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Discovery of ART0380, a Potent and Selective ATR Kinase Inhibitor Undergoing Phase 2 Clinical Studies for the Treatment of Advanced or Metastatic Solid Cancers Carroll, Christopher L.; Johnson, Michael G.; Ding, Yanbing; Kang, Zhijun; Vijayan, R. S. K.; Bardenhagen, Jennifer P.; Fang, Cheng; Lapointe, David; Li, Meng; Liu, Chiu-Yi; Lv, Xiaobing; Ma, Xiaoyan; Pang, Jihai; Shepard, Hannah E.; Suarez, Catalina; Yau, Anne Ju; Williams, Christopher C.; Wu, Qi; Heald, Robert A.; Robinson, Helen M. R.; Smith, Graeme C. M.; Cross, Jason B.; Do, Mary K. Geck; Jiang, Yongying; Lively, Sarah; Yap, Timothy A.; Giuliani, Virginia; Heffernan, Timothy; Jones, Philip; Di Francesco, M. Emilia Share Save
The ATR inhibitor ART0380 shows preclinical efficacy in monotherapy or in combination with gemcitabine, aPD1, PARP inhibitors and topoisomerase 1 poisons Majithiya, Jayesh Bhanabhai; Luzarraga, Marina Roy; Newman, Richard; Costales, Paula; Jones, Philip; Di Francesco, Maria Emilia; Giuliani, Virginia; Caroll, Chris; Do, Mary Geck; Heffernan, Tim; Feng, Ningpeng; Ma, XiaoYan; Lively, Sarah; Johnson, Michael G.; Geo, Lerin; Piscitello, Desiree; Rajendra, Eeson; Grinkevich, Vera; Ranzani, Marco; Stockley, Martin; Langford, Gillian; Heald, Robert; Robinson, Helen M.; Smith, Graeme C. Share Save
PRMT1-dependent regulation of RNA metabolism and DNA damage response sustains pancreatic ductal adenocarcinoma Giuliani, Virginia; Miller, Meredith A.; Liu, Chiu-Yi; Hartono, Stella R.; Class, Caleb A.; Bristow, Christopher A.; Suzuki, Erika; Sanz, Lionel A.; Gao, Guang; Gay, Jason P.; Feng, Ningping; Rose, Johnathon L.; Tomihara, Hideo; Daniele, Joseph R.; Peoples, Michael D.; Bardenhagen, Jennifer P.; Geck Do, Mary K.; Chang, Qing E.; Vangamudi, Bhavatarini; Vellano, Christopher; Ying, Haoqiang; Deem, Angela K.; Do, Kim-Anh; Genovese, Giannicola; Marszalek, Joseph R.; Kovacs, Jeffrey J.; Kim, Michael; Fleming, Jason B.; Guccione, Ernesto; Viale, Andrea; Maitra, Anirban; Emilia Di Francesco, M.; Yap, Timothy A.; Jones, Philip; Draetta, Giulio; Carugo, Alessandro; Chedin, Frederic; Heffernan, Timothy P. Share Save
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties Soth, Michael J.; Le, Kang; Di Francesco, Maria Emilia; Hamilton, Matthew M.; Liu, Gang; Burke, Jason P.; Carroll, Chris L.; Kovacs, Jeffrey J.; Bardenhagen, Jennifer P.; Bristow, Christopher A.; Cardozo, Mario; Czako, Barbara; de Stanchina, Elisa; Feng, Ningping; Garvey, Jill R.; Gay, Jason P.; Do, Mary K. Geck; Greer, Jennifer; Han, Michelle; Harris, Angela; Herrera, Zachary; Huang, Sha; Giuliani, Virginia; Jiang, Yongying; Johnson, Sarah B.; Johnson, Troy A.; Kang, Zhijun; Leonard, Paul G.; Liu, Zhen; McAfoos, Timothy; Miller, Meredith; Morlacchi, Pietro; Mullinax, Robert A.; Palmer, Wylie S.; Pang, Jihai; Rogers, Norma; Rudin, Charles M.; Shepard, Hannah E.; Spencer, Nakia D.; Theroff, Jay; Wu, Qi; Xu, Alan; Yau, Ju Anne; Draetta, Giulio; Toniatti, Carlo; Heffernan, Timothy P.; Jones, Philip Share Save
Functional Genomics Reveals Synthetic Lethality between Phosphogluconate Dehydrogenase and Oxidative Phosphorylation Sun, Yuting; Bandi, Madhavi; Lofton, Timothy; Smith, Melinda; Bristow, Christopher A.; Carugo, Alessandro; Rogers, Norma; Leonard, Paul; Chang, Qing; Mullinax, Robert; Han, Jing; Shi, Xi; Seth, Sahil; Meyers, Brooke A.; Miller, Meredith; Miao, Lili; Ma, Xiaoyan; Feng, Ningping; Giuliani, Virginia; Do, Mary Geck; Czako, Barbara; Palmer, Wylie S.; Mseeh, Faika; Asara, John M.; Jiang, Yongying; Morlacchi, Pietro; Zhao, Shuping; Peoples, Michael; Tieu, Trang N.; Warmoes, Marc O.; Lorenzi, Philip L.; Muller, Florian L.; DePinho, Ronald A.; Draetta, Giulio F.; Toniatti, Carlo; Jones, Philip; Heffernan, Timothy P.; Marszalek, Joseph R. Share Save
Discovery and development of IACS-010759, a novel inhibitor of Complex I currently in phase I studies to exploit oxidative phosphorylation dependency in acute myeloid leukemia and solid tumors Di Francesco, Maria Emilia; Marszalek, Joseph R.; McAfoos, Timothy; Carroll, Christopher L.; Kang, Zhijun; Liu, Gang; Theroff, Jay P.; Bardenhager, Jennifer P.; Bandi, Madhavi L.; Molina, Jennifer R.; Gera, Sonal; Protopopova, Marina; Sun, Yuting; Do, Mary K. Geck; Feng, Ningping; Gay, Jason P.; Muller, Florian; Konopleva, Marina; Meric-Bernstam, Funda; Toniatti, Carlo; Heffernan, Timothy P.; Draetta, Giulio F.; Jones, Philip Share Save
An inhibitor of oxidative phosphorylation exploits cancer vulnerability Molina, Jennifer R.; Sun, Yuting; Protopopova, Marina; Gera, Sonal; Bandi, Madhavi; Bristow, Christopher; McAfoos, Timothy; Morlacchi, Pietro; Ackroyd, Jeffrey; Agip, Ahmed-Noor A.; Al-Atrash, Gheath; Asara, John; Bardenhagen, Jennifer; Carrillo, Caroline C.; Carroll, Christopher; Chang, Edward; Ciurea, Stefan; Cross, Jason B.; Czako, Barbara; Deem, Angela; Daver, Naval; de Groot, John Frederick; Dong, Jian-Wen; Feng, Ningping; Gao, Guang; Gay, Jason; Do, Mary Geck; Greer, Jennifer; Giuliani, Virginia; Han, Jing; Han, Lina; Henry, Verlene K.; Hirst, Judy; Huang, Sha; Jiang, Yongying; Kang, Zhijun; Khor, Tin; Konoplev, Sergej; Lin, Yu-Hsi; Liu, Gang; Lodi, Alessia; Lofton, Timothy; Ma, Helen; Mahendra, Mikhila; Matre, Polina; Mullinax, Robert; Peoples, Michael; Petrocchi, Alessia; Rodriguez-Canale, Jaime; Serreli, Riccardo; Shi, Thomas; Smith, Melinda; Tabe, Yoko; Theroff, Jay; Tiziani, Stefano; Xu, Quanyun; Zhang, Qi; Muller, Florian; DePinho, Ronald A.; Toniatti, Carlo; Draetta, Giulio F.; Heffernan, Timothy P.; Konopleva, Marina; Jones, Philip; Di Francesco, M. Emilia; Marszalek, Joseph R. Share Save
IACS-010759, a novel inhibitor of complex I in Phase I clinical development to target OXPHOS dependent tumors Molina, Jennifer; Bandi, Madhavi; Bardenhagen, Jennifer; Bristow, Christopher; Carroll, Christopher; Chang, Edward; Cross, Jason; Daver, Naval; Feng, Ningping; Gay, Jason; Do, Mary Geck; Greer, Jennifer; Han, Jing; Hirst, Judy; Huang, Sha; Jiang, Yongying; Kang, Zhijun; Konopleva, Marina; Liu, Gang; Ma, Helen; Matre, Polina; McAfoos, Timothy; Meric-Bernstam, Funda; Morlacchi, Pietro; Muller, Florian; Protopopova, Marina; Smith, Melinda; Sonal, Sonal; Sun, Yuting; Theroff, Jay; Viale, Andrea; Xu, Quanyun; Toniatti, Carlo; Draetta, Giulio; Jones, Philip; Di Francesco, M. Emilia; Marszalek, Joseph R. Share Save
Title: IACS-010759 is a novel clinical candidate that targets AML cells by inducing a metabolic catastrophe through inhibition of oxidative phosphorylation Molina, Jennifer R.; Protopopova, Marina; Bandi, Madhavi; Bardenhagen, Jennifer; Bristow, Christopher; Carroll, Christopher; Chang, Edward; Feng, Ningping; Gay, Jason; Do, Mary Geck; Greer, Jennifer; Huang, Sha; Jiang, Yongying; Konopleva, Marina; Matre, Polina; Han, Jing; Kang, Zhijun; Liu, Gang; McAfoos, Timothy; Morlacchi, Pietro; Smith, Melinda; Gera, Sonal; Theroff, Jay; Xu, Quanyun; Velez, Juliana; Toniatti, Carlo; Heffernan, Timothy; Draetta, Giulio; Di Francesco, M. Emilia; Jones, Philip; Marszalek, Joseph R. Share Save
Functional genomics reveals dependency on 6-phosphogluconate dehydrogenase in OXPHOS-deficient tumors Sun, Yuting; Bandi, Madhavi; Lofton, Timothy; Smith, Melinda; Bristow, Christopher; Rogers, Norma; Edward, Chang; Do, Mary Geck; Jiang, Yongying; Morlacchi, Pietro; Muller, Florian; Mseeh, Faika; Czako, Barbara; Palmer, Wylie; Toniatti, Carlo; Jones, Philip; Draetta, Giulio; Heffernan, Timothy; Marszalek, Joseph Share Save
IACS-10759: A novel OXPHOS inhibitor that selectively kills tumors with metabolic vulnerabilities Protopopova, Marina; Bandi, Madhavi; Sun, Yuting; Bardenhagen, Jennifer; Bristow, Christopher; Carroll, Christopher; Chang, Edward; Feng, Ningping; Gay, Jason; Do, Mary Geck; Greer, Jennifer; Konopleva, Marina; Matre, Polina; Kang, Zhijun; Liu, Gang; Muller, Florian; Lofton, Timothy; McAfoos, Timothy; Smith, Melinda; Theroff, Jay; Han, Jing; Wu, Yuanqing; Chin, Lynda; Draetta, Giulio; Jones, Philip; Toniatti, Carlo; Di Francesco, M. Emilia; Marszalek, Joseph R. Share Save
Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery Zhan, Yanai; Kost-Alimova, Maria; Shi, Xi; Leo, Elisabetta; Bardenhagen, Jennifer P.; Shepard, Hannah E.; Appikonda, Srikanth; Vangamudi, Bhavatarini; Zhao, Shuping; Tieu, Trang N.; Jiang, Shiming; Heffernan, Timothy P.; Marszalek, Joseph R.; Toniatti, Carlo; Draetta, Giulio; Tyler, Jessica; Barton, Michelle; Jones, Philip; Palmer, Wylie S.; Do, Mary K. Geck; Andersen, Jannik N. Share Save
Relapsed/refractory AML responds robustly to IACS-10759, a novel OXPHOS inhibitor Protopopova, Marina; Bandi, Madhavi; Bardenhagen, Jennifer; Bristow, Christophor; Carroll, Christopher; Chang, Edward; Feng, Ningping; Gay, Jason; Do, Mary Geck; Greer, Jennifer; Konopleva, Marina; Matre, Polina; Kang, Zhijun; Liu, Gang; Muller, Florian; Lofton, Timothy; McAfoos, Timothy; Theroff, Jay; Sun, Yuting; Wu, Yuanqiang; Smith, Melinda; Chin, Lynda; Draetta, Giulio; Jones, Philip; Toniatti, Carlo; Di Francesco, M. Emilia; Marszalek, Joseph R. Share Save
IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities Protopopova, Marina; Bandi, Madhavi; Bardenhagen, Jennifer; Bristow, Christopher; Carroll, Christopher; Chang, Edward; Feng, Ningping; Gay, Jason; Do, Mary Geck; Greer, Jennifer; Konopleva, Marina; Matre, Polina; Kang, Zhijun; Liu, Gang; Muller, Florian; Lofton, Timothy; McAfoos, Timothy; Sun, Yuting; Smith, Melinda; Theroff, Jay; Wu, Yuanqiang; Chin, Lynda; Draetta, Giulio; Jones, Philip; Toniatti, Carlo; Di Francesco, M. Emilia; Marszalek, Joseph R. Share Save
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor Palmer, Wylie S.; Poncet-Montange, Guillaume; Liu, Gang; Petrocchi, Alessia; Reyna, Naphtali; Subramanian, Govindan; Theroff, Jay; Yau, Anne; Kost-Alimova, Maria; Bardenhagen, Jennifer P.; Leo, Elisabetta; Shepard, Hannah E.; Tieu, Trang N.; Shi, Xi; Zhao, Yanai; Zhao, Shuping; Barton, Michelle C.; Draetta, Giulio; Toniatti, Carlo; Jones, Philip; Do, Mary Geck; Andersen, Jannik N. Share Save
Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2 Poncet-Montange, Guillaume; Zhan, Yanai; Bardenhagen, Jennifer P.; Petrocchi, Alessia; Leo, Elisabetta; Shi, Xi; Lee, Gilbert R.; Leonard, Paul G.; Do, Mary K. Geck; Cardozo, Mario G.; Andersen, Jannik N.; Palmer, Wylie S.; Jones, Philip; Ladbury, John E. Share Save
8-Tetrahydropyran-2-yl Chromans: Highly Selective Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors Thomas, Allen A.; Hunt, Kevin W.; Newhouse, Brad; Watts, Ryan J.; Liu, Xingrong; Vigers, Guy; Smith, Darin; Rhodes, Susan P.; Brown, Karin D.; Otten, Jennifer N.; Burkard, Michael; Cox, April A.; Do, Mary K. Geck; Dutcher, Darrin; Rana, Sumeet; DeLisle, Robert K.; Regal, Kelly; Wright, Albion D.; Groneberg, Robert; Liao, Jiangpeng; Scearce-Levie, Kimberly; Siu, Michael; Purkey, Hans E.; Lyssikatos, Joseph P. Share Save
Identification of OXPHOS inhibitors which selectively kill tumors with specific metabolic vulnerabilities Marszalek, Joseph R.; Bandi, Madhavi; Bardenhagen, Jennifer; Bristow, Christopher; Carroll, Christopher; Chang, Edward; Feng, Ninping; Czako, Barbara; Gay, Jason; Do, Mary Geck; Greer, Jennifer; Johnson, Ryan M.; Konopleva, Marina; Kang, Zhijun; Liu, Gang; Lofton, Timothy; McAfoos, Timothy; Protopopova, Marina; Petrocchi, Alessia; Muller, Florian; Theroff, Jay; Wu, Yuanqing; Chin, Lynda; Draetta, Giulio; Jones, Philip; Toniatti, Carlo; Di Francesco, Emilia Share Save
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