未登录 Discovery of Atirmociclib (PF-07220060): A Potent and Selective CDK4 Inhibitor Gallego, Gary M.; Palmer, Cynthia; Orr, Suvi; Bernier, Louise; Chen, Ping; Cho-Schultz, Sujin; Deal, Judith G.; Dress, Klaus; Edwards, Martin; Jalaie, Mehran; Johnson, Eric; Kania, Robert; Kath, John C.; Lafontaine, Jennifer; Ninkovic, Sacha; Sach, Neal; Shen, Hong; Anders, Lars; Boras, Britton; Cao, Fengjuan; Cianfrogna, Julie A.; Cox, Loretta; Marroquin, Lisa; Pascual, Bernadette; Petroski, Matthew; Quinlan, Casey; Sacaan, Aida; Wei, Na; Nair, Sajiv K. 分享 收藏
Modulation of the substrate preference of a MYST acetyltransferase by a scaffold protein Sengupta, Raghuvir N.; Brodsky, Oleg; Bingham, Patrick; Diehl, Wade C.; Ferre, Roseann; Greasley, Samantha E.; Johnson, Eric; Kraus, Michelle; Lieberman, Whitney; Meier, Jordan L.; Paul, Thomas A.; Maegley, Karen A. 分享 收藏
Discovery of PF-07265028, A Selective Small Molecule Inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1) for the Treatment of Cancer Gallego, Rebecca A.; Cho-Schultz, Sujin; Del Bel, Matthew; Dechert-Schmitt, Anne-Marie; Donaldson, Joyann S.; He, Mingying; Jalaie, Mehran; Kania, Rob; Matthews, Jean; Mctigue, Michele; Tuttle, Jamison B.; Risley, Hud; Zhou, Dahui; Zhou, Ru; Ahmad, Omar K.; Bernier, Louise; Berritt, Simon; Braganza, John; Chen, Zecheng; Cianfrogna, Julie A.; Collins, Michael; Jones, Cinthia Costa; Cronin, Ciaran N.; Davis, Carl; Dress, Klaus; Edwards, Martin; Farrell, William; France, Scott P.; Grable, Nicole; Johnson, Eric; Johnson, Ted W.; Jones, Rhys; Knauber, Thomas; Lafontaine, Jennifer; Loach, Richard P.; Maestre, Michael; Miller, Nichol; Moen, Mark; Monfette, Sebastien; Morse, Peter; Nager, Andrew Ross; Niosi, Mark; Richardson, Paul; Rohner, Allison K.; Sach, Neal W.; Timofeevski, Sergei; Tucker, Joseph W.; Vetelino, Beth; Zhang, Lei; Nair, Sajiv K. 分享 收藏
An allosteric cyclin E-CDK2 site mapped by paralog hopping with covalent probes Zhang, Yuanjin; Liu, Zhonglin; Hirschi, Marscha; Brodsky, Oleg; Johnson, Eric; Won, Sang Joon; Nagata, Asako; Bezwada, Divya; Petroski, Matthew D.; Majmudar, Jaimeen D.; Niessen, Sherry; Vanarsdale, Todd; Gilbert, Adam M.; Hayward, Matthew M.; Stewart, Al E.; Nager, Andrew R.; Melillo, Bruno; Cravatt, Benjamin F. 分享 收藏
Phase 1 study of ABBV-155 ± paclitaxel in relapsed/ refractory solid tumors: Results in Japanese patients Shimizu, Toshio; Yonemori, Kan; Kuboki, Yasutoshi; Tolcher, Anthony; Kurokawa, Misaki; Munasinghe, Wijith; Phillips, Andrew; Souers, Andrew; Johnson, Eric; He, Lei; Weitzman, Aaron; Powderly, John; Lorusso, Patricia; Naito, Yoichi 分享 收藏
Selective MCL-1 inhibitor ABBV-467 is efficacious in tumor models but is associated with cardiac troponin increases in patients Yuda, Junichiro; Will, Christine; Phillips, Darren C.; Abraham, Linu; Alvey, Cory; Avigdor, Abraham; Buck, Wayne; Besenhofer, Lauren; Boghaert, Erwin; Cheng, Dong; Cojocari, Dan; Doyle, Kelly; Hansen, T. Matthew; Huang, Kevin; Johnson, Eric F.; Judd, Andrew S.; Judge, Russell A.; Kalvass, John C.; Kunzer, Aaron; Lam, Lloyd T.; Li, Rachel; Martin, Ruth L.; Mastracchio, Anthony; Mitten, Mike; Petrich, Adam; Wang, Jin; Ward, James E.; Zhang, Haichao; Wang, Xilu; Wolff, Johannes E.; Bell-McGuinn, Katherine M.; Souers, Andrew J. 分享 收藏
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer 发现一种高效，选择性，口服生物利用度的KAT6A/B组蛋白乙酰转移酶抑制剂，对KAT6A-high ER乳腺癌有效 Sharma, Shikhar; Chung, Chi-Yeh; Uryu, Sean; Petrovic, Jelena; Cao, Joan; Rickard, Amanda; Nady, Nataliya; Greasley, Samantha; Johnson, Eric; Brodsky, Oleg; Khan, Showkhin; Wang, Hui; Wang, Zhenxiong; Zhang, Yong; Tsaparikos, Konstantinos; Chen, Lei; Mazurek, Anthony; Lapek, John; Kung, Pei-Pei; Sutton, Scott; Richardson, Paul F.; Greenwald, Eric C.; Yamazaki, Shinji; Jones, Rhys; Maegley, Karen A.; Bingham, Patrick; Lam, Hieu; Stupple, Alexandra E.; Kamal, Aileen; Chueh, Anderly; Cuzzupe, Anthony; Morrow, Benjamin J.; Ren, Bin; Carrasco-Pozo, Catalina; Tan, Chin Wee; Bhuva, Dharmesh D.; Allan, Elizabeth; Surgenor, Elliot; Vaillant, Francois; Pehlivanoglu, Havva; Falk, Hendrik; Whittle, James R.; Newman, Janet; Cursons, Joseph; Doherty, Judy P.; White, Karen L.; Macpherson, Laura; Devlin, Mark; Dennis, Matthew L.; Hattarki, Meghan K.; De Silva, Melanie; Camerino, Michelle A.; Butler, Miriam S.; Dolezal, Olan; Pilling, Patricia; Foitzik, Richard; Stupple, Paul A.; Lagiakos, H. Rachel; Walker, Scott R.; Hediyeh-Zadeh, Soroor; Nuttall, Stewart; Spall, Sukhdeep; Charman, Susan A.; Connor, Theresa; Peat, Thomas S.; Avery, Vicky M.; Bozikis, Ylva E.; Yang, Yuqing; Zhang, Ming; Monahan, Brendon J.; Voss, Anne K.; Street, Ian P.; Dawson, Sarah-Jane; Dawson, Mark A.; Lindeman, Geoffrey J.; Davis, Melissa J.; Visvader, Jane E.; Paul, Thomas A. 分享 收藏
Design and Synthesis of Functionally Active 5-Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1 Gallego, Rebecca A.; Bernier, Louise; Chen, Hui; Cho-Schultz, Sujin; Chung, Loanne; Collins, Michael; Del Bel, Matthew; Elleraas, Jeff; Jones, Cinthia Costa; Cronin, Ciaran N.; Edwards, Martin; Fang, Xu; Fisher, Timothy; He, Mingying; Hoffman, Jacqui; Huo, Ruiduan; Jalaie, Mehran; Johnson, Eric; Johnson, Ted W.; Kania, Robert S.; Kraus, Manfred; Lafontaine, Jennifer; Le, Phuong; Liu, Tongnan; Maestre, Michael; Matthews, Jean; McTigue, Michele; Miller, Nichol; Mu, Qiming; Qin, Xulong; Ren, Shijian; Richardson, Paul; Rohner, Allison; Sach, Neal; Shao, Li; Smith, Graham; Su, Ruirui; Sun, Bin; Timofeevski, Sergei; Tran, Phuong; Wang, Shuiwang; Wang, Wei; Zhou, Ru; Zhu, Jinjiang; Nair, Sajiv K. 分享 收藏
Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation Johnson, Eric; McTigue, Michele; Gallego, Rebecca A.; Johnson, Ted W.; Timofeevski, Sergei; Maestre, Michael; Fisher, Timothy S.; Kania, Robert; Sawasdikosol, Sansana; Burakoff, Steven; Cronin, Ciaran N. 分享 收藏
PARP1 Trapping by PARP Inhibitors Drives Cytotoxicity in Both Cancer Cells and Healthy Bone Marrow PARP抑制剂捕获的PARP1可驱动癌细胞和健康骨髓中的细胞毒性 Hopkins, Todd A.; Ainsworth, William B.; Ellis, Paul A.; Donawho, Cherrie K.; DiGiammarino, Enrico L.; Panchal, Sanjay C.; Abraham, Vivek C.; Algire, Mikkel A.; Shi, Yan; Olson, Amanda M.; Johnson, Eric F.; Wilsbacher, Julie L.; Maag, David 分享 收藏
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain Bagal, Sharan K.; Andrews, Mark; Bechle, Bruce M.; Bian, Jianwei; Bilsland, James; Blakemore, David C.; Braganza, John F.; Bungay, Peter J.; Corbett, Matthew S.; Cronin, Ciaran N.; Cui, Jingrong Jean; Dias, Rebecca; Flanagan, Neil J.; Greasley, Samantha E.; Grimley, Rachel; James, Kim; Johnson, Eric; Kitching, Linda; Kraus, Michelle L.; McAlpine, Indrawan; Nagata, Asako; Ninkovic, Sacha; Omoto, Kiyoyuki; Scales, Stephanie; Skerratt, Sarah E.; Sun, Jianmin; Tran-Dube, Michelle; Waldron, Gareth J.; Wang, Fen; Warmus, Joseph S. 分享 收藏
Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors Bagal, Sharan K.; Omoto, Kiyoyuki; Blakemore, David C.; Bungay, Peter J.; Bilsland, James G.; Clarke, Philip J.; Corbett, Matthew S.; Cronin, Ciaran N.; Cui, J. Jean; Dias, Rebecca; Flanagan, Neil J.; Greasley, Samantha E.; Grimley, Rachel; Johnson, Eric; Fengas, David; Kitching, Linda; Kraus, Michelle L.; McAlpine, Indrawan; Nagata, Asako; Waldron, Gareth J.; Warmus, Joseph S. 分享 收藏
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A randomized Phase II study of veliparib with temozolomide or carboplatin/paclitaxel versus placebo with carboplatin/paclitaxel in BRCA1/2 metastatic breast cancer: design and rationale 维利帕尼联合替莫唑胺或卡铂/紫杉醇与安慰剂联合卡铂/紫杉醇治疗BRCA1/2转移性乳腺癌的随机II期研究: 设计和原理 Isakoff, Steven J.; Puhalla, Shannon; Domchek, Susan M.; Friedlander, Michael; Kaufman, Bella; Robson, Mark; Telli, Melinda L.; Dieras, Veronique; Han, Hyo Sook; Garber, Judy E.; Johnson, Eric F.; Maag, David; Qin, Qin; Giranda, Vincent L.; Shepherd, Stacie P. 分享 收藏
Mechanistic Dissection of PARP1 Trapping and the Impacton In Vivo Tolerability and Efficacy of PARP Inhibitors Hopkins, Todd A.; Shi, Yan; Rodriguez, Luis E.; Solomon, Larry R.; Donawho, Cherrie K.; DiGiammarino, Enrico L.; Panchal, Sanjay C.; Wilsbacher, Julie L.; Gao, Wenqing; Olson, Amanda M.; Stolarik, DeAnne F.; Osterling, Donald J.; Johnson, Eric F.; Maag, David 分享 收藏
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Axitinib targets gatekeeper-mutant BCR-ABL1(T315I)-driven leukemia in a distinct and selective fashion Pemovska, Tea; Johnson, Eric; Kontro, Mika; Repasky, Gretchen A.; Chen, Jeffrey; Wells, Peter; Cronin, Ciaran N.; McTigue, Michele; Kallioniemi, Olli; Porkka, Kimmo; Murray, Brion W.; Wennerberg, Krister 分享 收藏
PARP inhibitors trap PARP1 onto damaged DNA via catalytic inhibition and not by an allosteric mechanism Hopkins, T.; Solomon, L.; Shi, Y.; Rodriguez, L.; Donawho, C.; DiGiammarino, E.; Panchal, S.; Olson, A.; Stolarik, D.; Osterling, D.; Gao, W.; Johnson, E.; Maag, D. 分享 收藏
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Pyrimidine-Based Tricyclic Molecules as Potent and Orally Efficacious Inhibitors of Wee1 Kinase 基于嘧啶的三环分子作为Wee1激酶的有效和口服有效抑制剂 Tong, Yunsong; Torrent, Maricel; Florjancic, Alan S.; Bromberg, Kenneth D.; Buchanan, Fritz G.; Ferguson, Debra C.; Johnson, Eric F.; Lasko, Loren M.; Maag, David; Merta, Philip J.; Olson, Amanda M.; Osterling, Donald J.; Soni, Nirupama; Shoemaker, Alexander R.; Penning, Thomas D. 分享 收藏
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