未登录Discovery and Characterization of Novel BLIMP-1 Heterobifunctional Ligand-Directed Degraders新型BLIMP-1杂双功能配体定向降解剂的发现与表征
Simmons, Bryan J.; Groocock, Lynda; Moreno, Jesus; Peters, David S.; Hughes, Meredith E.; Veeravalli, Vijay; Crawford, Jennifer M.; Chalkley, Matthew; Griffith, Mark; Plooster, Melissa; Hu, Bo; Gamez, Jim; Leisten, Jim; Barnes, Michael J.; Chinn, Jason; Deb, Gauri; Modi, Hardik; Katepalli, Madhu; Weiss, Dahlia; Won, Walter; Sun, Zhenghang; Yu, Shan; Reid, Cameron; Donnell, Andrew F.; Li, Ling; Watson, Edmond R.; Perrin-Ninkovic, Sophie; Shi, Lihong; Narla, Rama Krishna; Zapf, Christoph W.; Bence, Neil; Lopez-Girona, Antonia; Riggs, Jennifer R. .png)
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收藏Synergistic Activity of BMS-986397, a First-in-Class a Cereblon (CRBN) E3 Ligase Modulator (CELMoD) Targeting Casein Kinase 1α (CK1α), in Combination with Venetoclax and/or Azacitidine in Preclinical Models of Acute Myeloid Leukemia (AML)BMS-986397的协同活性，BMS-986397是一种靶向酪蛋白激酶1α（CK1α）的首创类cereblon（CRBN）E3连接酶调节剂（CELMoD），与Venetoclax和/或Azacitidine在急性髓系白血病（AML）的预临床模型中的联合作用。Jimenez, Carmen; Lopez, Jose Francisco; Garcia, Estela; Regalado, Laura Diaz; Panjkovich, Alejandro; Peng, Sophie; Narla, Rama Krishna; Purroy, Noelia; Rolfe, Mark; Pierce, Daniel W.; Carrancio, Soraya 分享 收藏 BMS-986397, a First-in-Class Molecular Glue Degrader of Casein Kinase 1α (CK1α) for the Treatment of Acute Myeloid Leukemia (AML) and High-Risk Myelodysplastic Syndrome (HR-MDS) Harboring Functional TP53BMS-986397，一种新型分子胶降解剂，可靶向酪蛋白激酶1α（CK1α），用于治疗携带功能性TP53基因的急性髓系白血病（AML）和高风险骨髓增生异常综合征（HR-MDS）。Jimenez, Carmen; Peng, Sophie; Narla, Rama Krishna; Baughman, Joshua; Wood, Scott; Lu, Jean; Purroy, Noelia; Yanochko, Gina; Nagy, Mark; Lu, Gang; Rolfe, Mark; Pierce, Daniel W.; Carrancio, Soraya 分享 收藏 Discovery of BMS-986365, a ligand-directed androgen receptor degrader (AR LDD) with a dual mechanism-of-action and best-in-class potential, for the treatment of advanced prostate cancerXu, Shuichan; Nayak, Surendra; Norris, John D.; Ammirante, Massimo; Rychak, Emyly; Wardell, Suzanne E.; Tsuji, Toshiya; Liu, Ken; Meiring, Joseph; Piccotti, Joseph R.; Dalvie, Deepak; Liao, Debbie; Kandimalla, Raju; Guerrero, Nadia; Sapinoso, Lisa; Baker, Jennifer G.; Bae, Yeeun; Baughman, Joshua; Toyama, Brandon; Fontanillo, Celia Fontanillo; Norris, Stephen; Horn, Evan J.; Plantevin-Krenitsky, Veronique; Mortensen, Deborah; Cathers, Brian; Nguyen, Marie Hong; Hensen, Joshua D.; Hamann, Lawrence G.; McDonnell, Donald P.; Narla, Rama Krishna; Rolfe, Mark 分享 收藏 CC-96673 (BMS-986358), an affinity-tuned anti-CD47 and CD20 bispecific antibody with fully functional fc, selectively targets and depletes non-Hodgkin's lymphomaCC-96673 (BMS-986358) 是一种亲和力调节的anti-CD47和CD20双特异性抗体，具有完全功能的fc，选择性靶向和耗尽非霍奇金淋巴瘤Zhu, Dan; Hadjivassiliou, Haralambos; Jennings, Catherine; Mikolon, David; Ammirante, Massimo; Acharya, Sharmistha; Lloyd, Jon; Abbasian, Mahan; Narla, Rama Krishna; Piccotti, Joseph R.; Stamp, Katie; Cho, Ho; Hariharan, Kandasamy 分享 收藏 SMG1, a nonsense-mediated mRNA decay (NMD) regulator, as a candidate therapeutic target in multiple myelomaLeeksma, Alexander C.; Derks, Ingrid A. M.; Garrick, Brett; Jongejan, Aldo; Colombo, Martino; Bloedjes, Timon; Trowe, Torsten; Leisten, Jim C.; Howarth, Michelle; Malek, Mehnaz; Mortensen, Deborah S.; Blease, Kate; Groza, Mathew C.; Narla, Rama Krishna; Loos, Remco; Kersten, Marie-Jose; Moerland, Perry D.; Guikema, Jeroen E. J.; Kater, Arnon P.; Eldering, Eric; Filvaroff, Ellen H. 分享 收藏 Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor ActivityElsner, Jan; Cashion, Dan; Robinson, Dale; Bahmanyar, Sogole; Tehrani, Lida; Fultz, Kimberly E.; Narla, Rama Krishna; Peng, Xiaohui; Tran, Tam; Apuy, Julius; LeBrun, Laurie; Leftheris, Katerina; Boylan, John F.; Zhu, Dan; Riggs, Jennifer R. 分享 收藏 CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid LeukemiaHansen, Joshua D.; Correa, Matthew; Alexander, Matt; Nagy, Mark; Huang, Dehua; Sapienza, John; Lu, Gang; LeBrun, Laurie A.; Cathers, Brian E.; Zhang, Weihong; Tang, Yang; Ammirante, Massimo; Narla, Rama K.; Piccotti, Joseph R.; Pourdehnad, Michael; Lopez-Girona, Antonia 分享 收藏 Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple MyelomaHansen, Joshua D.; Correa, Matthew; Nagy, Mark A.; Alexander, Matt; Plantevin, Veronique; Grant, Virginia; Whitefield, Brandon; Huang, Dehua; Kercher, Timothy; Harris, Roy; Narla, Rama Krishna; Leisten, Jim; Tang, Yang; Moghaddam, Mehran; Ebinger, Katalin; Piccotti, Joseph; Havens, Courtney G.; Cathers, Brian; Carmichael, James; Daniel, Thomas; Vessey, Rupert; Hamann, Lawrence G.; Leftheris, Katerina; Mendy, Derek; Baculi, Frans; LeBrun, Laurie A.; Khambatta, Gody; Lopez-Girona, Antonia 分享 收藏 Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent EfficacyRiggs, Jennifer R.; Elsner, Jan; Cashion, Dan; Robinson, Dale; Tehrani, Lida; Nagy, Mark; Fultz, Kimberly E.; Narla, Rama Krishna; Peng, Xiaohui; Tran, Tam; Kulkarni, Ashutosh; Bahmanyar, Sogole; Condroski, Kevin; Pagarigan, Barbra; Fenalti, Gustavo; LeBrun, Laurie; Leftheris, Katerina; Zhu, Dan; Boylan, John F. 分享 收藏 Synthetic Lethal Strategy Identifies a Potent and Selective TTK and CLK1/2 Inhibitor for Treatment of Triple-Negative Breast Cancer with a Compromised G1-S CheckpointZhu, Dan; Xu, Shuichan; Deyanat-Yazdi, Gordafaried; Peng, Sophie X.; Barnes, Leo A.; Narla, Rama Krishna; Tran, Tam; Mikolon, David; Ning, Yuhong; Shi, Tao; Jiang, Ning; Raymon, Heather K.; Riggs, Jennifer R.; Boylan, John F. 分享 收藏 分享 收藏 The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic ScreenRiggs, Jennifer R.; Nagy, Mark; Elsner, Jan; Erdman, Paul; Cashion, Dan; Robinson, Dale; Harris, Roy; Huang, Dehua; Tehrani, Lida; Deyanat-Yazdi, Gordafaried; Narla, Rama Krishna; Peng, Xiaohui; Tam Tran; Barnes, Leo; Miller, Terra; Katz, Jason; Tang, Yang; Chen, Ming; Moghaddam, Mehran F.; Bahmanyar, Sogole; Pagarigan, Barbra; Delker, Silvia; LeBrun, Laurie; Chamberlain, Philip P.; Calabrese, Andrew; Canan, Stacie S.; Leftheris, Katerina; Zhu, Dan; Boylan, John F. 分享 收藏 CC-90002 (anti-CD47 antibody) in vivo anti-tumor activity is associated with an increase in M1-polarized macrophagesZheng, Bing; Wong, Piu; Yang, WenQing; Narla, Rama; Burgess, Michael; Escoubet, Laure; Raymon, Heather; Hariharan, Kandasamy; Boylan, John; Hege, Kristen; Sung, Victoria 分享 收藏 The humanized anti-CD47 monclonal antibody, CC-90002, has antitumor activity in vitro and in vivoNarla, Rama Krishna; Modi, Hardik; Wong, Lilly; Abassian, Mahan; Bauer, Daniel; Desai, Pragnya; Gaffney, Bonny; Jackson, Pilgrim; Leisten, Jim; Liu, Jing; Lopez-Girona, Antonia; Romero, Maria; Yang, WenQing; Eckelman, Brendan P.; Deveraux, Quinn; Phillips, Laurie; Raymon, Heather K.; Escoubet, Laure; Boylan, John; Hariharan, Kandasamy 分享 收藏 Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115Mortensen, Deborah S.; Perrin-Ninkovic, Sophie M.; Shevlin, Graziella; Elsner, Jan; Zhao, Jingjing; Whitefield, Brandon; Tehrani, Lida; Sapienza, John; Riggs, Jennifer R.; Parnes, Jason S.; Papa, Patrick; Packard, Garrick; Lee, Branden G. S.; Harris, Roy; Correa, Matthew; Bahmanyar, Sogole; Richardson, Samantha J.; Peng, Sophie X.; Leisten, Jim; Khambatta, Godrej; Hickman, Matt; Gamez, James C.; Bisonette, Rene R.; Apuy, Julius; Gathers, Brian E.; Canan, Stacie S.; Moghaddam, Mehran F.; Raymon, Heather K.; Worland, Peter; Narla, Rama Krishna; Fultz, Kimberly E.; Sankar, Sabita 分享 收藏 Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223Mortensen, Deborah S.; Perrin-Ninkovic, Sophie M.; Shevlin, Graziella; Zhao, Jingjing; Packard, Garrick; Bahmanyar, Sogole; Correa, Matthew; Elsner, Jan; Harris, Roy; Lee, Branden G. S.; Papa, Patrick; Parnes, Jason S.; Riggs, Jennifer R.; Sapienza, John; Tehrani, Lida; Whitefield, Brandon; Apuy, Julius; Bisonette, Rene R.; Gamez, James C.; Hickman, Matt; Khambatta, Godrej; Leisten, Jim; Peng, Sophie X.; Richardson, Samantha J.; Gathers, Brian E.; Callan, Stacie S.; Moghaddam, Mehran F.; Raymon, Heather K.; Worland, Peter; Narla, Rama Krishna; Fultz, Kimberly E.; Sankar, Sabita 分享 收藏 CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo CharacterizationMortensen, Deborah S.; Fultz, Kimberly E.; Xu, Shuichan; Xu, Weiming; Packard, Garrick; Khambatta, Godrej; Gamez, James C.; Leisten, Jim; Zhao, Jingjing; Apuy, Julius; Ghoreishi, Kamran; Hickman, Matt; Narla, Rama Krishna; Bissonette, Rene; Richardson, Samantha; Peng, Sophie X.; Perrin-Ninkovic, Sophie; Tran, Tam; Shi, Tao; Yang, Wen Qing; Tong, Zeen; Cathers, Brian E.; Moghaddam, Mehran F.; Canan, Stacie S.; Worland, Peter; Sankar, Sabita; Raymon, Heather K. 分享 收藏 Antitumor activity of mTOR kinase and DNA-PK inhibitor CC-115 in a mouse model of glioblastomaRaymon, H.; Peng, S.; Katz, J.; Zhao, C.; Phan, C.; Moghaddam, M. F.; Fultz, K. E.; Sankar, S.; Mortensen, D. S.; Narla, R. K. 分享 收藏 Preclinical characterization of CC-115, a novel inhibitor of DNA-PK and mTOR kinase currently under clinical investigationMortensen, D. S.; Fultz, K. E.; Xu, W.; Tsuji, T.; Hickman, M.; Abbasian, M.; Khambatta, G.; Cathers, B.; Worland, P.; Moghaddam, M. F.; Apuy, J.; Richardson, S.; Elsner, J.; Shevlin, G.; Perrin-Ninkovic, S.; Canan, S.; Raymon, H. K.; Narla, R. K.; Peng, S.; Sankar, S. 分享 收藏 
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