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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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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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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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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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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Conference Proceeding
Structure-Based Design of an Osteoclast-Selective, Nonpeptide Src Homology 2 Inhibitor with in vivo Antiresorptive Activity
Shakespeare, William, Yang, Michael, Bohacek, Regine, Cerasoli, Franklin, Stebbins, Karin, Sundaramoorthi, Raji, Azimioara, Mihai, Vu, Chi, Pradeepan, Selvi, Metcalf, Chester, Haraldson, Chad, Merry, Taylor, Dalgarno, David, Narula, Surinder, Hatada, Marcos, Lu, Xiaode, van Schravendijk, Marie Rose, Adams, Susan, Violette, Shelia, Smith, Jeremy, Guan, Wei, Bartlett, Catherine, Herson, Jay, Iuliucci, John, Weigele, Manfred, Sawyer, Tomi
Published in Proceedings of the National Academy of Sciences - PNAS (15.08.2000)
Published in Proceedings of the National Academy of Sciences - PNAS (15.08.2000)
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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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SRC homology-2 inhibitors: peptidomimetic and nonpeptide
Sawyer, Tomi K, Bohacek, Regine S, Dalgarno, David C, Eyermann, Charles J, Kawahata, Noriyuki, Metcalf, 3rd, Chester A, Shakespeare, William C, Sundaramoorthi, Raji, Wang, Yihan, Yang, Michael G
Published in Mini reviews in medicinal chemistry (01.10.2002)
Published in Mini reviews in medicinal chemistry (01.10.2002)
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Novel Protein Kinase Inhibitors: SMART Drug Design Technology
Sawyer, Tomi K, Bohacek, Regine S, III, Chester A. Metcalf, Shakespeare, William C, Wang, Yihan, Sundaramoorthi, Raji, Keenan, Terence, Narula, Surinder, Weigele, Manfred, Dalgarno, David C
Published in BioTechniques (01.06.2003)
Published in BioTechniques (01.06.2003)
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Selective Inhibition of Src SH2 by a Novel Thiol-Targeting Tricarbonyl-Modified Inhibitor and Mechanistic Analysis by 1H/ 13C NMR Spectroscopy
Sundaramoorthi, Raji, Siedem, Chris, Vu, Chi B, Dalgarno, David C, Laird, Ellen C, Botfield, Martyn C, Combs, Amanda B, Adams, Susan E, Yuan, Ruth W, Weigele, Manfred, Narula, Surinder S
Published in Bioorganic & medicinal chemistry letters (01.07.2001)
Published in Bioorganic & medicinal chemistry letters (01.07.2001)
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9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation
Huang, Wei-Sheng, Zhu, Xiaotian, Wang, Yihan, Azam, Mohammad, Wen, David, Sundaramoorthi, Raji, Thomas, R. Mathew, Liu, Shuangying, 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, Daley, George Q, Iuliucci, John, Dalgarno, David C, Clackson, Tim, Sawyer, Tomi K, Shakespeare, William C
Published in Journal of medicinal chemistry (13.08.2009)
Published in Journal of medicinal chemistry (13.08.2009)
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Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR–ABL including the T315I gatekeeper mutant
Thomas, Mathew, Huang, Wei-Sheng, Wen, David, Zhu, Xiaotian, Wang, Yihan, Metcalf, Chester A., Liu, Shuangying, Chen, Ingrid, Romero, Jan, Zou, Dong, Sundaramoorthi, Raji, Li, Feng, Qi, Jiwei, Cai, Lisi, Zhou, Tianjun, Commodore, Lois, Xu, Qihong, Keats, Jeff, Wang, Frank, Wardwell, Scott, Ning, Yaoyu, Snodgrass, Joseph T., Broudy, Marc I., Russian, Karin, Iuliucci, John, Rivera, Victor M., Sawyer, Tomi K., Dalgarno, David C., Clackson, Tim, Shakespeare, William C.
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Structural Basis of Src Tyrosine Kinase Inhibition with a New Class of Potent and Selective Trisubstituted Purine-based Compounds
Dalgarno, David, Stehle, Thilo, Narula, Surinder, Schelling, Pierre, Rose van Schravendijk, Marie, Adams, Susan, Andrade, Lawrence, Keats, Jeff, Ram, Mary, Jin, Lei, Grossman, Trudy, MacNeil, Ian, Metcalf III, Chester, Shakespeare, William, Wang, Yihan, Keenan, Terry, Sundaramoorthi, Raji, Bohacek, Regine, Weigele, Manfred, Sawyer, Tomi
Published in Chemical biology & drug design (01.01.2006)
Published in Chemical biology & drug design (01.01.2006)
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Abstract 2671: Structural analysis of the inhibitory mechanism of AP24534, a pan-BCR-ABL inhibitor overriding the T315I gatekeeper mutation
Zhu, Xiaotian, Zhou, Tianjun, Shakespeare, William C., Huang, Wei-Sheng, Commodore, Lois, Metcalf, Chester A., Wang, Yihan, Thomas, Mathew, Sundaramoorthi, Raji, Zou, Dong, Sawyer, Tomi K., Clackson, Tim, Dalgarno, David C.
Published in Cancer research (Chicago, Ill.) (15.04.2010)
Published in Cancer research (Chicago, Ill.) (15.04.2010)
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In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit
Corbin, Amie S., Demehri, Shadmehr, Griswold, Ian J., Wang, Yihan, Metcalf, Chester A., Sundaramoorthi, Raji, Shakespeare, William C., Snodgrass, Joseph, Wardwell, Scott, Dalgarno, David, Iuliucci, John, Sawyer, Tomi K., Heinrich, Michael C., Druker, Brian J., Deininger, Michael W.N.
Published in Blood (01.07.2005)
Published in Blood (01.07.2005)
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Facile synthesis of 9-(arenethenyl)purines via Heck reaction of 9-vinylpurines and aryl halides
Huang, Wei-Sheng, Wang, Yihan, Sundaramoorthi, Raji, Thomas, R. Mathew, Wen, David, Liu, Shuangying, Lentini, Scott P., Das, Sasmita, Banda, Geetha, Sawyer, Tomi K., Shakespeare, William C.
Published in Tetrahedron letters (08.10.2007)
Published in Tetrahedron letters (08.10.2007)
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Future Anti-Catabolic Therapeutic Targets in Bone Disease
BOYCE, BRENDAN F., XING, LIANPING, YAO, ZHENQIANG, SHAKESPEARE, WILLIAM C., WANG, YIHAN, METCALF III, CHESTER A., SUNDARAMOORTHI, RAJI, DALGARNO, DAVID C., IULIUCCI, JOHN D., SAWYER, TOMI K.
Published in Annals of the New York Academy of Sciences (01.04.2006)
Published in Annals of the New York Academy of Sciences (01.04.2006)
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Journal Article
Novel N super(9)-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors
Wang, Yihan, Shakespeare, William C, Huang, Wei-Sheng, Sundaramoorthi, Raji, Lentini, Scott, Das, Sasmita, Liu, Shuangying, Banda, Geeta, Wen, David, Zhu, Xiaotian, Xu, Qihong, Keats, Jeffrey, Wang, Frank, Wardwell, Scott, Ning, Yaoyu, Snodgrass, Joseph T, Broudy, Mark I, Russian, Karin, Dalgarno, David, Clackson, Tim, Sawyer, Tomi K
Published in Bioorganic & medicinal chemistry (01.09.2008)
Published in Bioorganic & medicinal chemistry (01.09.2008)
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