; Gill, Adrian L.; Smith, Jacqueline A. M.; Rosen, Neal 分享 收藏
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Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth (Jun, 10.1038/s41589-021-00813-7, 2021) Lee, Bianca J.; Boyer, Jacob A.; Burnett, G. Leslie; Thottumkara, Arun P.; Tibrewal, Nidhi; Wilson, Stacy L.; Hsieh, Tientien; Marquez, Abby; Lorenzana, Edward G.; Evans, James W.; Hulea, Laura; Kiss, Gert; Liu, Hui; Lee, Dong; Larsson, Ola; McLaughlan, Shannon; Topisirovic, Ivan; Wang, Zhengping; Wang, Zhican; Zhao, Yongyuan; Wildes, David; Aggen, James B.; Singh, Mallika; Gill, Adrian L.; Smith, Jacqueline A. M.; Rosen, Neal 分享 收藏
Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth Lee, Bianca J.; Boyer, Jacob A.; Burnett, G. Leslie; Thottumkara, Arun P.; Tibrewal, Nidhi; Wilson, Stacy L.; Hsieh, Tientien; Marquez, Abby; Lorenzana, Edward G.; Evans, James W.; Hulea, Laura; Kiss, Gert; Liu, Hui; Lee, Dong; Larsson, Ola; McLaughlan, Shannon; Topisirovic, Ivan; Wang, Zhengping; Wang, Zhican; Zhao, Yongyuan; Wildes, David; Aggen, James B.; Singh, Mallika; Gill, Adrian L.; Smith, Jacqueline A. M.; Rosen, Neal 分享 收藏
Positioning a selective, bi-steric inhibitor of mTORC1 as a combination partner in RAS-driven cancers Yang, Yu Chi; Schulze, Christopher; Jiang, Jingjing; Reyes, Denise F.; Choy, Tiffany; Nguyen, Tram; Wang, Zhican; Lee, Dong; Nichols, Robert J.; Wang, Zhengping; Smith, Jacqueline A.; Kelsey, Steve M.; Singh, Mallika 分享 收藏
Vitamin D Metabolism Is Dysregulated in Asthma and Chronic Obstructive Pulmonary Disease Jolliffe, David A.; Stefanidis, Christos; Wang, Zhican; Kermani, Nazanin Z.; Dimitrov, Vassil; White, John H.; McDonough, John E.; Janssens, Wim; Pfeffer, Paul; Griffiths, Christopher J.; Bush, Andrew; Guo, Yike; Christenson, Stephanie; Adcock, Ian M.; Chung, Kian Fan; Thummel, Kenneth E.; Martineau, Adrian R. 分享 收藏
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