Not logged in 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
Complex I inhibitor of oxidative phosphorylation in advanced solid tumors and acute myeloid leukemia: phase I trials Yap, Timothy A.; Daver, Naval; Mahendra, Mikhila; Zhang, Jixiang; Kamiya-Matsuoka, Carlos; Meric-Bernstam, Funda; Kantarjian, Hagop M.; Ravandi, Farhad; Collins, Meghan E.; Di Francesco, Maria Emilia; Dumbrava, Ecaterina E.; Fu, Siqing; Gao, Sisi; Gay, Jason P.; Gera, Sonal; Han, Jing; Hong, David S.; Jabbour, Elias J.; Ju, Zhenlin; Karp, Daniel D.; Lodi, Alessia; Molina, Jennifer R.; Baran, Natalia; Naing, Aung; Ohanian, Maro; Pant, Shubham; Pemmaraju, Naveen; Bose, Prithviraj; Piha-Paul, Sarina A.; Rodon, Jordi; Salguero, Carolina; Sasaki, Koji; Singh, Anand K.; Subbiah, Vivek; Tsimberidou, Apostolia M.; Xu, Quanyun A.; Yilmaz, Musa; Zhang, Qi; Li, Yuan; Bristow, Christopher A.; Bhattacharjee, Meenakshi B.; Tiziani, Stefano; Heffernan, Timothy P.; Vellano, Christopher P.; Jones, Philip; Heijnen, Cobi J.; Kavelaars, Annemieke; Marszalek, Joseph R.; Konopleva, Marina Share Save
Inhibition of mitochondrial complex I reverses NOTCH1-driven metabolic reprogramming in T-cell acute lymphoblastic leukemia Baran, Natalia; Lodi, Alessia; Dhungana, Yogesh; Herbrich, Shelley; Collins, Meghan; Sweeney, Shannon; Pandey, Renu; Skwarska, Anna; Patel, Shraddha; Tremblay, Mathieu; Kuruvilla, Vinitha Mary; Cavazos, Antonio; Kaplan, Mecit; Warmoes, Marc O.; Veiga, Diogo Troggian; Furudate, Ken; Rojas-Sutterin, Shanti; Haman, Andre; Gareau, Yves; Marinier, Anne; Ma, Helen; Harutyunyan, Karine; Daher, May; Garcia, Luciana Melo; Al-Atrash, Gheath; Piya, Sujan; Ruvolo, Vivian; Yang, Wentao; Shanmugavelandy, Sriram Saravanan; Feng, Ningping; Gay, Jason; Du, Di; Yang, Jun J.; Hoff, Fieke W.; Kaminski, Marcin; Tomczak, Katarzyna; Eric Davis, R.; Herranz, Daniel; Ferrando, Adolfo; Jabbour, Elias J.; Emilia Di Francesco, M.; Teachey, David T.; Horton, Terzah M.; Kornblau, Steven; Rezvani, Katayoun; Sauvageau, Guy; Gagea, Mihai; Andreeff, Michael; Takahashi, Koichi; Marszalek, Joseph R.; Lorenzi, Philip L.; Yu, Jiyang; Tiziani, Stefano; Hoang, Trang; Konopleva, Marina Share Save
Discovery of 6-[(3S,4S)-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor Czako, Barbara; Sun, Yuting; McAfoos, Timothy; Cross, Jason B.; Leonard, Paul G.; Burke, Jason P.; Carroll, Christopher L.; Feng, Ningping; Harris, Angela L.; Jiang, Yongying; Kang, Zhijun; Kovacs, Jeffrey J.; Mandal, Pijus; Meyers, Brooke A.; Mseeh, Faika; Parker, Connor A.; Yu, Simon S.; Williams, Christopher C.; Wu, Qi; Di Francesco, Maria Emilia; Draetta, Giulio; Heffernan, Timothy; Marszalek, Joseph R.; Kohl, Nancy E.; Jones, Philip Share Save
Oxidative Phosphorylation Is a Metabolic Vulnerability in Chemotherapy-Resistant Triple-Negative Breast Cancer Evans, Kurt W.; Yuca, Erkan; Scott, Stephen S.; Zhao, Ming; Arango, Natalia Paez; Pico, Christian X. Cruz; Saridogan, Turcin; Shariati, Maryam; Class, Caleb A.; Bristow, Christopher A.; Vellano, Christopher P.; Zheng, Xiaofeng; Gonzalez-Angulo, Ana Maria; Su, Xiaoping; Tapia, Coya; Chen, Ken; Akcakanat, Argun; Lim, Bora; Tripathy, Debu; Yap, Timothy A.; Di Francesco, Maria Emilia; Draetta, Giulio F.; Jones, Philip; Heffernan, Timothy P.; Marszalek, Joseph R.; Meric-Bernstam, Funda 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
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Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib Sun, Yuting; Meyers, Brooke A.; Czako, Barbara; Leonard, Paul; Mseeh, Faika; Harris, Angela L.; Wu, Qi; Johnson, Sarah; Parker, Connor A.; Cross, Jason B.; Di Francesco, Maria Emilia; Bivona, Benjamin J.; Bristow, Christopher A.; Burke, Jason P.; Carrillo, Caroline C.; Carroll, Christopher L.; Chang, Qing; Feng, Ningping; Gao, Guang; Gera, Sonal; Giuliani, Virginia; Huang, Justin K.; Jiang, Yongying; Kang, Zhijun; Kovacs, Jeffrey J.; Liu, Chiu-Yi; Lopez, Anastasia M.; Ma, Xiaoyan; Mandal, Pijus K.; McAfoos, Timothy; Miller, Meredith A.; Mullinax, Robert A.; Peoples, Michael; Ramamoorthy, Vandhana; Seth, Sahil; Spencer, Nakia D.; Suzuki, Erika; Williams, Christopher C.; Yu, Simon S.; Zuniga, Andy M.; Draetta, Giulio F.; Marszalek, Joseph R.; Heffernan, Timothy P.; Kohl, Nancy E.; Jones, Philip 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
Discovery of IACS-13909, an allosteric SHP2 inhibitor that overcomes multiple mechanisms underlying osimertinib resistance Sun, Yuting; Meyers, Brooke A.; Johnson, Sarah B.; Harris, Angela L.; Czako, Barbara; Cross, Jason B.; Leonard, Paul G.; Mseeh, Faika; Di Francesco, Maria E.; Parker, Connor A.; Wu, Qi; Bristow, Christopher A.; Burke, Jason P.; Carrillo, Caroline C.; Carroll, Christopher L.; Chang, Qing; Feng, Ningping; Gera, Sonal; Guang, Gao; Huang, Justin Kwang-Lay; Jiang, Yongying; Kang, Zhijun; Kovacs, Jeffrey J.; Ma, Xiaoyan; Mandal, Pijus K.; McAfoos, Timothy; Mullinax, Robert A.; Peoples, Michael D.; Ramamoorthy, Vandhana; Seth, Sahil; Suzuki, Erika; Williams, Christopher Conrad; Yu, Simon S.; Zuniga, Andy M.; Draetta, Giulio F.; Marszalek, Joseph R.; Heffernan, Timothy P.; Kohl, Nancy E.; Jones, Philip Share Save
Oxidative phosphorylation is a metabolic vulnerability in chemotherapy resistant triple negative breast cancer Evans, Kurt; Moulder, Stacy; Yuca, Erkan; Scott, Stephen; Arango, Natalia Paez; Shariati, Maryam; Vellano, Christopher P.; Saridogan, Turcin; Zheng, Xiaofeng; Gonzalez-Angulo, Ana Maria; Zhao, Ming; Su, Xiaoping; Tapia, Coya; Chen, Ken; Akcakanat, Argun; Perou, Charles M.; Lim, Bora; Tripathy, Debu; Yap, Timothy A.; Di Francesco, Maria E.; Draetta, Giulio; Jones, Philip; Marszalek, Joe; Meric-Bernstam, Funda Share Save
Mechanism-Specific Pharmacodynamics of a Novel Complex-I Inhibitor Quantified by Imaging Reversal of Consumptive Hypoxia with [18F]FAZA PET In Vivo Gammon, Seth T.; Pisaneschi, Federica; Bandi, Madhavi L.; Smith, Melinda G.; Sun, Yuting; Rao, Yi; Muller, Florian; Wong, Franklin; De Groot, John; Ackroyd, Jeffrey; Mawlawi, Osama; Davies, Michael A.; Gopal, Y. N. Vashisht; Di Francesco, M. Emilia; Marszalek, Joseph R.; Dewhirst, Mark; Piwnica-Worms, David Share Save
Dissection of clonal heterogeneity unmasks pre-existing chemoresistance and new metabolic vulnerabilities in pancreatic cancer Seth, Sahil; Li, Chieh-Yuan; Loponte, Sara; Ho, I-Lin; Corti, Denise; Sapio, Luigi; Del Poggetto, Edoardo; Peoples, Michael; Karpinets, Tatiana; Robinson, Frederick S.; Jiang, Shan; Dutta, Prasanta; Marszalek, Joseph; Di Francesco, Maria E.; Heffernan, Timothy P.; Giuliani, Virginia; Bhattacharya, Pratip K.; Genovese, Giannicola; Futreal, Andrew; Draetta, Giulio; Viale, Andrea; Carugo, Alessandro Share Save
Inhibition of protein arginine methylation alters RNA metabolism and DNA damage response providing a new therapeutic strategy in pancreatic ductal adenocarcinoma Giuliani, Virginia; Carugo, Alessandro; Miller, Meredith; Sanz, Lionel; Liu, Chiu-Yi; Bristow, Christopher A.; Suzuki, Erika; Class, Caleb A.; Hartono, Stella R.; Gao, Guang; Feng, Ningping; Gay, Jason P.; Vangamudi, Bhavatarini; Marszalek, Joseph R.; Kovacs, Jeffrey; Di Francesco, Maria Emilia; Chedin, Frederic; Jones, Philip; Draetta, Giulio; Heffernan, Timothy Share Save
Metabolic reprogramming toward oxidative phosphorylation identifies a therapeutic target for mantle cell lymphoma Zhang, Liang; Yao, Yixin; Zhang, Shaojun; Liu, Yang; Guo, Hui; Ahmed, Makhdum; Bell, Taylor; Zhang, Hui; Han, Guangchun; Lorence, Elizabeth; Badillo, Maria; Zhou, Shouhao; Sun, Yuting; Di Francesco, M. Emilia; Feng, Ningping; Haun, Randy; Lan, Renny; Mackintosh, Samuel G.; Mao, Xizeng; Song, Xingzhi; Zhang, Jianhua; Pham, Lan, V; Lorenzi, Philip L.; Marszalek, Joseph; Heffernan, Tim; Draetta, Giulio; Jones, Philip; Futreal, Andrew; Nomie, Krystle; Wang, Linghua; Wang, Michael Share Save
Oxidative metabolism as a novel therapeutic target to eradicate T-ALL with mitochondrial complex I inhibitor IACS-010759 Baran, Natalia; Lodi, Alessia; Sweeney, Shannon; Kuruvilla, Vinitha Mary; Cavazos, Antonio; Skwarska, Anna; Velandy, Sriram Shanmuga; Harutyunyan, Karine; Feng, Ningping; Gay, Jason; Kaminski, Marcin; Jabbour, Elias J.; Ferrando, Adolfo; Di Francesco, M. Emilia; Marszalek, Joseph R.; Tiziani, Stefano; Konopleva, Marina Share Save
Targeting OXPHOS with IACS-010759 to eliminate standard of care resistant tumor cells Marszalek, Joseph R.; Seth, Sahil; Corti, Denise; Zhang, Qi; Echeverria, Gloria V.; Han, Lina; Sun, Yuting; Molina, Jennifer; Gera, Sonal; Chang, Edward; Khor, Tin O.; Mahendra, Mikhila; Feng, Ningping; Gay, Jason P.; McAfoos, Timothy; Giuliani, Virginia; Shi, Xi; Jeter-Jones, Sabrina; Loponte, Sarah; Li, Chieh-Yuan; Bristow, Christopher A.; Di Francesco, Maria Emilia; Piwnica-Worms, Helen; Konopleva, Marina; Carugo, Alessandro; Viale, Andrea; Jones, Philip; Heffernan, Timothy P.; Draetta, Giulio F. 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
Metabolic targeting of chemoresistance perturbs clonal complexity in pancreatic cancer Loponte, Sara; Corti, Denise; Seth, Sahil; Del Poggetto, Edoardo; Ho, I-Lin; Li, Chieh-Yuan; Jiang, Shan; Marszalek, Joseph R.; Di Francesco, Maria Emilia; Genovese, Giannicola; Draetta, Giulio; Carugo, Alessandro; Viale, Andrea Share Save
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