H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers
Seiler, Michael, Yoshimi, Akihide, Darman, Rachel, Chan, Betty, Keaney, Gregg, Thomas, Michael, Agrawal, Anant A, Caleb, Benjamin, Csibi, Alfredo, Sean, Eckley, Fekkes, Peter, Karr, Craig, Klimek, Virginia, Lai, George, Lee, Linda, Kumar, Pavan, Lee, Stanley Chun-Wei, Liu, Xiang, Mackenzie, Crystal, Meeske, Carol, Mizui, Yoshiharu, Padron, Eric, Park, Eunice, Pazolli, Ermira, Peng, Shouyong, Prajapati, Sudeep, Taylor, Justin, Teng, Teng, Wang, John, Warmuth, Markus, Yao, Huilan, Yu, Lihua, Zhu, Ping, Abdel-Wahab, Omar, Smith, Peter G, Buonamici, Silvia
Published in Nature medicine (01.04.2018)
Published in Nature medicine (01.04.2018)
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Journal Article
The cryo-EM structure of the SF3b spliceosome complex bound to a splicing modulator reveals a pre-mRNA substrate competitive mechanism of action
Finci, Lorenzo I, Zhang, Xiaofeng, Huang, Xiuliang, Zhou, Qiang, Tsai, Jennifer, Teng, Teng, Agrawal, Anant, Chan, Betty, Irwin, Sean, Karr, Craig, Cook, Andrew, Zhu, Ping, Reynolds, Dominic, Smith, Peter G, Fekkes, Peter, Buonamici, Silvia, Larsen, Nicholas A
Published in Genes & development (01.02.2018)
Published in Genes & development (01.02.2018)
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Journal Article
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma
Joshi, Jaya Julie, Coffey, Heather, Corcoran, Erik, Tsai, Jennifer, Huang, Chia-Ling, Ichikawa, Kana, Prajapati, Sudeep, Hao, Ming-Hong, Bailey, Suzanna, Wu, Jeremy, Rimkunas, Victoria, Karr, Craig, Subramanian, Vanitha, Kumar, Pavan, MacKenzie, Crystal, Hurley, Raelene, Satoh, Takashi, Yu, Kun, Park, Eunice, Rioux, Nathalie, Kim, Amy, Lai, Weidong G, Yu, Lihua, Zhu, Ping, Buonamici, Silvia, Larsen, Nicholas, Fekkes, Peter, Wang, John, Warmuth, Markus, Reynolds, Dominic J, Smith, Peter G, Selvaraj, Anand
Published in Cancer research (Chicago, Ill.) (15.12.2017)
Published in Cancer research (Chicago, Ill.) (15.12.2017)
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Journal Article
Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators
Aird, Daniel, Teng, Teng, Huang, Chia-Ling, Pazolli, Ermira, Banka, Deepti, Cheung-Ong, Kahlin, Eifert, Cheryl, Furman, Craig, Wu, Zhenhua Jeremy, Seiler, Michael, Buonamici, Silvia, Fekkes, Peter, Karr, Craig, Palacino, James, Park, Eunice, Smith, Peter G, Yu, Lihua, Mizui, Yoshiharu, Warmuth, Markus, Chicas, Agustin, Corson, Laura, Zhu, Ping
Published in Nature communications (11.01.2019)
Published in Nature communications (11.01.2019)
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Journal Article
Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A-SF3b complex
Teng, Teng, Tsai, Jennifer Hc, Puyang, Xiaoling, Seiler, Michael, Peng, Shouyong, Prajapati, Sudeep, Aird, Daniel, Buonamici, Silvia, Caleb, Benjamin, Chan, Betty, Corson, Laura, Feala, Jacob, Fekkes, Peter, Gerard, Baudouin, Karr, Craig, Korpal, Manav, Liu, Xiang, T Lowe, Jason, Mizui, Yoshiharu, Palacino, James, Park, Eunice, Smith, Peter G, Subramanian, Vanitha, Wu, Zhenhua Jeremy, Zou, Jian, Yu, Lihua, Chicas, Agustin, Warmuth, Markus, Larsen, Nicholas, Zhu, Ping
Published in Nature communications (25.05.2017)
Published in Nature communications (25.05.2017)
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Journal Article
The Giardia intestinalis filamentous cyst wall contains a novel β(1-3)-N-acetyl-d-galactosamine polymer: a structural and conformational study
Gerwig, Gerrit J., van Kuik, J. Albert, Leeflang, Bas R., Kamerling, Johannis P., Vliegenthart, Johannes F.G., Karr, Craig D., Jarroll, Edward L.
Published in Glycobiology (Oxford) (01.08.2002)
Published in Glycobiology (Oxford) (01.08.2002)
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Journal Article
Regulation of Carbohydrate Metabolism During Giardia Encystment
JARROLL, EDWARD L., MACECHKO, P. TIMOTHY, STEIMLE, PAUL A., BULIK, DOROTA, KARR, CRAIG D., van KEULEN, HARRY, PAGET, TIMOTHY A., GERWIG, GERRIT, KAMERLING, JOHANNES, VLIEGENTHART, JOHANNES, ERLANDSEN, STANLEY
Published in The Journal of eukaryotic microbiology (01.01.2001)
Published in The Journal of eukaryotic microbiology (01.01.2001)
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Conference Proceeding
Biochemical and structural basis for the pharmacological inhibition of nuclear hormone receptor PPARγ by inverse agonists
Irwin, Sean, Karr, Craig, Furman, Craig, Tsai, Jennifer, Gee, Patricia, Banka, Deepti, Wibowo, Ardian S., Dementiev, Alexey A., O’Shea, Morgan, Yang, Joyce, Lowe, Jason, Mitchell, Lorna, Ruppel, Sabine, Fekkes, Peter, Zhu, Ping, Korpal, Manav, Larsen, Nicholas A.
Published in The Journal of biological chemistry (01.11.2022)
Published in The Journal of biological chemistry (01.11.2022)
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Journal Article
Abstract 281: Sensitivity to splicing modulation of BCL2 family genes reveals cancer therapeutic strategies for splicing modulators
Aird, Daniel, Teng, Teng, Huang, Chia-Ling, Pazolli, Ermira, Banka, Deepti, Cheung-Ong, Kahlin, Eifert, Cheryl, Furman, Craig, Wu, Jeremy, Seiler, Michael, Buonamici, Silvia, Fekkes, Peter, Karr, Craig, Palacino, James, Park, Eunice, Smith, Peter, Yu, Lihua, Mizui, Yoshiharu, Warmuth, Markus, Chicas, Agustin, Corson, Laura, Zhu, Ping
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3
Brawn, Ryan A., Cook, Andrew, Omoto, Kiyoyuki, Ke, Jiyuan, Karr, Craig, Colombo, Federico, Virrankoski, Milena, Prajapati, Sudeep, Reynolds, Dominic, Bolduc, David M., Tuong-Vi Nguyen, Gee, Patricia, Borrelli, Deanna, Caleb, Benjamin, Yao, Shihua, Irwin, Sean, Larsen, Nicholas A., Selvaraj, Anand, Zhao, Xuesong, Ioannidis, Stephanos
Published in ACS medicinal chemistry letters (14.01.2021)
Published in ACS medicinal chemistry letters (14.01.2021)
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Journal Article
Combined inhibition of FGFR4 and VEGFR signaling enhances efficacy in FGF19 driven hepatocellular carcinoma
Zhao, Xuesong, Joshi, Jaya Julie, Aird, Daniel, Karr, Craig, Yu, Kun, Huang, Chialing, Colombo, Federico, Virrankoski, Milena, Prajapati, Sudeep, Selvaraj, Anand
Published in American journal of cancer research (01.01.2022)
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Published in American journal of cancer research (01.01.2022)
Journal Article
Abstract 3013: Identification of PHF5A as a common cellular target of splicing-modulating chemical probes
Teng, Teng, Puyang, Xiaoling, Peng, Shouyong, Feala, Jacob, Chan, Betty, Tsai, Jennifer, Caleb, Benjamin, Karr, Craig, Park, Eunice, Corson, Laura, Mizui, Yoshiharu, Smith, Peter, Larsen, Nicholas, Yu, Lihua, Warmuth, Markus, Zhu, Ping, Chicas, Agustin
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 3126: H3B6527, a selective and potent FGFR4 inhibitor for FGF19-driven hepatocellular carcinoma
Selvaraj, Anand, Corcoran, Erik, Coffey, Heather, Prajapati, Sudeep, Hao, Ming-Hong, Larsen, Nicholas, Tsai, Jennifer, Satoh, Takashi, Ichikawa, Kana, Joshi, Julie Jaya, Hurley, Raelene, Wu, Jeremy, Huang, Chia-Ling, Bailey, Suzanna, Karr, Craig, Kumar, Pavan, Rimkunas, Victoria, Mackenzie, Crystal, Rioux, Nathalie, Kim, Amy, Akare, Sandeep, Lai, George, Yu, Lihua, Fekkes, Peter, Wang, John, Warmuth, Markus, Smith, Peter, Reynolds, Dominic
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 126: A chemogenomic approach reveals the action of splicing modulators at the branch point adenosine binding pocket defined by the PHF5A/SF3b complex
Teng, Teng, Tsai, Jennifer, Puyang, Xiaoling, Seiler, Michael, Peng, Shouyong, Aird, Daniel, Buonamici, Silvia, Caleb, Benjamin, Chan, Betty, Corson, Laura, Feala, Jacob, Fekkes, Peter, Karr, Craig, Korpal, Manav, Mizui, Yoshiharu, Park, Eunice, Palacino, James, Smith, Peter, Subramanian, Vanitha, Wu, Jeremy, Yu, Lihua, Chicas, Agustin, Warmuth, Markus, Larsen, Nicholas, Zhu, Ping
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Regulation of Carbohydrate Metabolism During Giardia Encystment1
JARROLL, EDWARD L, MACECHKO, P. TIMOTHY, STEIMLE, PAUL A, BULIK, DOROTA, KARR, CRAIG D, KEULEN, HARRY van, PAGET, TIMOTHY A, GERWIG, GERRIT, KAMERLING, JOHANNES, VLIEGENTHART, JOHANNES, ERLANDSEN, STANLEY
Published in The Journal of eukaryotic microbiology (01.01.2001)
Published in The Journal of eukaryotic microbiology (01.01.2001)
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Journal Article
H3B-8800, an Orally Bioavailable Modulator of the SF3b Complex, Shows Efficacy in Spliceosome-Mutant Myeloid Malignancies
Buonamici, Silvia, Yoshimi, Akihide, Thomas, Michael, Seiler, Michael, Chan, Betty, Caleb, Benjamin, Darman, Rachel, Fekkes, Peter, Karr, Craig, Keaney, Gregg F., Klimek, Virginia M., Kunii, Kaiko, Lee, Linda, Lee, Stanley Chun-Wei, Liu, Xiang, Meeske, Carol, Mizui, Yoshiharu, Padron, Eric, Park, Eunice, Pazolli, Ermira, Prajapati, Sudeep, Taylor, Justin, Wang, John, Warmuth, Markus, Yu, Lihua, Zhu, Ping, Abdel-Wahab, Omar, Smith, Peter G
Published in Blood (02.12.2016)
Published in Blood (02.12.2016)
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Journal Article
Abstract 1185: H3B-8800, a novel orally available SF3b modulator, shows preclinical efficacy across spliceosome mutant cancers
Buonamici, Silvia, Yoshimi, Akihide, Thomas, Michael, Seiler, Michael, Chan, Betty, Caleb, Benjamin, Csibi, Fred, Darman, Rachel, Fekkes, Peter, Karr, Craig, Keaney, Gregg, Kim, Amy, Klimek, Virginia, Kumar, Pavan, Kunii, Kaiko, Lee, Stanley Chun-Wei, Liu, Xiang, MacKenzie, Crystal, Meeske, Carol, Mizui, Yoshiharu, Padron, Eric, Park, Eunice, Pazolli, Ermira, Prajapati, Sudeep, Rioux, Nathalie, Taylor, Justin, Wang, John, Warmuth, Markus, Yao, Huilan, Yu, Lihua, Zhu, Ping, Abdel-Wahab, Omar, Smith, Peter
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 DDT01-04: Discovery and development of H3B-6545: A novel, oral, selective estrogen receptor covalent antagonist (SERCA) for the treatment of breast cancer
Smith, Peter G., Puyang, Xiaoling, Furman, Craig, Zheng, Guo Zhu, Banka, Deepti, Thomas, Michael, Subramanian, Vanitha, Irwin, Sean, Larsen, Nicholas, Caleb, Benjamin, Karr, Craig, Wu, Jeremy, O’Shea, Morgan, Yang, Joyce, Davis, Allison, Kim, Amy, Rioux, Nathalie, Rimkunas, Victoria, Yao, Huilan, MacKenzie, Crystal, Kumar, Pavan, Smith, Sherri, Eckley, Sean, Hart, Andrew, Lai, George, Rowbottom, Christopher, Fekkes, Peter, Buonamici, Silvia, Reynolds, Dominic, Yu, Lihua, Sahmoud, Tarek, Warmuth, Markus, Mitchell, Lorna, Zhu, Ping, Korpal, Manav
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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