未登录NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound MutationsNVL-655是多种ALK突变癌蛋白的选择性和脑渗透性抑制剂,包括对氯拉替尼耐药的化合物突变
Lin, Jessica J.; Horan, Joshua C.; Tangpeerachaikul, Anupong; Swalduz, Aurelie; Valdivia, Augusto; Johnson, Melissa L.; Besse, Benjamin; Camidge, D. Ross; Fujino, Toshio; Yoda, Satoshi; Nguyen-Phuong, Linh; Mizuta, Hayato; Bigot, Ludovic; Nobre, Catline; Lee, Jii Bum; Yu, Mi Ra; Mente, Scot; Sun, Yuting; Kohl, Nancy E.; Porter, James R.; Shair, Matthew D.; Zhu, Viola W.; Felip, Enriqueta; Cho, Byoung Chul; Friboulet, Luc; Hata, Aaron N.; Pelish, Henry E.; Drilon, Alexander
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收藏A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis
Barrington, RE; Subler, MA; Rands, E; Omer, CA; Miller, PJ; Hundley, JE; Koester, SK; Troyer, DA; Bearss, DJ; Conner, MW; Gibbs, JB; Hamilton, K; Koblan, KS; Mosser, SD; O'Neill, TJ; Schaber, MD; Senderak, ET; Windle, JJ; Oliff, A; Kohl, NE
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收藏NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance MutationsNVL-520是ROS1融合和继发性耐药突变的选择性,TRK保留和脑渗透抑制剂
Drilon, Alexander; Horan, Joshua C.; Tangpeerachaikul, Anupong; Besse, Benjamin; Ou, Sai-Hong Ignatius; Gadgeel, Shirish M.; Camidge, D. Ross; Wekken, Anthonie J. van der; Nguyen-Phuong, Linh; Acker, Adam; Keddy, Clare; Nicholson, Katelyn S.; Yoda, Satoshi; Mente, Scot; Sun, Yuting; Soglia, John R.; Kohl, Nancy E.; Porter, James R.; Shair, Matthew D.; Zhu, Viola; Davare, Monika A.; Hata, Aaron N.; Pelish, Henry E.; Lin, Jessica J.
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收藏BBP-398, a potent, small molecule inhibitor of SHP2, enhances the response of established NSCLC xenografts to KRASG12C and mutEGFR inhibitors
Stice, James P.; Donovan, Sofia; Sun, Yuting; Kohl, Nancy; Czako, Barbara; Mseeh, Faika; Leonard, Paul; Wade, Anna; Lim, Justin; Jones, Phil; Wallace, Eli; Sinkevicius, Kerstin; Beltran, Pedro
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收藏Discovery of 6-[(3S,4S)-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor
Czako, Barbara; Sun, Yuting; McAfoos, Timothy; Cross, Jason B.; Leonard, Paul G.; Burke, Jason P.; Carroll, Christopher L.; Feng, Ningping; Harris, Angela L.; Jiang, Yongying; Kang, Zhijun; Kovacs, Jeffrey J.; Mandal, Pijus; Meyers, Brooke A.; Mseeh, Faika; Parker, Connor A.; Yu, Simon S.; Williams, Christopher C.; Wu, Qi; Di Francesco, Maria Emilia; Draetta, Giulio; Heffernan, Timothy; Marszalek, Joseph R.; Kohl, Nancy E.; Jones, Philip
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收藏Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib变构SHP2抑制剂,IACS-13909克服了对奥希替尼的EGFR依赖性和EGFR非依赖性耐药机制
Sun, Yuting; Meyers, Brooke A.; Czako, Barbara; Leonard, Paul; Mseeh, Faika; Harris, Angela L.; Wu, Qi; Johnson, Sarah; Parker, Connor A.; Cross, Jason B.; Di Francesco, Maria Emilia; Bivona, Benjamin J.; Bristow, Christopher A.; Burke, Jason P.; Carrillo, Caroline C.; Carroll, Christopher L.; Chang, Qing; Feng, Ningping; Gao, Guang; Gera, Sonal; Giuliani, Virginia; Huang, Justin K.; Jiang, Yongying; Kang, Zhijun; Kovacs, Jeffrey J.; Liu, Chiu-Yi; Lopez, Anastasia M.; Ma, Xiaoyan; Mandal, Pijus K.; McAfoos, Timothy; Miller, Meredith A.; Mullinax, Robert A.; Peoples, Michael; Ramamoorthy, Vandhana; Seth, Sahil; Spencer, Nakia D.; Suzuki, Erika; Williams, Christopher C.; Yu, Simon S.; Zuniga, Andy M.; Draetta, Giulio F.; Marszalek, Joseph R.; Heffernan, Timothy P.; Kohl, Nancy E.; Jones, Philip
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收藏First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant FGF19 Signaling as a Driver Event in Hepatocellular CarcinomaFisogatinib (BLU-554) 的首次人体I期研究验证了异常FGF19信号传导作为肝细胞癌的驱动事件
Kim, Richard D.; Sarker, Debashis; Meyer, Tim; Yau, Thomas; Macarulla, Teresa; Park, Joong-Won; Choo, Su Pin; Hollebecque, Antoine; Sung, Max W.; Lim, Ho-Yeong; Mazzaferro, Vincenzo; Trojan, Joerg; Zhu, Andrew X.; Yoon, Jung-Hwan; Sharma, Sunil; Lin, Zhong-Zhe; Chan, Stephen L.; Faivre, Sandrine; Feun, Lynn G.; Yen, Chia-Jui; Dufour, Jean-Francois; Palmer, Daniel H.; Llovet, Josep M.; Manoogian, Melissa; Tugnait, Meera; Stransky, Nicolas; Hagel, Margit; Kohl, Nancy E.; Lengauer, Christoph; Sherwin, Cori Ann; Schmidt-Kittler, Oleg; Hoeflich, Klaus P.; Shi, Hongliang; Wolf, Beni B.; Kang, Yoon-Koo
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收藏Discovery of IACS-13909, an allosteric SHP2 inhibitor that overcomes multiple mechanisms underlying osimertinib resistance
Sun, Yuting; Meyers, Brooke A.; Johnson, Sarah B.; Harris, Angela L.; Czako, Barbara; Cross, Jason B.; Leonard, Paul G.; Mseeh, Faika; Di Francesco, Maria E.; Parker, Connor A.; Wu, Qi; Bristow, Christopher A.; Burke, Jason P.; Carrillo, Caroline C.; Carroll, Christopher L.; Chang, Qing; Feng, Ningping; Gera, Sonal; Guang, Gao; Huang, Justin Kwang-Lay; Jiang, Yongying; Kang, Zhijun; Kovacs, Jeffrey J.; Ma, Xiaoyan; Mandal, Pijus K.; McAfoos, Timothy; Mullinax, Robert A.; Peoples, Michael D.; Ramamoorthy, Vandhana; Seth, Sahil; Suzuki, Erika; Williams, Christopher Conrad; Yu, Simon S.; Zuniga, Andy M.; Draetta, Giulio F.; Marszalek, Joseph R.; Heffernan, Timothy P.; Kohl, Nancy E.; Jones, Philip
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收藏A precision therapy against cancers driven by KIT/PDGFRA mutations
Evans, Erica K.; Gardino, Alexandra K.; Kim, Joseph L.; Hodous, Brian L.; Shutes, Adam; Davis, Alison; Zhu, Xing Julia; Schmidt-Kittler, Oleg; Wilson, Doug; Wilson, Kevin; DiPietro, Lucian; Zhang, Yulian; Brooijmans, Natasja; LaBranche, Timothy P.; Wozniak, Agnieszka; Gebreyohannes, Yemarshet K.; Schoffski, Patrick; Heinrich, Michael C.; DeAngelo, Daniel J.; Miller, Stephen; Wolf, Beni; Kohl, Nancy; Guzi, Timothy; Lydon, Nicholas; Boral, Andy; Lengauer, Christoph
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收藏The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi kinase inhibitors
Rahal, Rami; Evans, Erica K.; Hu, Wei; Maynard, Michelle; Fleming, Paul; DiPietro, Lucian; Kim, Joseph L.; Sheets, Michael P.; Wilson, Doug P.; Wilson, Kevin J.; Stransky, Nicolas; Brubaker, Jason D.; Guzi, Timothy; Kohl, Nancy E.; Lengauer, Christoph
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收藏BLU-285, the first selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants
Evans, Erica K.; Hodous, Brian L.; Gardino, Alexandra K.; Davis, Alison; Zhu, Julia; Shutes, Adam; Kim, Joseph L.; Wilson, Kevin J.; Wilson, Doug; Zhang, Yulian; Chu, Tat; Kohl, Nancy E.; Kadambi, Vivek; Guzi, Timothy; Lengauer, Christoph
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收藏First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway
Hagel, Margit; Miduturu, Chandra; Sheets, Michael; Rubin, Nooreen; Weng, Weifan; Stransky, Nicolas; Bifulco, Neil; Kim, Joseph L.; Hodous, Brian; Brooijmans, Natasja; Shutes, Adam; Winter, Christopher; Lengauer, Christoph; Kohl, Nancy E.; Guzi, Timothy
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收藏FIRST SELECTIVE SMALL MOLECULE INHIBITOR OF FGFR4 FOR THE TREATMENT OF HEPATOCELLULAR CARCINOMAS WITH AN ACTIVATED FGFR4 SIGNALING PATHWAY
Hoeflich, K.; Hagel, M.; Miduturu, C.; Sheets, M.; Rubin, N.; Weng, W.; Stransky, N.; Bifulco, N.; Kim, J.; Hodous, B.; Brooijmans, N.; Shutes, A.; Winter, C.; Lengauer, C.; Kohl, N.; Guzi, T.
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收藏IMMUNE CHECKPOINT BLOCKADE FOR GLIOBLASTOMA: PRECLINICAL ACTIVITY OF SINGLE AGENT AND COMBINATORIAL THERAPY
Reardon, David; Gokhale, Prafulla; Ligon, Keith; Liao, Xiaoyun; Rodig, Scott; Zhou, Jun; Qin, Lei; Hodi, Stephen; Jones, Kristen; Sauer, Amy; Kohl, Nancy; Dranoff, Glenn; Freeman, Gordon
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收藏Selinexor (KPT-330), a novel selective inhibitor of nuclear export (SINE), shows single agent efficacy against alveolar soft part sarcoma (ASPS) in vivo
Crochiere, Marsha L.; Kashyap, Trinayan; Klebanov, Boris; Senapedis, William; del Alamo, Diego; Tamir, Sharon; Baloglu, Erkan; McCauley, Dilara; Carlson, Robert; Kauffman, Michael; Shacham, Sharon; Demetri, George; Wagner, Andrew; Sicinska, Ewa; Gokhale, Prafulla; Kohl, Nancy; Saur, Amy; Landesman, Yosef
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收藏High-Throughput Tyrosine Kinase Activity Profiling Identifies FAK as a Candidate Therapeutic Target in Ewing Sarcoma
Crompton, Brian D.; Carlton, Anne L.; Thorner, Aaron R.; Christie, Amanda L.; Du, Jinyan; Calicchio, Monica L.; Rivera, Miguel N.; Fleming, Mark D.; Kohl, Nancy E.; Kung, Andrew L.; Stegmaier, Kimberly
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收藏PDK1 Attenuation Fails to Prevent Tumor Formation in PTEN-Deficient Transgenic Mouse Models
Ellwood-Yen, Katharine; Keilhack, Heike; Kunii, Kaiko; Dolinski, Brian; Connor, Yamicia; Hu, Kun; Nagashima, Kumiko; O'Hare, Erin; Erkul, Yusuf; Di Bacco, Alessandra; Gargano, Diana; Shomer, Nirah H.; Angagaw, Minilik; Leccese, Erica; Andrade, Paula; Hurd, Melissa; Shin, Myung K.; Vogt, Thomas F.; Northrup, Alan; Bobkova, Ekaterina V.; Kasibhatla, Shailaja; Bronson, Roderick T.; Scott, Martin L.; Draetta, Giulio; Richon, Victoria; Kohl, Nancy; Blume-Jensen, Peter; Andersen, Jannik N.; Kraus, Manfred
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