未登录 Discovery and Optimization of Pyrazine Carboxamide AZ3246, a Selective HPK1 Inhibitor 吡嗪羧酰胺AZ3246的发现与优化：一种选择性HPK1抑制剂 Shields, Jason D.; Baker, David; Balazs, Amber Y. S.; Bommakanti, Gayathri; Casella, Robert; Cao, Shenggen; Cook, Steve; Escobar, Randolph A.; Fawell, Stephen; Gibbons, Francis D.; Giblin, Kathryn A.; Goldberg, Frederick W.; Gosselin, Eric; Grebe, Tyler; Hariparsad, Niresh; Hatoum-Mokdad, Holia; Howells, Rachel; Hughes, Samantha J.; Jackson, Anne; Reddy, Iswarya Karapa; Kettle, Jason G.; Lamont, Gillian M.; Lamont, Scott; Li, Min; Lill, Sten O. Nilsson; Mele, Deanna A.; Metrano, Anthony J.; Mfuh, Adelphe M.; Morrill, Lucas A.; Peng, Bo; Pflug, Alexander; Proia, Theresa A.; Rezaei, Hadi; Richards, Ryan; Richter, Magdalena; Robbins, Kevin J.; San Martin, Maryann; Schimpl, Marianne; Schuller, Alwin G.; Sha, Li; Shen, Minhui; Sheppeck, James E.; Singh, Meha; Stokes, Stephen; Song, Kun; Sun, Yuanyuan; Tang, Haoran; Wagner, David J.; Wang, Jianyan; Wang, Yanjun; Wilson, David M.; Wu, Allan; Wu, Chengyan; Wu, Dedong; Wu, Ye; Xu, Kevin; Yang, Yue; Yao, Tieguang; Ye, Minwei; Zhang, Andrew X.; Zhang, Hui; Zhai, Xiang; Zhou, Yanxiao; Ziegler, Robert E.; Grimster, Neil P. 分享 收藏
Discovery of (2R,4R)-4-((S)-2-Amino-3-methylbutanamido)-2-(4-boronobutyl)pyrrolidine-2-carboxylic Acid (AZD0011), an Actively Transported Prodrug of a Potent Arginase Inhibitor to Treat Cancer Mlynarski, Scott N.; Aquila, Brian M.; Cantin, Susan; Cook, Steve; Doshi, Aatman; Finlay, M. Raymond V.; Gangl, Eric T.; Grebe, Tyler; Gu, Chungang; Kawatkar, Sameer P.; Petersen, Jens; Pop-Damkov, Petar; Schuller, Alwin G.; Shao, Wenlin; Shields, Jason D.; Simpson, Iain; Tavakoli, Siavash; Tentarelli, Sharon; Throner, Scott; Wang, Haixia; Wang, Jianyan; Wu, Dedong; Ye, Qing 分享 收藏
The MET inhibitor savolitinib shows anti-tumor activity in a pre-clinical, intracranial, MET dependent, xenograft model Schuller, A.; Gordon, J.; Beaumont, K.; Jones, K.; Suksomboon, M.; Rosenthal, S.; Jones, R. 分享 收藏
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Targeting tumor infiltrating myeloid cells in prostate cancer De Velasco, Marco A.; Kura, Yurie; Ando, Naomi; Sako, Noriko; Fujita, Kazutoshi; Sakai, Kazuko; Schuller, Alwin G.; Sachsenmeier, Kris F.; Nozawa, Masahiro; Banno, Eri; Yoshimura, Kazuhiro; Nishio, Kazuto; Uemura, Hirotsugu 分享 收藏
Novel Arginase Inhibitor, AZD0011, Demonstrates Immune Cell Stimulation and Antitumor Efficacy with Diverse Combination Partners Doshi, Aatman S.; Cantin, Susan; Hernandez, Marylens; Srinivasan, Srimathi; Tentarelli, Sharon; Griffin, Matthew; Wang, Yanjun; Pop-Damkov, Petar; Prickett, Laura B.; Kankkonen, Cecilia; Shen, Minhui; Martin, Maryann San; Wu, Song; Castaldi, M. Paola; Ghadially, Hormas; Varnes, Jeffrey; Gales, Sonya; Henry, David; Hoover, Clare; Mele, Deanna A.; Simpson, Iain; Gangl, Eric T.; Mlynarski, Scott N.; Finlay, M. Raymond V.; Drew, Lisa; Fawell, Stephen E.; Shao, Wenlin; Schuller, Alwin G. 分享 收藏
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Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR-mutant lung cancer Eser, Pinar Ozden; Paranal, Raymond M.; Son, Jieun; Ivanova, Elena; Kuang, Yanan; Haikala, Heidi M.; To, Ciric; Okoro, Jeffrey J.; Dholakia, Kshiti H.; Choi, Jihyun; Eum, Yoonji; Ogino, Atsuko; Missios, Pavlos; Ercan, Dalia; Xu, Man; Poitras, Michael J.; Wang, Stephen; Ngo, Kenneth; Dills, Michael; Yanagita, Masahiko; Lopez, Timothy; Lin, Mika; Tsai, Jeanelle; Floch, Nicolas; Chambers, Emily S.; Heng, Jennifer; Anjum, Rana; Santucci, Alison D.; Michael, Kesi; Schuller, Alwin G.; Cross, Darren; Smith, Paul D.; Oxnard, Geoffrey R.; Barbie, David A.; Sholl, Lynette M.; Bahcall, Magda; Palakurthi, Sangeetha; Gokhale, Prafulla C.; Paweletz, Cloud P.; Daley, George Q.; Janne, Pasi A. 分享 收藏
Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy Patterson, Claire M.; Balachander, Srividya B.; Grant, Iain; Pop-Damkov, Petar; Kelly, Brian; McCoull, William; Parker, Jeremy; Giannis, Michael; Hill, Kathryn J.; Gibbons, Francis D.; Hennessy, Edward J.; Kemmitt, Paul; Harmer, Alexander R.; Gales, Sonya; Purbrick, Stuart; Redmond, Sean; Skinner, Matthew; Graham, Lorraine; Secrist, J. Paul; Schuller, Alwin G.; Wen, Shenghua; Adam, Ammar; Reimer, Corinne; Cidado, Justin; Wild, Martin; Gangl, Eric; Fawell, Stephen E.; Saeh, Jamal; Davies, Barry R.; Owen, David J.; Ashford, Marianne B. 分享 收藏
A pharmacokinetic-pharmacodynamic model for the MET tyrosine kinase inhibitor, savolitinib, to explore target inhibition requirements for anti-tumour activity Jones, Rhys D. O.; Grondine, Mike; Borodovsky, Alexandra; San Martin, Maryann; DuPont, Michelle; D'Cruz, Celina; Schuller, Alwin; Henry, Ryan; Barry, Evan; Castriotta, Lillian; Anjum, Rana; Petersson, Klas; Sahota, Tarjinder; Ahmed, Ghada F. 分享 收藏
Targeting A2aR in mouse Pten-deficient prostate cancer De Velasco, Marco A.; Kura, Yurie; Sako, Noriko; Ando, Naomi; Sakai, Kazuko; Nozawa, Masahiro; Yoshimura, Kazuhiro; Yoshikawa, Kazuhiro; Schuller, Alwin; Nishio, Kazuto; Uemura, Hirotsugu 分享 收藏
Inhibition of arginase in combination with anti-PDL1 leads to increased infiltration and activation of CD8+T cells, NK cells, and CD103+dendritic cells in mouse syngeneic tumor models Schuller, Alwin; Doshi, Aatman; Cantin, Susan; Secinaro, Michael; Wang, Yanjun; Prickett, Laura; Tentarelli, Sharon; Gangl, Eric; Ghadially, Horma; Ilieva, Kristina; Proia, Theresa; Mlynarski, Scott; Finlay, Ray; Shao, Wenlin 分享 收藏
The A2AR antagonist AZD4635 prevents adenosine-mediated immunosuppression of CD103+dendritic cells Barbon, Christine M.; Borodovsky, Alexandra; Wang, Yanjun; Prickett, Laura; Sachsenmeier, Kris; Schuller, Alwin; Shao, Wenlin; Barrett, Carl; Fawell, Stephen; Mele, Deanna A. 分享 收藏
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia Tron, Adriana E.; Belmonte, Matthew A.; Adam, Ammar; Aquila, Brian M.; Boise, Lawrence H.; Chiarparin, Elisabetta; Cidado, Justin; Embrey, Kevin J.; Gangl, Eric; Gibbons, Francis D.; Gregory, Gareth P.; Hargreaves, David; Hendricks, J. Adam; Johannes, Jeffrey W.; Johnstone, Ricky W.; Kazmirski, Steven L.; Kettle, Jason G.; Lamb, Michelle L.; Matulis, Shannon M.; Nooka, Ajay K.; Packer, Martin J.; Peng, Bo; Rawlins, Philip B.; Robbins, Daniel W.; Schuller, Alwin G.; Su, Nancy; Yang, Wenzhan; Ye, Qing; Zheng, Xiaolan; Secrist, J. Paul; Clark, Edwin A.; Wilson, David M.; Fawell, Stephen E.; Hird, Alexander W. 分享 收藏
Selective Mcl-1 inhibition by AZD5991 induces on-target cell death and achieves antitumor activity in multiple myeloma and acute myeloid leukemia Tron, Adriana E.; Belmonte, Matthew A.; Criscione, Steven; Clark, Edwin A.; Gangl, Eric; Gibbons, Francis D.; Tyner, Jeffrey W.; Kurtz, Stephen E.; Ye, Qing; Hird, Alexander W.; Schuller, Alwin; Secrist, J. Paul 分享 收藏
A semi-mechanistic pharmacokinetic-pharmacodynamic (PK-PD) model of savolitinib (AZD6094/HMPL-504), a novel MET inhibitor, to explore extent and duration of target inhibition required for optimal efficacy in the EBC-1 mouse xenograft model Jones, Rhys D.; Grondine, Michael; Borodovsky, Alexandra; San Martin, Maryann; DuPont, Michelle; D'Cruz, Celina; Schuller, Alwin; Henry, Ryan; Barry, Evan; Petersson, Klas; Sahota, Tarjinder; Ahmed, Ghada F. 分享 收藏
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Pharmacodynamic response and anti-tumor activity of the MET inhibitor AZD6094 in papillary renal cell carcinoma patient derived xenograft models Schuller, Alwin; Barry, Evan; Jones, Rhys; Frigault, Melanie; Beran, Garry; Henry, Ryan; Linsenmayer, David; Hattersley, Maureen; Smith, Aaron; Wilson, Joanne; Adam, Ammar; Zinda, Michael; Reimer, Corinne; Fawell, Stephen; Clark, Edwin; D'Cruz, Celina 分享 收藏
Changing the paradigm for treating drug resistance in NSCLC: Novel combinations of AZD6094, a selective MET inhibitor, and an irreversible, selective (EGFRm/T790M) EGFRTKI, AZD9291 D'Cruz, Celina; Barry, Evan; Henry, Ryan; Castriotta, Lillian; Schuller, Alwin; Beran, Garry; Ashton, Susan; Eberlein, Cath; Reimer, Corinne; Frigault, Melanie; Zinda, Michael; Cross, Darren; Fawell, Stephen 分享 收藏
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