Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor
Zhang, Chao, Ibrahim, Prabha N., Zhang, Jiazhong, Burton, Elizabeth A., Habets, Gaston, Zhang, Ying, Powell, Ben, West, Brian L., Matusow, Bernice, Tsang, Garson, Shellooe, Rafe, Carias, Heidi, Nguyen, Hoa, Marimuthu, Adhirai, Zhang, Kam Y. J., Oh, Angela, Bremer, Ryan, Hurt, Clarence R., Artis, Dean R., Wu, Guoxian, Nespi, Marika, Spevak, Wayne, Lin, Paul, Nolop, Keith, Hirth, Peter, Tesch, Greg H., Bollag, Gideon
Published in Proceedings of the National Academy of Sciences - PNAS (02.04.2013)
Published in Proceedings of the National Academy of Sciences - PNAS (02.04.2013)
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Journal Article
The RUNX1/IL-34/CSF-1R axis is an autocrinally regulated modulator of resistance to BRAF-V600E inhibition in melanoma
Giricz, Orsi, Mo, Yongkai, Dahlman, Kimberly B, Cotto-Rios, Xiomaris M, Vardabasso, Chiara, Nguyen, Hoa, Matusow, Bernice, Bartenstein, Matthias, Polishchuk, Veronika, Johnson, Douglas B, Bhagat, Tushar D, Shellooe, Rafe, Burton, Elizabeth, Tsai, James, Zhang, Chao, Habets, Gaston, Greally, John M, Yu, Yiting, Kenny, Paraic A, Fields, Gregg B, Pradhan, Kith, Stanley, E Richard, Bernstein, Emily, Bollag, Gideon, Gavathiotis, Evripidis, West, Brian L, Sosman, Jeffrey A, Verma, Amit K
Published in JCI insight (26.07.2018)
Published in JCI insight (26.07.2018)
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Journal Article
RAF inhibitors that evade paradoxical MAPK pathway activation
Zhang, Chao, Spevak, Wayne, Zhang, Ying, Burton, Elizabeth A., Ma, Yan, Habets, Gaston, Zhang, Jiazhong, Lin, Jack, Ewing, Todd, Matusow, Bernice, Tsang, Garson, Marimuthu, Adhirai, Cho, Hanna, Wu, Guoxian, Wang, Weiru, Fong, Daniel, Nguyen, Hoa, Shi, Songyuan, Womack, Patrick, Nespi, Marika, Shellooe, Rafe, Carias, Heidi, Powell, Ben, Light, Emily, Sanftner, Laura, Walters, Jason, Tsai, James, West, Brian L., Visor, Gary, Rezaei, Hamid, Lin, Paul S., Nolop, Keith, Ibrahim, Prabha N., Hirth, Peter, Bollag, Gideon
Published in Nature (London) (22.10.2015)
Published in Nature (London) (22.10.2015)
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Journal Article
Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor
Tap, William D, Wainberg, Zev A, Anthony, Stephen P, Ibrahim, Prabha N, Zhang, Chao, Healey, John H, Chmielowski, Bartosz, Staddon, Arthur P, Cohn, Allen Lee, Shapiro, Geoffrey I, Keedy, Vicki L, Singh, Arun S, Puzanov, Igor, Kwak, Eunice L, Wagner, Andrew J, Von Hoff, Daniel D, Weiss, Glen J, Ramanathan, Ramesh K, Zhang, Jiazhong, Habets, Gaston, Zhang, Ying, Burton, Elizabeth A, Visor, Gary, Sanftner, Laura, Severson, Paul, Nguyen, Hoa, Kim, Marie J, Marimuthu, Adhirai, Tsang, Garson, Shellooe, Rafe, Gee, Carolyn, West, Brian L, Hirth, Peter, Nolop, Keith, van de Rijn, Matt, Hsu, Henry H, Peterfy, Charles, Lin, Paul S, Tong-Starksen, Sandra, Bollag, Gideon
Published in The New England journal of medicine (30.07.2015)
Published in The New England journal of medicine (30.07.2015)
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Journal Article
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF -mutant melanoma
Marimuthu, Adhirai, D'Andrea, Kurt, Lin, Paul S, Puzanov, Igor, Chapman, Paul B, Zhang, Jiazhong, Tsai, James, Ibrahim, Prabha N, Cho, Hanna, West, Brian L, Nathanson, Katherine L, Zhang, Kam Y. J, Zhang, Ying, Nolop, Keith, Schlessinger, Joseph, Grippo, Joseph, Shellooe, Rafe, Zhang, Chao, Flaherty, Keith T, Tsang, Garson, Powell, Ben, Kim, Kevin B, Wong, Bernice, Stumm, Michael, Ribas, Antoni, Spevak, Wayne, Higgins, Brian, Sosman, Jeffrey A, Artis, Dean R, Habets, Gaston, Hirth, Peter, Burton, Elizabeth A, Iyer, Raman, Su, Fei, Koehler, Astrid, Lee, Richard J, Bollag, Gideon, Nguyen, Hoa, McArthur, Grant A, Xu, Xiaowei
Published in Nature (London) (30.09.2010)
Published in Nature (London) (30.09.2010)
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Journal Article
BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor
Ozer, Hatice Gulcin, El-Gamal, Dalia, Powell, Ben, Hing, Zachary A, Blachly, James S, Harrington, Bonnie, Mitchell, Shaneice, Grieselhuber, Nicole R, Williams, Katie, Lai, Tzung-Huei, Alinari, Lapo, Baiocchi, Robert A, Brinton, Lindsey, Baskin, Elizabeth, Cannon, Matthew, Beaver, Larry, Goettl, Virginia M, Lucas, David M, Woyach, Jennifer A, Sampath, Deepa, Lehman, Amy M, Yu, Lianbo, Zhang, Jiazhong, Ma, Yan, Zhang, Ying, Spevak, Wayne, Shi, Songyuan, Severson, Paul, Shellooe, Rafe, Carias, Heidi, Tsang, Garson, Dong, Ken, Ewing, Todd, Marimuthu, Adhirai, Tantoy, Christina, Walters, Jason, Sanftner, Laura, Rezaei, Hamid, Nespi, Marika, Matusow, Bernice, Habets, Gaston, Ibrahim, Prabha, Zhang, Chao, Mathé, Ewy A, Bollag, Gideon, Byrd, John C, Lapalombella, Rosa
Published in Cancer discovery (01.04.2018)
Published in Cancer discovery (01.04.2018)
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Journal Article
Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397
Smith, Catherine C, Zhang, Chao, Lin, Kimberly C, Lasater, Elisabeth A, Zhang, Ying, Massi, Evan, Damon, Lauren E, Pendleton, Matthew, Bashir, Ali, Sebra, Robert, Perl, Alexander, Kasarskis, Andrew, Shellooe, Rafe, Tsang, Garson, Carias, Heidi, Powell, Ben, Burton, Elizabeth A, Matusow, Bernice, Zhang, Jiazhong, Spevak, Wayne, Ibrahim, Prabha N, Le, Mai H, Hsu, Henry H, Habets, Gaston, West, Brian L, Bollag, Gideon, Shah, Neil P
Published in Cancer discovery (01.06.2015)
Published in Cancer discovery (01.06.2015)
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Journal Article
Discovery of a Selective Inhibitor of Oncogenic B-Raf Kinase with Potent Antimelanoma Activity
Tsai, James, Lee, John T., Wang, Weiru, Zhang, Jiazhong, Cho, Hanna, Mamo, Shumeye, Bremer, Ryan, Gillette, Sam, Kong, Jun, Haass, Nikolas K., Sproesser, Katrin, Li, Ling, Smalley, Keiran S. M., Fong, Daniel, Zhu, Yong-Liang, Marimuthu, Adhirai, Nguyen, Hoa, Lam, Billy, Liu, Jennifer, Cheung, Ivana, Rice, Julie, Suzuki, Yoshihisa, Luu, Catherine, Settachatgul, Calvin, Shellooe, Rafe, Cantwell, John, Kim, Sung-Hou, Schlessinger, Joseph, Zhang, Kam Y. J., West, Brian L., Powell, Ben, Habets, Gaston, Zhang, Chao, Ibrahim, Prabha N., Hirth, Peter, Artis, Dean R., Herlyn, Meenhard, Bollag, Gideon
Published in Proceedings of the National Academy of Sciences - PNAS (26.02.2008)
Published in Proceedings of the National Academy of Sciences - PNAS (26.02.2008)
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Journal Article
Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial
Wagner, Andrew J, Severson, Paul L, Shields, Anthony F, Patnaik, Amita, Chugh, Rashmi, Tinoco, Gabriel, Wu, Guoxian, Nespi, Marika, Lin, Jack, Zhang, Ying, Ewing, Todd, Habets, Gaston, Burton, Elizabeth A, Matusow, Bernice, Tsai, James, Tsang, Garson, Shellooe, Rafe, Carias, Heidi, Chan, Katrina, Rezaei, Hamid, Sanftner, Laura, Marimuthu, Adhirai, Spevak, Wayne, Ibrahim, Prabha N, Inokuchi, Kerry, Alcantar, Oscar, Michelson, Glenn, Tsiatis, Athanasios C, Zhang, Chao, Bollag, Gideon, Trent, Jonathan C, Tap, William D
Published in JAMA oncology (01.09.2021)
Published in JAMA oncology (01.09.2021)
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Journal Article
Abstract 660: OPN-6602, a potent dual EP300/CBP bromodomain inhibitor, targets multiple myeloma through concomitant suppression of IRF4 and c-MYC
Matusow, Bernice, Spevak, Wayne, Zhang, Chao, Ma, Yan, Shellooe, Rafe, Tsai, James, Li, Pei Pei, Yu Chen, Pan, Habets, Gaston, Nichols, Christine, Singh, Parmveer, Inokuchi, Kerry, Walling, Jackie, Halladay, Jason, Bollag, Gideon
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Published in Cancer research (Chicago, Ill.) (22.03.2024)
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Journal Article
Abstract C085: OPN-6602, a dual EP300/CBP bromodomain inhibitor modulates androgen-driven transcription, including MYC, in mCRPC
Matusow, Bernice, Spevak, Wayne, Zhang, Chao, Ma, Yan, Shellooe, Rafe, Li, Peipei, Tsai, James, Yu Chen, Pan, Singh, Parmveer, Walling, Jackie, Nichols, Christine, Halladay, Jason, Inokuchi, Kerry, Habets, Gaston, Bollag, Gideon
Published in Molecular cancer therapeutics (01.12.2023)
Published in Molecular cancer therapeutics (01.12.2023)
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Journal Article
Abstract 2515: Aberrant expression of CSF1R in melanoma is driven through an endogenous viral promoter and it contributes to malignant growth and BRAF-inhibitor resistance
Giricz, Orsolya, Mo, Yongkai, Dahlman, Kimberly B., Cotto-Rios, Xiomaris M., Vardabasso, Chiara, Nguyen, Hoa, Matusow, Bernice, Bartenstein, Matthias, Polishchuck-Lee, Veronika, Johnson, Douglas B., Bhagat, Tushar B., Shellooe, Rafe, Burton, Elizabeth, Habets, Gaston, Greally, John M., Yu, Yiting, Bollag, Gideon, Kenny, Paraic A., Pradhan, Kith, Stanley, E. Richard, Bernstein, Emily, Gavathiotis, Evripidis, West, Brian L., Sosman, Jeffrey A., Verma, Amit
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Phase 1/2 precision medicine study of the next-generation BRAF inhibitor PLX8394
Janku, Filip, Vaishampayan, Ulka N., Khemka, Vivek, Bhatty, Minny, Sherman, Eric Jeffrey, Tao, Jessica, Whisenant, Jonathan R., Hong, David S., Bui, Nam, Kummar, Shivaani, Feun, Lynn G., Parikh, Aparna Raj, Zhang, Chao, Michelson, Glenn, Martin, Eric, Shellooe, Rafe, Severson, Paul, Pelayo, Michael, Karlin, David Alan, Sharma, Sunil
Published in Journal of clinical oncology (20.05.2018)
Published in Journal of clinical oncology (20.05.2018)
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Journal Article
Abstract 1224: A patient derived xenograft (PDX) platform for development of next generation KIT kinase inhibitors in imatinib-resistant gastrointestinal stromal tumors (GIST)
Mullins, Chelsea, Ricono, Jill, Carson, Patrick, Habets, Gaston, Shellooe, Rafe, Nguyen, Hoa, Broudy, Thomas, Mirsaidi, Cyrus, Nair, Praveen
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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Journal Article
Abstract 1885: Integrated epigenomic profiling reveals widespread demethylation in melanoma and points to the role of CSF1R-RUNX1 axis in resistance against BRAF inhibition
Giricz, Orsolya, Mo, Yongkai, Hu, Caroline H., Dahlman, Kimberly, Ramachandra, Nandini, Bartenstein, Matthias, Pradhan, Kith, Bhagat, Tushar, Yu, Yiting, Nguyen, Hoa, Burton, Elizabeth, Matusow, Bernice, Habets, Gaston, Shellooe, Rafe, Bollag, Gideon, West, Brian, Greally, John, Sosman, Jeffrey, Kenny, Paraic, Verma, Amit
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 3332: Aberrant expression of CSF1R in melanoma is driven through an endogenous viral promoter and it contributes to malignant growth and the acquisition of resistance against BRAF inhibition
Giricz, Orsolya, Mo, Yongkai, Hu, Caroline Y., Yu, Yiting, Pradhan, Kith, Bartenstein, Matthias, Ramachandra, Nandini, Polishchuck, Veronika, Dahlman, Kimberly B., Bhagat, Tushar, Nguyen, Hoa, Matusow, Bernice, Shellooe, Rafe, Burton, Elizabeth, Kenny, Paraic, Greally, John, Sosman, Jeffrey, Bollag, Gideon, West, Brian, Verma, Amit
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 PR06: Integrated epigenomic profiling reveals widespread demethylation in melanoma and reveals CSF-1 Receptor as an aberrant regulator of malignant growth and invasion
Giricz, Orsolya, Mo, Yongkai, Hu, Caroline, Dahlman, Kimberly, Bhattacharyya, Sanchari, Nguyen, Hoa, Matusow, Bernice, Bhagat, Tushar, Yu, Yiting, Shellooe, Rafe, Burton, Elizabeth, Habets, Gaston, Greally, John, Paraic, Kenny, Sosman, Jeffrey, Bollag, Gideon, West, Brian, Verma, Amit
Published in Cancer research (Chicago, Ill.) (15.07.2015)
Published in Cancer research (Chicago, Ill.) (15.07.2015)
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Journal Article
Abstract 4781: Integrated epigenomic profiling reveals widespread demethylation in melanoma and reveals CSF-1 receptor as an aberrant regulator of malignant growth and invasion
Mo, Yongkai, Giricz, Orsolya, Hu, Caroline H., Dahlman, Kimberly B., Bhattacharyya, Sanchari, Nguyen, Hoa, Matusow, Bernice, Bhagat, Tushar, Shellooe, Rafe, Burton, Elizabeth, Tsai, James, Zhang, Chao, Habets, Gaston, Shyr, Yu, Greally, John, Yu, Yiting, Bollag, Gideon E., Stanley, Richard, Trent, Jeffrey, Kenny, Paraic A., West, Brian L., Sosman, Jeffrey, Verma, Amit K.
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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Journal Article
Abstract A26: Integrated epigenomic profiling reveals widespread demethylation in melanoma, and reveals aberrant CSF-1 receptor expression as a regulator of malignant growth and invasion inhibited by PLX3397
Mo, Yongkai, Giricz, Orsolya, Hu, Caroline, Dahlman, Kimberly, Bhattacharyya, Sanchari, Nguyen, Hoa, Matusow, Bernice, Bhagat, Tushar, Yu, Yiting, Shellooe, Rafe, Burton, Elizabeth, Habets, Gaston, Greally, John, Kenny, Paraic, Sosman, Jeffrey, Bollag, Gideon, West, Brian L., Verma, Amit
Published in Cancer research (Chicago, Ill.) (01.02.2013)
Published in Cancer research (Chicago, Ill.) (01.02.2013)
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Journal Article
Abstract 553: Discovery of novel TRK/FMS dual inhibitors as therapeutic candidates for pancreatic cancer
Tsai, James, Zhang, Jiazhong, West, Brian L., Wong, Bernice, Burton, Betsy, Habets, Gaston, Marimuthu, Adhirai, Light, Emily, Powell, Ben, Shellooe, Rafe, Carias, Heidi, Shi, Songyuan, Spevak, Wayne, Nguyen, Hoa, Tsang, Garson, Zhang, Ying, Ewing, Todd, Zhang, Chao, Ibrahim, Prabha, Bollag, Gideon
Published in Cancer research (Chicago, Ill.) (15.04.2011)
Published in Cancer research (Chicago, Ill.) (15.04.2011)
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