未登录 BBO-10203, an orally bioavailable small molecule that disrupts the RAS-PI3Kα interaction leading to pAKT and tumor growth inhibition in models of breast, lung and colorectal cancer Simanshu, D.; Xu, R.; Stice, J.; Czyzyk, D.; Feng, S.; Yang, Y.; Denson, J. P.; Riegler, E.; Zhang, C.; Fu, L.; Lin, K.; Lightstone, F. C.; Wang, K.; Stephen, A. G.; Maciag, A. E.; Sinkevicius, K.; Nissley, D. V.; Wallace, E. M.; McCormick, F.; Beltran, P. 分享 收藏
BBO-10203, a first-in-class, orally bioavailable, selective covalent small molecule that inhibits RAS- driven PI3Kalpha activity without affecting glucose metabolism Beltran, Pedro; Dhirendra, Simanshu; Xu, Rui; Chen, Ming; Czyzyk, Daniel; Donovan, Sofia; Feng, Siyu; Feng, Cindy; Fu, Lijuan; Lightstone, Felice; Lin, Ken; Maciag, Anna; Nissley, Dwight; Riegler, Erin; Sinkevicius, Kerstin; Stephen, Andrew; Stice, James; Turner, David; Wang, Bin; Wang, Keshi; Yang, Yue; Zhang, Cathy; McCormick, Frank; Wallace, Eli 分享 收藏
BBO-8520, a first-in-class, direct inhibitor of KRASG12C (ON), locks GTP-bound KRASG12C in the state 1 conformation resulting in rapid and complete blockade of effector binding Maciag, Anna E.; Stice, James; Wang, Bin; Sharma, Alok; Chan, Albert; Lin, Ken; Singh, Devansh; Dyba, Marcin; Yang, Yue; Setoodeh, Saman; Smith, Brian P.; Rabara, Dana; Zhang, Zuhui; Larsen, Erik K.; Esposito, Dom; Denson, John Paul; Ranieri, Michela; Meynardie, Mary; Mehdizadeh, Sadaf; Alexander, Patrick; Blanco, Maria Abreu; Turner, David; Xu, Rui; Lightstone, Felice C.; Wong, Kwok Kin; Simanshu, Dhirendra; Wang, Keshi; Stephen, Andrew G.; Sinkevicius, Kerstin; Nissley, Dwight V.; Wallace, Eli; McCormick, Frank; Beltran, Pedro J. 分享 收藏
Therapeutic targeting of cellular senescence in diabetic macular edema: preclinical and phase 1 trial results Crespo-Garcia, Sergio; Fournier, Frederik; Diaz-Marin, Roberto; Klier, Sharon; Ragusa, Derek; Masaki, Lauren; Cagnone, Gael; Blot, Guillaume; Hafiane, Ikhlas; Dejda, Agnieszka; Rizk, Rana; Juneau, Rachel; Buscarlet, Manuel; Chorfi, Sarah; Patel, Priyanka; Beltran, Pedro J.; Joyal, Jean-Sebastien; Rezende, Flavio A.; Hata, Masayuki; Nguyen, Alex; Sullivan, Lynne; Damiano, Jason; Wilson, Ariel M.; Mallette, Frederick A.; David, Nathaniel E.; Ghosh, Anirvan; Tsuruda, Pamela R.; Dananberg, Jamie; Sapieha, Przemyslaw 分享 收藏
Revealing the mechanism of action of a fi rst-in-class covalent inhibitor of KRASG12C (ON) and other functional properties of oncogenic KRAS by 31 P NMR 通过31 p NMR揭示一类共价抑制剂KRASG12C (ON) 的作用机理和致癌KRAS的其他功能特性 Sharma, Alok K.; Pei, Jun; Yang, Yue; Dyba, Marcin; Smith, Brian; Rabara, Dana; Larsen, Erik K.; Lightstone, Felice C.; Esposito, Dominic; Stephen, Andrew G.; Wang, Bin; Beltran, Pedro J.; Wallace, Eli; Nissley, Dwight V.; McCormick, Frank; Maciag, Anna E. 分享 收藏
Small-molecule inhibition of kinesin KIF18A reveals a mitotic vulnerability enriched in chromosomally unstable cancers Payton, Marc; Belmontes, Brian; Hanestad, Kelly; Moriguchi, Jodi; Chen, Kui; Mccarter, John D.; Chung, Grace; Ninniri, Maria Stefania; Sun, Jan; Manoukian, Raffi; Chambers, Stuart; Ho, Seok-Man; Kurzeja, Robert J. M.; Edson, Katheryne Z.; Dahal, Upendra P.; Wu, Tian; Wannberg, Sharon; Beltran, Pedro J.; Canon, Jude; Boghossian, Andrew S.; Rees, Matthew G.; Ronan, Melissa M.; Roth, Jennifer A.; Minocherhomji, Sheroy; Bourbeau, Matthew P.; Allen, Jennifer R.; Coxon, Angela; Tamayo, Nuria A.; Hughes, Paul E. 分享 收藏
Use of the natural nucleotide, GTP, is essential for the identification of potent, active-state KRASG12C inhibitors that bind in the switch II pocket Wang, Bin; Sharma, Alok; Stice, James; Smith, Brian; Dyba, Marcin; Singh, Devansh; Denson, John-Paul; Rabara, Dana; Larsen, Erik; Yang, Yue; Lightstone, Felice C.; Stephen, Andrew; Nissley, Dwight; McCormick, Frank; Wallace, Eli; Maciag, Anna E.; Beltran, Pedro J. 分享 收藏
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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 分享 收藏
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Pathological angiogenesis in retinopathy engages cellular senescence and is amenable to therapeutic elimination via BCL-xL inhibition Crespo-Garcia, Sergio; Tsuruda, Pamela R.; Dejda, Agnieszka; Ryan, Rathi D.; Fournier, Frederik; Chaney, Shawnta Y.; Pilon, Frederique; Dogan, Taner; Cagnone, Gael; Patel, Priyanka; Buscarlet, Manuel; Dasgupta, Sonali; Girouard, Gabrielle; Rao, Surabhi R.; Wilson, Ariel M.; O'Brien, Robert; Juneau, Rachel; Guber, Vera; Dubrac, Alexandre; Beausejour, Christian; Armstrong, Scott; Mallette, Frederick A.; Yohn, Christopher B.; Joyal, Jean-Sebastien; Marquess, Dan; Beltran, Pedro J.; Sapieha, Przemyslaw 分享 收藏
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AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies Caenepeel, Sean; Brown, Sean P.; Belmontes, Brian; Moody, Gordon; Keegan, Kathleen S.; Chui, Danny; Whittington, Douglas A.; Huang, Xin; Poppe, Leszek; Cheng, Alan C.; Cardozom, Mario; Houze, Jonathan; Li, Yunxiao; Lucas, Brian; Paras, Nick A.; Wang, Xianghong; Taygerly, Joshua P.; Vimolratana, Marc; Zancanella, Manuel; Zhu, Liusheng; Cajulis, Elaina; Osgood, Tao; Sun, Jan; Damon, Leah; Egan, Regina K.; Greninger, Patricia; McClanaghan, Joseph D.; Gong, Jianan; Moujalled, Donia; Pomilio, Giovanna; Beltran, Pedro; Benes, Cyril H.; Roberts, Andrew W.; Huang, David C.; Wei, Andrew; Canon, Jude; Coxon, Angela; Hughes, Paul E. 分享 收藏
Late-life targeting of the IGF-1 receptor improves healthspan and lifespan in female mice Mao, Kai; Quipildor, Gabriela Farias; Tabrizian, Tahmineh; Novaj, Ardijana; Guan, Fangxia; Walters, Ryan O.; Delahaye, Fabien; Hubbard, Gene B.; Ikeno, Yuji; Ejima, Keisuke; Li, Peng; Allison, David B.; Salimi-Moosavi, Hossein; Beltran, Pedro J.; Cohen, Pinchas; Barzilai, Nir; Huffman, Derek M. 分享 收藏
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Developmentof a murine tumor immunophenotyping platform to support drug discovery anddevelopment in immuno-oncology Belmontes, Brian; Matyas, Stephanie; O'Brien, Sarah; Tan, Hong; Ganley, Kenneth; Merriam, Kimberly; Rottman, Jim; Egen, Jackson; Beltran, Pedro; Moody, Gordon 分享 收藏
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A novel bispecific CD3/CDH19 antibody construct (CDH19 BiTE) directs potent killing of melanoma cells in vitro and in vivo and is enhanced by blockade of PD-L1 Moody, Gordon E.; Moriguchi, Jodi; Li, Shyun; Lee, Fei; Frank, Brendon; Gilbert, Amy; Case, Ryan; Dang, Khue; Hinkle, Beth; Coberly, Suzanne; Rottman, James; Merriam, Kim; Bailis, Julie; Beltran, Pedro J. 分享 收藏
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