The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models
Zhang, Sen, Anjum, Rana, Squillace, Rachel, Nadworny, Sara, Zhou, Tianjun, Keats, Jeff, Ning, Yaoyu, Wardwell, Scott D, Miller, David, Song, Youngchul, Eichinger, Lindsey, Moran, Lauren, Huang, Wei-Sheng, Liu, Shuangying, Zou, Dong, Wang, Yihan, Mohemmad, Qurish, Jang, Hyun Gyung, Ye, Emily, Narasimhan, Narayana, Wang, Frank, Miret, Juan, Zhu, Xiaotian, Clackson, Tim, Dalgarno, David, Shakespeare, William C, Rivera, Victor M
Published in Clinical cancer research (15.11.2016)
Published in Clinical cancer research (15.11.2016)
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Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK
Katayama, Ryohei, Khan, Tahsin M., Benes, Cyril, Lifshits, Eugene, Ebi, Hiromichi, Rivera, Victor M., Shakespeare, William C., Iafrate, A. John, Engelman, Jeffrey A., Shaw, Alice T., Vogt, Peter K.
Published in Proceedings of the National Academy of Sciences - PNAS (03.05.2011)
Published in Proceedings of the National Academy of Sciences - PNAS (03.05.2011)
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Journal Article
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase
Huang, Wei-Sheng, Liu, Shuangying, Zou, Dong, Thomas, Mathew, Wang, Yihan, Zhou, Tianjun, Romero, Jan, Kohlmann, Anna, Li, Feng, Qi, Jiwei, Cai, Lisi, Dwight, Timothy A, Xu, Yongjin, Xu, Rongsong, Dodd, Rory, Toms, Angela, Parillon, Lois, Lu, Xiaohui, Anjum, Rana, Zhang, Sen, Wang, Frank, Keats, Jeffrey, Wardwell, Scott D, Ning, Yaoyu, Xu, Qihong, Moran, Lauren E, Mohemmad, Qurish K, Jang, Hyun Gyung, Clackson, Tim, Narasimhan, Narayana I, Rivera, Victor M, Zhu, Xiaotian, Dalgarno, David, Shakespeare, William C
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Journal Article
Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance
Zhou, Tianjun, Commodore, Lois, Huang, Wei-Sheng, Wang, Yihan, Thomas, Mathew, Keats, Jeff, Xu, Qihong, Rivera, Victor M, Shakespeare, William C, Clackson, Tim, Dalgarno, David C, Zhu, Xiaotian
Published in Chemical biology & drug design (01.01.2011)
Published in Chemical biology & drug design (01.01.2011)
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Journal Article
Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies
Gozgit, Joseph M, Wong, Matthew J, Wardwell, Scott, Tyner, Jeffrey W, Loriaux, Marc M, Mohemmad, Qurish K, Narasimhan, Narayana I, Shakespeare, William C, Wang, Frank, Druker, Brian J, Clackson, Tim, Rivera, Victor M
Published in Molecular cancer therapeutics (01.06.2011)
Published in Molecular cancer therapeutics (01.06.2011)
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Journal Article
Crizotinib-Resistant Mutants of EML4-ALK Identified Through an Accelerated Mutagenesis Screen
Zhang, Sen, Wang, Frank, Keats, Jeffrey, Zhu, Xiaotian, Ning, Yaoyu, Wardwell, Scott D., Moran, Lauren, Mohemmad, Qurish K., Anjum, Rana, Wang, Yihan, Narasimhan, Narayana I., Dalgarno, David, Shakespeare, William C., Miret, Juan J., Clackson, Tim, Rivera, Victor M.
Published in Chemical biology & drug design (01.12.2011)
Published in Chemical biology & drug design (01.12.2011)
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Journal Article
Activity of Dual SRC-ABL Inhibitors Highlights the Role of BCR/ABL Kinase Dynamics in Drug Resistance
Azam, Mohammad, Nardi, Valentina, Shakespeare, William C., Metcalf, Chester A., Bohacek, Regine S., Wang, Yihan, Sundaramoorthi, Raji, Sliz, Piotr, Veach, Darren R., Bornmann, William G., Clarkson, Bayard, Dalgarno, David C., Sawyer, Tomi K., Daley, George Q.
Published in Proceedings of the National Academy of Sciences - PNAS (13.06.2006)
Published in Proceedings of the National Academy of Sciences - PNAS (13.06.2006)
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Journal Article
Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML
O'Hare, Thomas, Pollock, Roy, Stoffregen, Eric P., Keats, Jeffrey A., Abdullah, Omar M., Moseson, Erika M., Rivera, Victor M., Tang, Hao, Metcalf, Chester A., Bohacek, Regine S., Wang, Yihan, Sundaramoorthi, Raji, Shakespeare, William C., Dalgarno, David, Clackson, Tim, Sawyer, Tomi K., Deininger, Michael W., Druker, Brian J.
Published in Blood (15.10.2004)
Published in Blood (15.10.2004)
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Journal Article
Abstract 2644: AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models
Gonzalvez, Francois, Zhu, Xiaotian, Huang, Wei-Sheng, Baker, Theresa E., Ning, Yaoyu, Wardwell, Scott D., Nadworny, Sara, Zhang, Sen, Das, Biplab, Gong, Yongjin, Greenfield, Matthew T., Jang, Hyun G., Kohlmann, Anna, Li, Feng, Taslimi, Paul M., Tugnait, Meera, Xu, Yongjin, Ye, Emily Y., Youngsaye, Willmen W., Zech, Stephan G., Zhang, Yun, Zhou, Tianjun, Narasimhan, Narayana I., Dalgarno, David C., Shakespeare, William C., Rivera, Victor M.
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Journal Article
Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer
Gonzalvez, Francois, Vincent, Sylvie, Baker, Theresa E, Gould, Alexandra E, Li, Shuai, Wardwell, Scott D, Nadworny, Sara, Ning, Yaoyu, Zhang, Sen, Huang, Wei-Sheng, Hu, Yongbo, Li, Feng, Greenfield, Matthew T, Zech, Stephan G, Das, Biplab, Narasimhan, Narayana I, Clackson, Tim, Dalgarno, David, Shakespeare, William C, Fitzgerald, Michael, Chouitar, Johara, Griffin, Robert J, Liu, Shengwu, Wong, Kwok-Kin, Zhu, Xiaotian, Rivera, Victor M
Published in Cancer discovery (01.07.2021)
Published in Cancer discovery (01.07.2021)
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AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes
Summy, Justin M, Trevino, Jose G, Lesslie, Donald P, Baker, Cheryl H, Shakespeare, William C, Wang, Yihan, Sundaramoorthi, Raji, Metcalf, 3rd, Chester A, Keats, Jeffrey A, Sawyer, Tomi K, Gallick, Gary E
Published in Molecular cancer therapeutics (01.12.2005)
Published in Molecular cancer therapeutics (01.12.2005)
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Journal Article
Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models
Gozgit, Joseph M, Wong, Matthew J, Moran, Lauren, Wardwell, Scott, Mohemmad, Qurish K, Narasimhan, Narayana I, Shakespeare, William C, Wang, Frank, Clackson, Tim, Rivera, Victor M
Published in Molecular cancer therapeutics (01.03.2012)
Published in Molecular cancer therapeutics (01.03.2012)
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Journal Article
Src Inhibitors in Metastatic Bone Disease
Boyce, Brendan F, Xing, Lianping, Yao, Zhenqiang, Yamashita, Teruhito, Shakespeare, William C, Wang, Yihan, Metcalf, 3rd, Chester A, Sundaramoorthi, Raji, Dalgarno, David C, Iuliucci, John D, Sawyer, Tomi K
Published in Clinical cancer research (15.10.2006)
Published in Clinical cancer research (15.10.2006)
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Journal Article
Conference Proceeding
AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance
O'Hare, Thomas, Shakespeare, William C., Zhu, Xiaotian, Eide, Christopher A., Rivera, Victor M., Wang, Frank, Adrian, Lauren T., Zhou, Tianjun, Huang, Wei-Sheng, Xu, Qihong, Metcalf, Chester A., Tyner, Jeffrey W., Loriaux, Marc M., Corbin, Amie S., Wardwell, Scott, Ning, Yaoyu, Keats, Jeffrey A., Wang, Yihan, Sundaramoorthi, Raji, Thomas, Mathew, Zhou, Dong, Snodgrass, Joseph, Commodore, Lois, Sawyer, Tomi K., Dalgarno, David C., Deininger, Michael W.N., Druker, Brian J., Clackson, Tim
Published in Cancer cell (06.11.2009)
Published in Cancer cell (06.11.2009)
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Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant
Huang, Wei-Sheng, Metcalf, Chester A, Sundaramoorthi, Raji, Wang, Yihan, Zou, Dong, Thomas, R. Mathew, Zhu, Xiaotian, Cai, Lisi, Wen, David, Liu, Shuangying, Romero, Jan, Qi, Jiwei, Chen, Ingrid, Banda, Geetha, Lentini, Scott P, Das, Sasmita, Xu, Qihong, Keats, Jeff, Wang, Frank, Wardwell, Scott, Ning, Yaoyu, Snodgrass, Joseph T, Broudy, Marc I, Russian, Karin, Zhou, Tianjun, Commodore, Lois, Narasimhan, Narayana I, Mohemmad, Qurish K, Iuliucci, John, Rivera, Victor M, Dalgarno, David C, Sawyer, Tomi K, Clackson, Tim, Shakespeare, William C
Published in Journal of medicinal chemistry (24.06.2010)
Published in Journal of medicinal chemistry (24.06.2010)
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Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non–small cell lung cancer
Huang, Wei-Sheng, Li, Feng, Gong, Yongjin, Zhang, Yun, Youngsaye, Willmen, Xu, Yongjin, Zhu, Xiaotian, Greenfield, Matthew T., Kohlmann, Anna, Taslimi, Paul M., Toms, Angela, Zech, Stephan G., Zhou, Tianjun, Das, Biplab, Jang, Hyun G., Tugnait, Meera, Ye, Yihua E., Gonzalvez, Francois, Baker, Theresa E., Nadworny, Sara, Ning, Yaoyu, Wardwell, Scott D., Zhang, Sen, Gould, Alexandra E., Hu, Yongbo, Lane, Weston, Skene, Robert J., Zou, Hua, Clackson, Tim, Narasimhan, Narayana I., Rivera, Victor M., Dalgarno, David C., Shakespeare, William C.
Published in Bioorganic & medicinal chemistry letters (15.01.2023)
Published in Bioorganic & medicinal chemistry letters (15.01.2023)
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Journal Article
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery
Zech, Stephan G, Kohlmann, Anna, Zhou, Tianjun, Li, Feng, Squillace, Rachel M, Parillon, Lois E, Greenfield, Matthew T, Miller, David P, Qi, Jiwei, Thomas, R. Mathew, Wang, Yihan, Xu, Yongjin, Miret, Juan J, Shakespeare, William C, Zhu, Xiaotian, Dalgarno, David C
Published in Journal of medicinal chemistry (28.01.2016)
Published in Journal of medicinal chemistry (28.01.2016)
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Journal Article
De novo design and synthesis of somatostatin non-peptide peptidomimetics utilizing .beta.-D-glucose as a novel scaffolding
Hirschmann, Ralph, Nicolaou, K. C, Pietranico, Sherrie, Leahy, Ellen M, Salvino, Joseph, Arison, Byron, Cichy, Maria A, Spoors, P. Grant, Shakespeare, William C
Published in Journal of the American Chemical Society (01.12.1993)
Published in Journal of the American Chemical Society (01.12.1993)
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Journal Article
Bone-Targeted 2,6,9-Trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases
Wang, Yihan, Metcalf, Chester A., Shakespeare, William C., Sundaramoorthi, Raji, Keenan, Terence P., Bohacek, Regine S., van Schravendijk, Marie Rose, Violette, Shiela M., Narula, Surinder S., Dalgarno, David C., Haraldson, Chad, Keats, Jeffrey, Liou, Shuenn, Mani, Ukti, Pradeepan, Selvi, Ram, Mary, Adams, Susan, Weigele, Manfred, Sawyer, Tomi K.
Published in Bioorganic & medicinal chemistry letters (15.09.2003)
Published in Bioorganic & medicinal chemistry letters (15.09.2003)
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Modulation of Receptor and Receptor Subtype Affinities Using Diastereomeric and Enantiomeric Monosaccharide Scaffolds as a Means to Structural and Biological Diversity. A New Route to Ether Synthesis
Hirschmann, Ralph, Hynes, John, Cichy-Knight, Maria A, van Rijn, Rachel D, Sprengeler, Paul A, Spoors, P. Grant, Shakespeare, William C, Pietranico-Cole, Sherrie, Barbosa, Joseph, Liu, Josephine, Yao, Wenqing, Rohrer, Susan, Smith, Amos B
Published in Journal of medicinal chemistry (23.04.1998)
Published in Journal of medicinal chemistry (23.04.1998)
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