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, Zhan, Yanai, Zhao, Shuping, Barton, Michelle C, Draetta, Giulio, Toniatti, Carlo, Jones, Philip, Geck Do, Mary, Andersen, Jannik N
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Journal Article
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
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Design, Synthesis, and Biological Evaluation of Sulfonyl Acrylonitriles as Novel Inhibitors of Cancer Metastasis and Spread
Shen, Yi, Zificsak, Craig A, Shea, Jill E, Lao, Xuegang, Bollt, Oana, Li, Xiufen, Lisko, Joseph G, Theroff, Jay P, Scaife, Courtney L, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D, Kuwada, Scott K
Published in Journal of medicinal chemistry (12.02.2015)
Published in Journal of medicinal chemistry (12.02.2015)
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Journal Article
Synthesis and structure–activity relationships of 1,2,3,4-tetrahydropyrido[2,3- b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase
Milkiewicz, Karen L., Weinberg, Linda R., Albom, Mark S., Angeles, Thelma S., Cheng, Mangeng, Ghose, Arup K., Roemmele, Renee C., Theroff, Jay P., Underiner, Ted L., Zificsak, Craig A., Dorsey, Bruce D.
Published in Bioorganic & medicinal chemistry (15.06.2010)
Published in Bioorganic & medicinal chemistry (15.06.2010)
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Journal Article
Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors
Zificsak, Craig A, Theroff, Jay P, Aimone, Lisa D, Angeles, Thelma S, Albom, Mark S, Cheng, Mangeng, Mesaros, Eugen F, Ott, Gregory R, Quail, Matthew R, Underiner, Ted L, Wan, Weihua, Dorsey, Bruce D
Published in Bioorganic & medicinal chemistry letters (01.07.2011)
Published in Bioorganic & medicinal chemistry letters (01.07.2011)
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Journal Article
Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors
Weinberg, Linda R., Albom, Mark S., Angeles, Thelma S., Husten, Jean, Lisko, Joseph G., McHugh, Robert J., Milkiewicz, Karen L., Murthy, Seetha, Ott, Gregory R., Theroff, Jay P., Tripathy, Rabindranath, Underiner, Ted L., Zificsak, Craig A., Dorsey, Bruce D.
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
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Journal Article
Synthesis and biological evaluation of sulfonyl acrylonitriles as novel inhibitors to peritoneal carcinomatosis
Zificsak, Craig A., Shen, Yi, Lisko, Joseph G., Theroff, Jay P., Lao, Xuegang, Bollt, Oana, Li, Xiufen, Dorsey, Bruce D., Kuwada, Scott K.
Published in Bioorganic & medicinal chemistry letters (01.03.2012)
Published in Bioorganic & medicinal chemistry letters (01.03.2012)
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Journal Article
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases
Zificsak, Craig A., Gingrich, Diane E., Breslin, Henry J., Dunn, Derek D., Milkiewicz, Karen L., Theroff, Jay P., Thieu, Tho V., Underiner, Ted L., Weinberg, Linda R., Aimone, Lisa D., Albom, Mark S., Mason, Jennifer L., Saville, Lisa, Husten, Jean, Angeles, Thelma S., Finn, James P., Jan, Mahfuza, O’Kane, Teresa M., Dobrzanski, Pawel, Dorsey, Bruce D.
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
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Journal Article
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines
Zificsak, Craig A., Theroff, Jay P., Aimone, Lisa D., Albom, Mark S., Angeles, Thelma S., Brown, Rebecca A., Galinis, Deborah, Grobelny, Jennifer V., Herbertz, Torsten, Husten, Jean, Kocsis, Laura S., LoSardo, Christine, Miknyoczki, Sheila J., Murthy, Seetha, Rolon-Steele, Damaris, Underiner, Ted L., Wells-Knecht, Kevin J., Worrell, Candace S., Zeigler, Kelli S., Dorsey, Bruce D.
Published in Bioorganic & medicinal chemistry letters (15.01.2011)
Published in Bioorganic & medicinal chemistry letters (15.01.2011)
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Journal Article
Structure–activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors
Varnes, Jeffrey G., Wacker, Dean A., Pinto, Donald J.P., Orwat, Michael J., Theroff, Jay P., Wells, Brian, Galemo, Robert A., Luettgen, Joseph M., Knabb, Robert M., Bai, Steven, He, Kan, Lam, Patrick Y.S., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry (15.01.2008)
Published in Bioorganic & medicinal chemistry (15.01.2008)
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Journal Article
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
Published in Nature medicine (01.07.2018)
Published in Nature medicine (01.07.2018)
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Journal Article
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
Published in Journal of medicinal chemistry (12.11.2020)
Published in Journal of medicinal chemistry (12.11.2020)
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Journal Article
Abstract 1655: 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
Francesco, Maria Emilia Di, 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
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Abstract PR01: IACS-010759 a novel inhibitor of oxidative phosphorylation advancing into first-in-human studies to exploit metabolic vulnerabilities
Jones, Philip, Francesco, M Emilia Di, Molina, Jennifer M., Protopopova, Marina, Bandi, Madhavi, Bardenhagen, Jennifer, Bristow, Christopher A., Carroll, Christopher L., Feng, Ningping, Gay, Jason P., Do, Mary K. Geck, Greer, Jennifer M., Konopleva, Marina, Kang, Zhijun, Liu, Gang, McAfoos, Timothy, Morlacchi, Pietro, Smith, Melinda G., Fnu, Sonal, Theroff, Jay P., Draetta, Giulio, Toniatti, Carlo, Marszalek, Joseph R.
Published in Clinical cancer research (01.01.2017)
Published in Clinical cancer research (01.01.2017)
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Journal Article
Abstract 4971: 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, Francesco, M. Emilia Di, Marszalek, Joseph R.
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Abstract 335: 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, Geck Do, Mary, 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.
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Journal Article
Abstract 4455: 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, Geck Do, Mary, 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.
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Journal Article
Abstract 4380: 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, Geck Do, Mary, 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.
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Journal Article
Abstract LB-A15: IACS-010759 is a novel inhibitor of oxidative phosphorylation that selectively targets AML cells by inducing a metabolic catastrophe
Molina, Jennifer R., Protopopova, Marina, Bandi, Madhavi, Bardenhagen, Jennifer, Bristow, Christopher, Alimova, Maria, Carroll, Christopher, Chang, Edward, Feng, Ningping, Gay, Jason, Geck Do, Mary, Greer, Jennifer, Huang, Sha, Jiang, Yongying, Konopleva, Marina, Matre, Polina, Kang, Zhijun, Liu, Gang, McAfoos, Timothy, Morlacchi, Pietro, Smith, Melinda, Sonal, Sonal, Theroff, Jay, Xu, Quanyun, Draetta, Giulio, Jones, Philip, Toniatti, Carlo, Di Francesco, M. Emilia, Marszalek, Joseph R.
Published in Molecular cancer therapeutics (01.12.2015)
Published in Molecular cancer therapeutics (01.12.2015)
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Journal Article
Abstract A65: 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, Francesco, M. Emilia Di, Marszalek, Joseph R.
Published in Molecular cancer research (01.01.2016)
Published in Molecular cancer research (01.01.2016)
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