未登录REM-422, a Small Molecule MYB mRNA Degrader, Demonstrates Anti-Leukemic Activity As Monotherapy and in Combination with Standards of Care in Preclinical Models of AMLREM-422,一种小分子MYB mRNA降解剂,在AML的临床前模型中显示出单药治疗以及与标准护理方案联合使用的抗白血病活性。
Levin-Furtney, Samantha; Thomas, Michael; Harney, Alycen M.; Shan, Mengge; Ivliev, Alexander; Stefek, Adam; Cameron, Michael; Prajapati, Sudeep; Seiler, Michael; Reynolds, Dominic; Buonamici, Silvia; Kung, Charles
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收藏REM-422, a potent, selective, oral small moleculemRNA degrader of the MYB oncogene, induces regressions in mouse patient-derived xenograft models of adenoid cystic carcinoma
Cameron, M.; Levin-Furtney, S.; Harney, A.; Thomas, M.; Dunyak, B.; Shan, M.; Prajapati, S.; Siu, Y. A.; Nguyen, D.; Buonamici, S.; Seiler, M.; Vaillancourt, F.; Smith, P.; Reynolds, D.; Kung, C.
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收藏Splicing modulators impair DNA damage response and induce killing of cohesin-mutant MDS and AML
Wheeler, Emily C.; Martin, Benjamin J. E.; Doyle, William C.; Neaher, Sofia; Conway, Caroline A.; Pitton, Caroline N.; Gorelov, Rebecca A.; Donahue, Melanie; Jann, Johann C.; Abdel-Wahab, Omar; Taylor, Justin; Seiler, Michael; Buonamici, Silvia; Pikman, Yana; Garcia, Jacqueline S.; Belizaire, Roger; Adelman, Karen; Tothova, Zuzana
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收藏Development of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for the treatment of lung cancers with MYC-induced translational addiction
Gavory, Gerald; Ghandi, Mahmoud; d'Alessandro, Anne-Cecile; Bonenfant, Debora; Cabanski, Maciej; Cantagallo, Lisa; Chicas, Agustin; Chen, Qian; Diesslin, Anna; King, Christopher; Massafra, Vittoria; Narayan, Rajiv; Osmont, Arnaud; Peck, Dave; Ortiz, Carolina Perdomo; Schillo, Martin; Singh, Ambika; Tiedt, Ralph; Tortoioli, Simone; Buonamici, Silvia; Janku, Filip; Wallace, Owen; Fasching, Bernhard
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收藏Identification of GSPT1-directed molecular glue degrader (MGD) for the treatment of Myc-driven breast cancer
Gavory, Gerald; Fasching, Bernhard; Bonenfant, Debora; Sadok, Amine; Singh, Ambika; Schillo, Martin; Massafra, Vittoria; d'Alessandro, Anne-Cecile; Castle, John; Ghandi, Mahmoud; Chicas, Agustin; Delobel, Frederic; Flohr, Alexander; Ottaviani, Giorgio; Ryckmans, Thomas; Laine, Anne-Laure; Eidam, Oliv; Wang, Hannah; Bernett, Ilona; Chan, Laura; Gorrini, Chiara; Roumiliotis, Theo; Choudhary, Jyoti; LeBihan, Yann-Vai; Cabry, Marc; Stubbs, Mark; Burke, Rosemary; Van Montfort, Rob; Caldwell, John; Chopra, Rajesh; Collins, Ian; Buonamici, Silvia
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收藏Intron retention is a hallmark and spliceosome represents a therapeutic vulnerability in aggressive prostate cancer
Zhang, Dingxiao; Hu, Qiang; Liu, Xiaozhuo; Ji, Yibing; Chao, Hsueh-Ping; Liu, Yan; Tracz, Amanda; Kirk, Jason; Buonamici, Silvia; Zhu, Ping; Wang, Jianmin; Liu, Song; Tang, Dean G.
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收藏Sensitivity to splicing modulation of BCL2 family genes reveals cancer therapeutic strategies for splicing modulators
Aird, Daniel; Teng, Teng; Huang, Chia-Ling; Pazolli, Ermira; Banka, Deepti; Cheung-Ong, Kahlin; Eifert, Cheryl; Furman, Craig; Wu, Jeremy; Seiler, Michael; Buonamici, Silvia; Fekkes, Peter; Karr, Craig; Palacino, James; Park, Eunice; Smith, Peter; Yu, Lihua; Mizui, Yoshiharu; Warmuth, Markus; Chicas, Agustin; Corson, Laura; Zhu, Ping
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收藏Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators
Aird, Daniel; Teng, Teng; Huang, Chia-Ling; Pazolli, Ermira; Banka, Deepti; Cheung-Ong, Kahlin; Eifert, Cheryl; Furman, Craig; Wu, Zhenhua Jeremy; Seiler, Michael; Buonamici, Silvia; Fekkes, Peter; Karr, Craig; Palacino, James; Park, Eunice; Smith, Peter G.; Yu, Lihua; Mizui, Yoshiharu; Warmuth, Markus; Chicas, Agustin; Corson, Laura; Zhu, Ping
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收藏Splicing modulation as novel therapeutic strategy against diffuse malignant peritoneal mesothelioma
Sciarrillo, Rocco; Wojtuszkiewicz, Anna; El Hassouni, Btissame; Funel, Niccola; Gandellini, Paolo; Lagerweij, Tonny; Buonamici, Silvia; Blijlevens, Maxime; van der Laan, Eveline A. Zeeuw; Zaffaroni, Nadia; Deraco, Marcello; Kusamura, Shigeki; Wurdinger, Tom; Peters, Godefridus J.; Molthoff, Carla F. M.; Jansen, Gerrit; Kaspers, Gertjan J. L.; Cloos, Jacqueline; Giovannetti, Elisa
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收藏SRPK1 maintains acute myeloid leukemia through effects on isoform usage of epigenetic regulators including BRD4
Tzelepis, Konstantinos; De Braekeleer, Etienne; Aspris, Demetrios; Barbieri, Isaia; Vijayabaskar, M. S.; Liu, Wen-Hsin; Gozdecka, Malgorzata; Metzakopian, Emmanouil; Toop, Hamish D.; Dudek, Monika; Robson, Samuel C.; Hermida-Prado, Francisco; Yang, Yu Hsuen; Babaei-Jadidi, Roya; Garyfallos, Dimitrios A.; Ponstingl, Hannes; Dias, Joao M. L.; Gallipoli, Paolo; Seiler, Michael; Buonamici, Silvia; Vick, Binje; Bannister, Andrew J.; Rad, Roland; Prinjha, Rab K.; Marioni, John C.; Huntly, Brian; Batson, Jennifer; Morris, Jonathan C.; Pina, Cristina; Bradley, Allan; Jeremias, Irmela; Bates, David O.; Yusa, Kosuke; Kouzarides, Tony; Vassiliou, George S.
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收藏Splicing modulation sensitizes chronic lymphocytic leukemia cells to venetoclax by remodeling mitochondrial apoptotic dependencies
ten Hacken, Elisa; Valentin, Rebecca; Regis, Fara Faye D.; Sun, Jing; Yin, Shanye; Werner, Lillian; Deng, Jing; Gruber, Michaela; Wong, Jessica; Zheng, Mei; Gill, Amy L.; Seiler, Michael; Smith, Peter; Thomas, Michael; Buonamici, Silvia; Ghia, Emanuela M.; Kim, Ekaterina; Rassenti, Laura Z.; Burger, Jan A.; Kipps, Thomas J.; Meyerson, Matthew L.; Bachireddy, Pavan; Wang, Lili; Reed, Robin; Neuberg, Donna; Carrasco, Ruben D.; Brooks, Angela N.; Letai, Anthony; Davids, Matthew S.; Wu, Catherine J.
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收藏Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer
Puyang, Xiaoling; Furman, Craig; Zheng, Guo Zhu; Wu, Zhenhua J.; Banka, Deepti; Aithal, Kiran; Agoulnik, Sergei; Bolduc, David M.; Buonamici, Silvia; Caleb, Benjamin; Das, Subhasree; Eckley, Sean; Fekkes, Peter; Hao, Ming-Hong; Hart, Andrew; Houtman, Rene; Irwin, Sean; Joshi, Jaya J.; Karr, Craig; Kim, Amy; Kumar, Namita; Kumar, Pavan; Kuznetsov, Galina; Lai, Weidong G.; Larsen, Nicholas; Mackenzie, Crystal; Martin, Lesley-Ann; Melchers, Diana; Moriarty, Alyssa; Tuong-Vi Nguyen; Norris, John; O'Shea, Morgan; Pancholi, Sunil; Prajapati, Sudeep; Rajagopalan, Sujatha; Reynolds, Dominic J.; Rimkunas, Victoria; Rioux, Nathalie; Ribas, Ricardo; Siu, Amy; Sivakumar, Sasirekha; Subramanian, Vanitha; Thomas, Michael; Vaillancourt, Frederic H.; Wang, John; Wardell, Suzanne; Wick, Michael J.; Yao, Shihua; Yu, Lihua; Warmuth, Markus; Smith, Peter G.; Zhu, Ping; Korpal, Manav
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收藏Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
Schoepfer, Joseph; Jahnke, Wolfgang; Berellini, Giuliano; Buonamici, Silvia; Cotesta, Simona; Cowan-Jacob, Sandra W.; Dodd, Stephanie; Drueckes, Peter; Fabbro, Doriano; Gabriel, Tobias; Groell, Jean-Marc; Grotzfeld, Robert M.; Hassan, A. Quamrul; Henry, Chrystele; Iyer, Varsha; Jones, Darryl; Lombardo, Franco; Loo, Alice; Manley, Paul W.; Pelle, Xavier; Rummel, Gabriele; Salem, Bahaa; Warmuth, Markus; Wylie, Andrew A.; Zoller, Thomas; Marzinzik, Andreas L.; Furet, Pascal
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收藏Structural Basis of Splicing Modulation by Antitumor Macrolide Compounds
Cretu, Constantin; Agrawal, Anant A.; Cook, Andrew; Will, Cindy L.; Fekkes, Peter; Smith, Peter G.; Luehrmann, Reinhard; Larsen, Nicholas; Buonamici, Silvia; Pena, Vladimir
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收藏H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers
Seiler, Michael; Yoshimi, Akihide; Darman, Rachel; Chan, Betty; Keaney, Gregg; Thomas, Michael; Agrawal, Anant A.; Caleb, Benjamin; Csibi, Alfredo; Sean, Eckley; Fekkes, Peter; Karr, Craig; Klimek, Virginia; Lai, George; Lee, Linda; Kumar, Pavan; Lee, Stanley Chun-Wei; Liu, Xiang; Mackenzie, Crystal; Meeske, Carol; Mizui, Yoshiharu; Padron, Eric; Park, Eunice; Pazolli, Ermira; Peng, Shouyong; Prajapati, Sudeep; Taylor, Justin; Teng, Teng; Wang, John; Warmuth, Markus; Yao, Huilan; Yu, Lihua; Zhu, Ping; Abdel-Wahab, Omar; Smith, Peter G.; Buonamici, Silvia
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收藏H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma
Joshi, Jaya Julie; Coffey, Heather; Corcoran, Erik; Tsai, Jennifer; Huang, Chia-Ling; Ichikawa, Kana; Prajapati, Sudeep; Hao, Ming-Hong; Bailey, Suzanna; Wu, Jeremy; Rimkunas, Victoria; Karr, Craig; Subramanian, Vanitha; Kumar, Pavan; MacKenzie, Crystal; Hurley, Raelene; Satoh, Takashi; Yu, Kun; Park, Eunice; Rioux, Nathalie; Kim, Amy; Lai, Weidong G.; Yu, Lihua; Zhu, Ping; Buonamici, Silvia; Larsen, Nicholas; Fekkes, Peter; Wang, John; Warmuth, Markus; Reynolds, Dominic J.; Smith, Peter G.; Selvaraj, Anand
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