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IACS-16559, a CBP/P300 bromodomain inhibitor for the treatment of specific AML subsets Zanca, Ciro; Soth, Michael; Gao, Guang; Gay, Jason; Feng, Ningping; Bristow, Christopher; Le, Kang; Xu, Quanyun; Phuong Nguyen; Jiang, Yongying; Perry, Teresa; Mseeh, Faika; Leonard, Paul; Cross, Jason; Giuliani, Virginia; Marszalek, Joe; Jones, Philip; Heffernan, Tim Share Save
Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site Liu, Zhiqing; Li, Yi; Chen, Haiying; Lai, Hsien-Tsung; Wang, Pingyuan; Wu, Shwu-Yuan; Wold, Eric A.; Leonard, Paul G.; Joseph, Sarah; Hu, Haitao; Chiang, Cheng-Ming; Brasier, Allan R.; Tian, Bing; Zhou, Jia Share Save
BBP-398, a potent, small molecule inhibitor of SHP2, enhances the response of established NSCLC xenografts to KRASG12C and mutEGFR inhibitors Stice, James P.; Donovan, Sofia; Sun, Yuting; Kohl, Nancy; Czako, Barbara; Mseeh, Faika; Leonard, Paul; Wade, Anna; Lim, Justin; Jones, Phil; Wallace, Eli; Sinkevicius, Kerstin; Beltran, Pedro 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
GRB2 enforces homology-directed repair initiation by MRE11 Ye, Zu; Xu, Shengfeng; Shi, Yin; Bacolla, Albino; Syed, Aleem; Moiani, Davide; Tsai, Chi-Lin; Shen, Qiang; Peng, Guang; Leonard, Paul G.; Jones, Darin E.; Wang, Bin; Tainer, John A.; Ahmed, Zamal Share Save
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme Hamilton, Matthew M.; Mseeh, Faika; McAfoos, Timothy J.; Leonard, Paul G.; Reyna, Naphtali J.; Harris, Angela L.; Xu, Alan; Han, Michelle; Soth, Michael J.; Czako, Barbara; Theroff, Jay P.; Mandal, Pijus K.; Burke, Jason P.; Virgin-Downey, Brett; Petrocchi, Alessia; Pfaffinger, Dana; Rogers, Norma E.; Parker, Connor A.; Yu, Simon S.; Jiang, Yongying; Krapp, Stephan; Lammens, Alfred; Trevitt, Graham; Tremblay, Martin R.; Mikule, Keith; Wilcoxen, Keith; Cross, Jason B.; Jones, Philip; Marszalek, Joseph R.; Lewis, Richard T. Share Save
An enolase inhibitor for the targeted treatment of ENO1-deleted cancers (vol 2, pg 1413, 2020) Lin, Yu-Hsi; Satani, Nikunj; Hammoudi, Naima; Yan, Victoria C.; Barekatain, Yasaman; Khadka, Sunada; Ackroyd, Jeffrey J.; Georgiou, Dimitra K.; Pham, Cong-Dat; Arthur, Kenisha; Maxwell, David; Peng, Zhenghong; Leonard, Paul G.; Czako, Barbara; Pisaneschi, Federica; Mandal, Pijus; Sun, Yuting; Zielinski, Rafal; Pando, Susana Castro; Wang, Xiaobo; Tran, Theresa; Xu, Quanyu; Wu, Qi; Jiang, Yongying; Kang, Zhijun; Asara, John M.; Priebe, Waldemar; Bornmann, William; Marszalek, Joseph R.; DePinho, Ronald A.; Muller, Florian L. Share Save
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-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R Czako, Barbara; Marszalek, Joseph. R.; Burke, Jason P.; Mandal, Pijus; Leonard, Paul G.; Cross, Jason B.; Mseeh, Faika; Jiang, Yongying; Chang, Edward Q.; Suzuki, Erika; Kovacs, Jeffrey J.; Feng, Ningping; Gera, Sonal; Harris, Angela L.; Liu, Zhen; Mullinax, Robert A.; Pang, Jihai; Parker, Connor A.; Spencer, Nakia D.; Yu, Simon S.; Wu, Qi; Tremblay, Martin R.; Mikule, Keith; Wilcoxen, Keith; Heffernan, Timothy P.; Draetta, Giulio F.; Jones, Philip Share Save
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation Liu, Zhiqing; Chen, Haiying; Wang, Pingyuan; Li, Yi; Wold, Eric A.; Leonard, Paul G.; Joseph, Sarah; Brasier, Allan R.; Tian, Bing; Zhou, Jia 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
The 3S Enantiomer Drives Enolase Inhibitory Activity in SF2312 and Its Analogues Pisaneschi, Federica; Lin, Yu-Hsi; Leonard, Paul G.; Satani, Nikunj; Yan, Victoria C.; Hammoudi, Naima; Raghavan, Sudhir; Link, Todd M.; Georgiou, Dimitra K.; Czako, Barbara; Muller, Florian L. Share Save
IACS-9779, a development candidate that inhibits 2,3-dioxygenase (IDO) activity by blocking heme incorporation into IDO apoenzyme Mseeh, Faika; Hamilton, Matthew M.; Marszalek, Joseph R.; Rogers, Norma E.; Parker, Connor A.; Yu, Simon S.; Liu, Zhen; Reyna, Naphtali J.; McAfoos, Timothy; Virgin-Downey, Brett W.; Leonard, Paul G.; Cross, Jason B.; Feng, Ningping; Harris, Angela L.; Zuniga, Andy M.; Mikule, Keith; Tremblay, Martin; Jiang, Yongying; Mahendra, Mikhila; Pang, Jihai; Wu, Qi; Xu, Quanyun; Heffernan, Timothy P.; Jones, Philip; Lewis, Richard T. 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
Neomorphic PDGFRA extracellular domain driver mutations are resistant to PDGFRA targeted therapies Ip, Carman K. M.; Ng, Patrick K. S.; Jeong, Kang Jin; Shao, S. H.; Ju, Zhenlin; Leonard, P. G.; Hua, Xu; Vellano, Christopher P.; Woessner, Richard; Sahni, Nidhi; Scott, Kenneth L.; Mills, Gordon B. Share Save
Discovery of an imidazopyridine series of potent human IDO1 inhibitors with robust target engagement in a preclinical tumor model Petrocchi, Alessia; Reyna, Naphtali J.; Mseeh, Faika; Parker, Connor A.; Yu, Simon; Xu, Quanyun; Feng, Ningping; Leonard, Paul; Rogers, Norma; Cross, Jason B.; Harris, Angela L.; Jiang, Yongying; Khor, Tin Oo; Mahendra, Mikhila G.; Pang, Jihai; Wu, Qi; Zuniga, Andy M.; McAfoos, Timothy; McAfoos, Timothy; Hamilton, Matthew M.; Marszalek, Joe R.; Mikule, Keith; Vancutsem, Paul; Wilcoxen, Keith; Tremblay, Martin; Jones, Philip; Lewis, Richard T. Share Save
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POMHEX, a cell-permeable enolase inhibitor for collateral lethality targeting of ENO1-deleted glioblastoma Lin, Y. H.; Satani, N.; Hammoudi, N.; Pisaneschi, F.; Leonard, P.; Maxwell, D.; Peng, Z.; Link, T.; Lee, G.; Sun, D.; Marszalek, J.; Sun, Y.; McMurray, J.; Mandal, P.; Di Francesco, M.; Czako, B.; Wang, A.; Bornmann, W.; DePinho, R.; Muller, F. Share Save