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收藏分享 收藏 分享 收藏 分享 收藏 A small-molecule inhibitor of WRN selectively kills MSI-H cancer cells and phenocopies WRN genetic defects
Rao, Yanhua; Srivatsan, Anjana; Liimatta, Marya; Munoz, Diana; Quirit, Jeanne; Shi, Jianxia; Nguyen, An; Xin Linghu; Federowicz, Federowicz; Jones, Brian; Fleury, Melissa; Newby, Zach; Dillon, Michael P.; Barsanti, Paul A.; Lackner, Mark R.; White, Michael A.; Lee, Yang; Landis, Phil; Peng, Yang; Cicchini, Michelle; Cottom, Josh; Nickels, Leng; Brnardic, Ed; DeMartino, Michael; Taygerly, Josh 分享 收藏 Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced MalignanciesHuang, Ying; Sendzik, Martin; Zhang, Jeff; Gao, Zhenting; Sun, Yongfeng; Wang, Long; Gu, Justin; Zhao, Kehao; Yu, Zhengtian; Zhang, Lijun; Zhang, Qiong; Blanz, Joachim; Chen, Zijun; Dubost, Valerie; Fang, Douglas; Feng, Lijian; Fu, Xingnian; Kiffe, Michael; Li, Ling; Luo, Fangjun; Luo, Xiao; Mi, Yuan; Mistry, Prakash; Pearson, David; Piaia, Alessandro; Scheufler, Clemens; Terranova, Remi; Weiss, Andreas; Zeng, Jue; Zhang, Hailong; Zhang, Jiangwei; Zhao, Mengxi; Dillon, Michael P.; Jeay, Sebastien; Qi, Wei; Moggs, Jonathan; Pissot-Soldermann, Carole; Li, En; Atadja, Peter; Lingel, Andreas; Oyang, Counde 分享 收藏 分享 收藏 分享 收藏 分享 收藏 分享 收藏 In vitro and in vivo characterization of novel MAT2A allosteric inhibitorsPei, Zhonghua; Alam, Muzaffar; Bhola, Neil; Cleary, Leah; Drummond, Jake; Fisher, Marcus; Fleury, Melissa; Garcia, Candy; Givmanesh, Atieh; Xin Linghu; McSpadden, Ethan; Mounir, Zineb; Neilan, Claire; Newby, Zach; Perumal, Senthil; Steel, Richard; Sutton, James; Vaidya, Kedar; Wagle, Marie-Claire; Wang, Jianhong; Yao, Bing; Lackner, Mark; Dillon, Michael P. 分享 收藏 Discovery of Potent and Selective Antibody-Drug Conjugates with Eg5 Inhibitors through Linker and Payload Optimization通过接头和有效载荷优化发现具有Eg5抑制剂的有效和选择性抗体-药物缀合物Karpov, Alexei S.; Nieto-Oberhuber, Cristina M.; Abrams, Tinya; Beng-Louka, Edwige; Blanco, Enrique; Chamoin, Sylvie; Chene, Patrick; Dacquignies, Isabelle; Daniel, Dylan; Dillon, Michael P.; Doumampouom-Metoul, Lionel; Drosos, Nikolaos; Fedoseev, Pavel; Furegati, Markus; Granda, Brian; Grotzfeld, Robert M.; Clark, Suzanna Hess; Joly, Emilie; Jones, Darryl; Lacaud-Baumlin, Marion; Lagasse-Guerro, Stephanie; Lorenzana, Edward G.; Mallet, William; Martyniuk, Piotr; Marzinzik, Andreas L.; Mesrouze, Yannick; Nocito, Sandro; Oei, Yoko; Perruccio, Francesca; Piizzi, Grazia; Richard, Etienne; Rudewicz, Patrick J.; Schindler, Patrick; Velay, Melanie; Venstrom, Kristine; Wang, Peiyin; Zurini, Mauro; Lafrance, Marc 分享 收藏 分享 收藏 分享 收藏 Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the ClinicRamurthy, Savithri; Taft, Benjamin R.; Aversa, Robert J.; Barsanti, Paul A.; Burger, Matthew T.; Lou, Yan; Nishiguchi, Gisele A.; Rico, Alice; Setti, Lina; Smith, Aaron; Subramanian, Sharadha; Tamez, Victoriano; Tanner, Huw; Wan, Lifeng; Hu, Cheng; Appleton, Brent A.; Mamo, Mulugeta; Tandeske, Laura; Tellew, John E.; Huang, Shenlin; Yue, Qn; Cliaudliary, Apurva; Tian, Hung; Iyer, Raman; Hassan, A. Quamrul; Griner, Lesley A. Mathews; La Bonte, Laura R.; Cooke, Vesselina G.; Van Abbema, Anne; Merritt, Hanne; Gampa, Kalyani; Feng, Fei; Yuan, Jing; Mishina, Yuji; Wang, Yingyun; Haling, Jacob R.; Vaziri, Sepideh; Hekmat-Nejad, Mohammad; Polyakov, Valery; Zang, Richard; Sethuraman, Vijay; Amiri, Payman; Singh, Mallika; Sellers, William R.; Lees, Emma; Shao, Wenlin; Dillon, Michael P.; Stuart, Darrin D. 分享 收藏 PARG inhibitors exhibit synthetic lethality with XRCC1 deficiency and a cellular mechanism of action that is distinct from PARP inhibitionMartin, Leenus; Cheng, Tzuling; James, Dominic I.; Begum, Habiba; Smith, Kate M.; Jordan, Allan; Waddell, Ian; Vaidya, Kedar; Fischer, Marcus; Yao, Bing; Drummond, Jason; Cleary, Leah; Martinez, Ruben; Sutton, James; Ravindran, Nandini; Joseph, James; Venetsanakos, Eleni; Dillon, Michael; Hager, Jeffrey H.; Belmont, Lisa D. 分享 收藏 Small-molecule antagonists of the Aryl Hydrocarbon Receptor (AhR) promote activation of human PBMCs in vitro and demonstrate significant impact on tumor growth and immune modulation in vivoJoseph, James; Gonzalez-Lopez, Marcos; Galang, Christina; Garcia, Candy; Lemar, Hadia; Lu, Jing; Vaidya, Kedar; Fischer, Marcus; Frey, Christian; Alam, Muzaffar; Yao, Bing; Dillon, Michael; Hager, Jeffrey H.; Venetsanakos, Eleni; Aswad, Fred 分享 收藏 Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitorStuart, Darrin D.; Shao, Wenlin; Mishina, Yuji; Feng, Yun; Caponigro, Giordano; Cooke, Vesselina G.; Rivera, Stacey; Shen, Fang; Korn, Joshua; Griner, Lesley A. Mathews; Nishiguchi, Giselle; Taft, Benjamin; Wan, Lifeng; Subramanian, Sharadha; Lou, Yan; Setti, Lina; Burger, Matthew; Tamez, Victor; Rico, Alice; Aversa, Robert; Tellew, John; Haling, Jacob R.; Polyakov, Valery; Lambert, Amy; Zang, Richard; Van Abbema, Ann; Hekmat-Nejad, Mohamad; Amiri, Payman; Singh, Mallika; Keen, Nicholas; Dillon, Michael P.; Lees, Emma; Sellers, William R.; Ramurthy, Savithri 分享 收藏 Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates烟酰胺磷酸核糖转移酶抑制剂作为抗体-药物缀合物的新型有效载荷Karpov, Alexei S.; Abrams, Tinya; Clark, Suzanna; Raikar, Ankita; D'Alessio, Joseph A.; Dillon, Michael P.; Gesner, Thomas G.; Jones, Darryl; Lacaud, Marion; Mallet, William; Martyniuk, Piotr; Meredith, Erik; Mohseni, Morvarid; Nieto-Oberhuber, Cristina M.; Palacios, Daniel; Perruccio, Francesca; Piizzi, Grazia; Zurini, Mauro; Bialucha, Carl Uli 分享 收藏 Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAFShao, Wenlin; Mishina, Yuji M.; Feng, Yun; Caponigro, Giordano; Cooke, Vesselina G.; Rivera, Stacy; Wang, Yingyun; Shen, Fang; Korn, Joshua M.; Griner, Lesley A. Mathews; Nishiguchi, Gisele; Rico, Alice; Tellew, John; Haling, Jacob R.; Aversa, Robert; Polyakov, Valery; Zang, Richard; Hekmat-Nejad, Mohammad; Amiri, Payman; Singh, Mallika; Keen, Nicholas; Dillon, Michael P.; Lees, Emma; Ramurthy, Savithri; Sellers, William R.; Stuart, Darrin D. 分享 收藏 
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