未登录 Discovery of small molecules that target a tertiary-structured RNA 发现靶向三级结构RNA的小分子 Menichelli, Elena; Lam, Bianca J.; Wang, Yu; Wang, Vivian S.; Shaffer, Jennifer; Tjhung, Katrina F.; Bursulaya, Badry; Truc Ngoc Nguyen; Vo, Todd; Alper, Phillip B.; McAllister, Christopher S.; Jones, David H.; Spraggon, Glen; Michellys, Pierre-Yves; Joslin, John; Joyce, Gerald F.; Rogers, Jeff 分享 收藏
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-d]pyrimidine RET Inhibitors Mathison, Casey J. N.; Yang, Yang; Nelson, John; Huang, Zhihong; Jiang, Jiqing; Chianelli, Donatella; V. Rucker, Paul; Roland, Jason; Xie, Yun Feng; Epple, Robert; Bursulaya, Badry; Lee, Christian; Gao, Mu-Yun; Shaffer, Jennifer; Briones, Sergio; Sarkisova, Yelena; Galkin, Anna; Li, Lintong; Li, Nanxin; Li, Chun; Hua, Su; Kasibhatla, Shailaja; Kinyamu-Akunda, Jacqueline; Kikkawa, Rie; Molteni, Valentina; Tellew, John E. 分享 收藏
Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases Nagle, Advait; Biggart, Agnes; Be, Celine; Srinivas, Honnappa; Hein, Andreas; Caridha, Diana; Sciotti, Richard J.; Pybus, Brandon; Kreishman-Deitrick, Mara; Bursulaya, Badry; Lai, Yin H.; Gao, Mu-Yun; Liang, Fang; Mathison, Casey J. N.; Liu, Xiaodong; Yeh, Vince; Smith, Jeffrey; Lerario, Isabelle; Xie, Yongping; Chianelli, Donatella; Gibney, Michael; Berman, Ashley; Chen, Yen-Liang; Jiricek, Jan; Davis, Lauren C.; Liu, Xianzhong; Ballard, Jaime; Khare, Shilpi; Eggimann, Fabian Kurt; Luneau, Alexandre; Groessl, Todd; Shapiro, Michael; Richmond, Wendy; Johnson, Kevin; Rudewicz, Patrick J.; Rao, Srinivasa P. S.; Thompson, Christopher; Tuntland, Tove; Spraggon, Glen; Glynne, Richard J.; Supek, Frantisek; Wiesmann, Christian; Molteni, Valentina 分享 收藏
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133 Liu, Yahu A.; Jin, Qihui; Zou, Yefen; Ding, Qiang; Yan, Shanshan; Wang, Zhicheng; Hao, Xueshi; Bao Nguyen; Zhang, Xiaoyue; Pan, Jianfeng; Mo, Tingting; Jacobsen, Kate; Thanh Lam; Wu, Tom Y-H; Petrassi, H. Michael; Bursulaya, Badry; DiDonato, Michael; Gordon, W. Perry; Liu, Bo; Baaten, Janine; Hill, Robert; Van Nguyen-Tran; Qiu, Minhua; Zhang, You-Qing; Kamireddy, Anwesh; Espinola, Sheryll; Deaton, Lisa; Ha, Sukwon; Harb, George; Jia, Yong; Li, Jing; Shen, Weijun; Schumacher, Andrew M.; Colman, Karyn; Glynne, Richard; Pan, Shifeng; McNamara, Peter; Laffitte, Bryan; Meeusen, Shelly; Molteni, Valentina; Loren, Jon 分享 收藏
Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma 吡唑并 [1，5-a] 嘧啶RET激酶抑制剂治疗肺腺癌的疗效和耐受性 Mathison, Casey J. N.; Chianelli, Donatella; Rucker, Paul V.; Nelson, John; Roland, Jason; Huang, Zhihong; Yang, Yang; Jiang, Jiqing; Xie, Yun Feng; Epple, Robert; Bursulaya, Badry; Lee, Christian; Gao, Mu-Yun; Shaffer, Jennifer; Briones, Sergio; Sarkisova, Yelena; Galkin, Anna; Li, Lintong; Li, Nanxin; Li, Chun; Hua, Su; Kasibhatla, Shailaja; Kinyamu-Akunda, Jacqueline; Kikkawa, Rie; Molteni, Valentina; Tellew, John E. 分享 收藏
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis Ndufexor (LMB763)，一种用于治疗非酒精性脂肪性肝炎的新型FXR调节剂 Chianelli, Donatella; Rucker, Paul, V; Roland, Jason; Tully, David C.; Nelson, John; Liu, Xiaodong; Bursulaya, Badry; Hernandez, Eloy D.; Wu, Jane; Prashad, Mahavir; Schlama, Thierry; Liu, Yugang; Chu, Alan; Schmeits, James; Huang, David J.; Hill, Robert; Bao, Dingjiu; Zoll, Jocelyn; Kim, Young; Groessl, Todd; McNamara, Peter; Liu, Bo; Richmond, Wendy; Sancho-Martinez, Ignatio; Phimister, Andrew; Seidel, H. Martin; Badman, Michael K.; Joseph, Sean B.; Laffitte, Bryan; Molteni, Valentina 分享 收藏
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH) Tully, David C.; Rucker, Paul V.; Chianelli, Donatella; Williams, Jennifer; Vidal, Agnes; Alper, Phil B.; Mutnick, Daniel; Bursulaya, Badry; Schmeits, James; Wu, Xiangdong; Bao, Dingjiu; Zoll, Jocelyn; Kim, Young; Groessl, Todd; McNamara, Peter; Seidel, H. Martin; Molteni, Valentina; Liu, Bo; Phimister, Andrew; Joseph, Sean B.; Laffitte, Bryan 分享 收藏
Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases He, Xiaohui; Da Ros, Sara; Nelson, John; Zhu, Xuefeng; Jiang, Tao; Okram, Barun; Jiang, Songchun; Michellys, Pierre-Yves; Iskandar, Maya; Espinola, Sheryll; Jia, Yong; Bursulaya, Badry; Kreusch, Andreas; Gao, Mu-Yun; Spraggon, Glen; Baaten, Janine; Clemmer, Leah; Meeusen, Shelly; Huang, David; Hill, Robert; Van Nguyen-Tran; Fathman, John; Liu, Bo; Tuntland, Tove; Gordon, Perry; Hollenbeck, Thomas; Ng, Kenneth; Shi, Jian; Bordone, Laura; Liu, Hong 分享 收藏
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers Lelais, Gerald; Epple, Robert; Marsilje, Thomas H.; Long, Yun O.; McNeill, Matthew; Chen, Bei; Lu, Wenshuo; Anumolu, Jaganmohan; Badiger, Sangamesh; Bursulaya, Badry; DiDonato, Michael; Fong, Rina; Juarez, Jose; Li, Jie; Manuia, Mari; Mason, Daniel E.; Gordon, Perry; Groessl, Todd; Johnson, Kevin; Jia, Yong; Kasibhatla, Shailaja; Li, Chun; Isbell, John; Spraggon, Glen; Bender, Steven; Michellys, Pierre-Yves 分享 收藏
EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor Jia, Yong; Juarez, Jose; Li, Jie; Manuia, Mari; Niederst, Matthew J.; Tompkins, Celin; Timple, Noelito; Vaillancourt, Mei-Ting; Pferdekamper, AnneMarie Culazzo; Lockerman, Elizabeth L.; Li, Chun; Anderson, Jennifer; Costa, Carlotta; Liao, Debbie; Murphy, Eric; DiDonato, Michael; Bursulaya, Badry; Lelais, Gerald; Barretina, Jordi; McNeill, Matthew; Epple, Robert; Marsilje, Thomas H.; Pathan, Nuzhat; Engelman, Jeffrey A.; Michellys, Pierre-Yves; McNamara, Peter; Harris, Jennifer; Bender, Steven; Kasibhatla, Shailaja 分享 收藏
Efficient Preparation of Site-Specific Antibody Drug Conjugates Using Phosphopantetheinyl Transferases Gruenewald, Jan; Klock, Heath E.; Cellitti, Susan E.; Bursulaya, Badry; McMullan, Daniel; Jones, David H.; Chiu, Hsien-Po; Wang, Xing; Patterson, Paula; Zhou, Huanfang; Vance, Julie; Nigoghossian, Edward; Tong, Hung; Daniel, Dylan; Mallet, William; Ou, Weijia; Uno, Tetsuo; Brock, Ansgar; Lesley, Scott A.; Geierstanger, Bernhard H. 分享 收藏
Discovery of a potent covalent mutant-selective EGFR inhibitor - the journey from high throughput screening to EGF816 Lelais, Gerald; Epple, Robert; Michellys, Pierre-Yves; Marsilje, Thomas H.; Long, Yun; McNeill, Matthew; Chen, Bei; Lu, Wenshuo; Bursulaya, Badry; DiDonato, Michael; Jia, Yong; Kasibhatla, Shailaja; Li, Chun; Matushansky, Igor; Bender, Steven 分享 收藏
In vitro characterization of EGF816, a third-generation mutant-selective EGFR inhibitor Jia, Yong; Juarez, Jose; Manuia, Mari; Lelais, Gerald; Kasibhatla, Shailaja; Long, Oliver; McNeill, Matthew; DiDonato, Michael; Bursulaya, Badry; Liao, Debbie; Murphy, Eric; Epple, Robert; Marsilje, Thomas; Pathan, Nuzhat; Michellys, Pierre-Yves; Bender, Steven; Harris, Jennifer 分享 收藏
Discovery of Trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as Potent, Orally Bioavailable TGR5 (GPBAR1) Agonists: Structure-Activity Relationships, Lead Optimization, and Chronic In Vivo Efficacy Phillips, Dean P.; Gao, Wenqi; Yang, Yang; Zhang, Guobao; Lerario, Isabelle K.; Lau, Thomas L.; Jiang, Jiqing; Wang, Xia; Nguyen, Deborah G.; Bhat, B. Ganesh; Trotter, Carol; Sullivan, Heather; Welzel, Gustav; Landry, Jannine; Chen, Yali; Joseph, Sean B.; Li, Chun; Gordon, W. Perry; Richmond, Wendy; Johnson, Kevin; Bretz, Angela; Bursulaya, Badry; Pan, Shifeng; McNamara, Peter; Seidel, H. Martin 分享 收藏
Synthesis, Structure-Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials Marsilje, Thomas H.; Pei, Wei; Chen, Bei; Lu, Wenshuo; Uno, Tetsuo; Jin, Yunho; Jiang, Tao; Kim, Sungjoon; Li, Nanxin; Warmuth, Markus; Sarkisova, Yelena; Sun, Frank; Steffy, Auzon; Pferdekamper, AnneMarie C.; Li, Allen G.; Joseph, Sean B.; Kim, Young; Liu, Bo; Tuntland, Tove; Cui, Xiaoming; Gray, Nathanael S.; Steensma, Ruo; Wan, Yongqin; Jiang, Jiqing; Chopiuk, Greg; Li, Jie; Gordon, W. Perry; Richmond, Wendy; Johnson, Kevin; Chang, Jonathan; Groessl, Todd; He, You-Qun; Phimister, Andrew; Aycinena, Alex; Lee, Christian C.; Bursulaya, Badry; Karanewsky, Donald S.; Seidel, H. Martin; Harris, Jennifer L.; Michellys, Pierre-Yves 分享 收藏
Structural basis for lack of toxicity of the diphtheria toxin mutant CRM197 Malito, Enrico; Bursulaya, Badry; Chen, Connie; Lo Surdo, Paola; Picchianti, Monica; Balducci, Enrico; Biancucci, Marco; Brock, Ansgar; Berti, Francesco; Bottomley, Matthew James; Nissum, Mikkel; Costantino, Paolo; Rappuoli, Rino; Spraggon, Glen 分享 收藏
A Chemical Genomic Analysis of Decoquinate, a Plasmodium falciparum Cytochrome b Inhibitor Nam, Tae-gyu; McNamara, Case W.; Bopp, Selina; Dharia, Neekesh V.; Meister, Stephan; Bonamy, Ghislain M. C.; Plouffe, David M.; Kato, Nobutaka; McCormack, Susan; Bursulaya, Badry; Ke, Hangjun; Vaidya, Akhil B.; Schultz, Peter G.; Winzeler, Elizabeth A. 分享 收藏
Loss of CD4 T-cell-dependent tolerance to proteins with modified amino acids Gauba, Varun; Gruenewald, Jan; Gorney, Vanessa; Deaton, Lisa M.; Kang, Mingchao; Bursulaya, Badry; Ou, Weijia; Lerner, Richard A.; Schmedt, Christian; Geierstanger, Bernhard H.; Schultz, Peter G.; Ramirez-Montagut, Teresa 分享 收藏
Genome scanning of Amazonian Plasmodium falciparum shows subtelomeric instability and clindamycin-resistant parasites Dharia, Neekesh V.; Plouffe, David; Bopp, Selina E. R.; Gonzalez-Paez, Gonzalo E.; Lucas, Carmen; Salas, Carola; Soberon, Valeria; Bursulaya, Badry; Kochel, Tadeusz J.; Bacon, David J.; Winzeler, Elizabeth A. 分享 收藏
Expanding the Diversity of Allosteric Ber-Abl Inhibitors Deng, Xianming; Okram, Barun; Ding, Qiang; Zhang, Jianming; Choi, Yongmun; Adrian, Francisco J.; Wojciechowski, Amy; Zhang, Guobao; Che, Jianwei; Bursulaya, Badry; Cowan-Jacob, Sandra W.; Rummel, Gabriele; Sim, Taebo; Gray, Nathanael S. 分享 收藏
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