Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors von McTigue, Michele, Murray, Brion William, Chen, Jeffrey H, Deng, Ya-Li, Solowiej, James, Kania, Robert S

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Multiple Mutations and Bypass Mechanisms Can Contribute to Development of Acquired Resistance to MET Inhibitors von JIE QI, MCTIGUE, Michele A, ROGERS, Andrew, LIFSHITS, Eugene, CHRISTENSEN, James G, JÄNNE, Pasi A, ENGELMAN, Jeffrey A

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Nonclinical Antiangiogenesis and Antitumor Activities of Axitinib (AG-013736), an Oral, Potent, and Selective Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kina... von HU-LOWE, Dana D, ZOU, Helen Y, MCTIGUE, Michele A, MURRAY, Brion W, KANIA, Robert S, O'CONNOR, Patrick, SHALINSKY, David R, BENDER, Steve L, GRAZZINI, Maren L, HALLIN, Max E, WICKMAN, Grant R, AMUNDSON, Karin, CHEN, Jeffrey H, REWOLINSKI, David A, YAMAZAKI, Shinji, WU, Ellen Y

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Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Ki... von Cui, J. Jean, Tran-Dubé, Michelle, Shen, Hong, Nambu, Mitchell, Kung, Pei-Pei, Pairish, Mason, Jia, Lei, Meng, Jerry, Funk, Lee, Botrous, Iriny, McTigue, Michele, Grodsky, Neil, Ryan, Kevin, Padrique, Ellen, Alton, Gordon, Timofeevski, Sergei, Yamazaki, Shinji, Li, Qiuhua, Zou, Helen, Christensen, James, Mroczkowski, Barbara, Bender, Steve, Kania, Robert S, Edwards, Martin P

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PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations von Zou, Helen Y., Li, Qiuhua, Engstrom, Lars D., West, Melissa, Appleman, Vicky, Wong, Katy A., McTigue, Michele, Deng, Ya-Li, Liu, Wei, Brooun, Alexei, Timofeevski, Sergei, McDonnell, Scott R. P., Jiang, Ping, Falk, Matthew D., Lappin, Patrick B., Affolter, Timothy, Nichols, Tim, Hu, Wenyue, Lam, Justine, Johnson, Ted W., Smeal, Tod, Charest, Al, Fantin, Valeria R.

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Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer von Freeman-Cook, Kevin D, Hoffman, Robert L, Behenna, Douglas C, Boras, Britton, Carelli, Jordan, Diehl, Wade, Ferre, Rose Ann, He, You-Ai, Hui, Andrea, Huang, Buwen, Huser, Nanni, Jones, Rhys, Kephart, Susan E, Lapek, John, McTigue, Michele, Miller, Nichol, Murray, Brion W, Nagata, Asako, Nguyen, Lisa, Niessen, Sherry, Ninkovic, Sacha, O’Doherty, Inish, Ornelas, Martha A, Solowiej, James, Sutton, Scott C, Tran, Khanh, Tseng, Elaine, Visswanathan, Ravi, Xu, Meirong, Zehnder, Luke, Zhang, Qin, Zhang, Cathy, Dann, Stephen

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KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients von Gajiwala, Ketan S, Wu, Joe C, Christensen, James, Deshmukh, Gayatri D, Diehl, Wade, DiNitto, Jonathan P, English, Jessie M, Greig, Michael J, He, You-Ai, Jacques, Suzanne L, Lunney, Elizabeth A, McTigue, Michele, Molina, David, Quenzer, Terri, Wells, Peter A, Yu, Xiu, Zhang, Yan, Zou, Aihua, Emmett, Mark R, Marshall, Alan G, Zhang, Hui-Min, Demetri, George D

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Missense mutations interfere with VEGFR-3 signalling in primary lymphoedema von Karkkainen, Marika J., Ferrell, Robert E., Lawrence, Elizabeth C., Kimak, Mark A., Levinson, Kara L., McTigue, Michele A., Alitalo, Kari, Finegold, David N.

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Discovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2‑(4-(1-... von Cui, J. Jean, McTigue, Michele, Nambu, Mitchell, Tran-Dubé, Michelle, Pairish, Mason, Shen, Hong, Jia, Lei, Cheng, Hengmiao, Hoffman, Jacqui, Le, Phuong, Jalaie, Mehran, Goetz, Gilles H, Ryan, Kevin, Grodsky, Neil, Deng, Ya-li, Parker, Max, Timofeevski, Sergei, Murray, Brion W, Yamazaki, Shinji, Aguirre, Shirley, Li, Qiuhua, Zou, Helen, Christensen, James

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Analysis of lorlatinib analogs reveals a roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer von Shiba-Ishii, Aya, Johnson, Ted W, Dagogo-Jack, Ibiayi, Mino-Kenudson, Mari, Johnson, Theodore R, Wei, Ping, Weinrich, Scott L, McTigue, Michele A, Walcott, Makeba A, Nguyen-Phuong, Linh, Dionne, Kristin, Acker, Adam, Kiedrowski, Lesli A, Do, Andrew, Peterson, Jennifer L, Barth, Jaimie L, Yeap, Beow Y, Gainor, Justin F, Lin, Jessica J, Yoda, Satoshi, Hata, Aaron N

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Enzymatic Characterization of c-Met Receptor Tyrosine Kinase Oncogenic Mutants and Kinetic Studies with Aminopyridine and Triazolopyrazine Inhibitors von Timofeevski, Sergei L, McTigue, Michele A, Ryan, Kevin, Cui, Jean, Zou, Helen Y, Zhu, Jeff X, Chau, Fannie, Alton, Gordon, Karlicek, Shannon, Christensen, James G, Murray, Brion W

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Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor von Zou, Helen Y, Li, Qiuhua, Lee, Joseph H, Arango, Maria E, Burgess, Kristina, Qiu, Ming, Engstrom, Lars D, Yamazaki, Shinji, Parker, Max, Timofeevski, Sergei, Cui, Jingrong Jean, McTigue, Michele, Los, Gerrit, Bender, Steven L, Smeal, Tod, Christensen, James G

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Reviving B‑Factors: Activating ALK Mutations Increase Protein Dynamics of the Unphosphorylated Kinase von Johnson, Ted W, Bolanos, Ben, Brooun, Alexei, Gallego, Rebecca A, Gehlhaar, Dan, Jalaie, Mehran, McTigue, Michele, Timofeevski, Sergei

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Characterizing the Effects of the Juxtamembrane Domain on Vascular Endothelial Growth Factor Receptor-2 Enzymatic Activity, Autophosphorylation, and Inhibition by Axitinib von Solowiej, James, Bergqvist, Simon, McTigue, Michele A, Marrone, Tami, Quenzer, Terri, Cobbs, Morena, Ryan, Kevin, Kania, Robert S, Diehl, Wade, Murray, Brion W

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Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2: a key enzyme in angiogenesis von McTigue, Michele A, Wickersham, John A, Pinko, Chris, Showalter, Richard E, Parast, Camran V, Tempczyk-Russell, Anna, Gehring, Michael R, Mroczkowski, Barbara, Kan, Chen-Chen, Villafranca, J Ernest, Appelt, Krzysztof

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Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F von Shaw, Alice T, Friboulet, Luc, Leshchiner, Ignaty, Gainor, Justin F, Bergqvist, Simon, Brooun, Alexei, Burke, Benjamin J, Deng, Ya-Li, Liu, Wei, Dardaei, Leila, Frias, Rosa L, Schultz, Kate R, Logan, Jennifer, James, Leonard P, Smeal, Tod, Timofeevski, Sergei, Katayama, Ryohei, Iafrate, A. John, Le, Long, McTigue, Michele, Getz, Gad, Johnson, Ted W, Engelman, Jeffrey A

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Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation von Pemovska, Tea, Johnson, Eric, Kontro, Mika, Repasky, Gretchen A., Chen, Jeffrey, Wells, Peter, Cronin, Ciarán N., McTigue, Michele, Kallioniemi, Olli, Porkka, Kimmo, Murray, Brion W., Wennerberg, Krister

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Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-0646392... von Johnson, Ted W, Richardson, Paul F, Bailey, Simon, Brooun, Alexei, Burke, Benjamin J, Collins, Michael R, Cui, J Jean, Deal, Judith G, Deng, Ya-Li, Dinh, Dac, Engstrom, Lars D, He, Mingying, Hoffman, Jacqui, Hoffman, Robert L, Huang, Qinhua, Kania, Robert S, Kath, John C, Lam, Hieu, Lam, Justine L, Le, Phuong T, Lingardo, Laura, Liu, Wei, McTigue, Michele, Palmer, Cynthia L, Sach, Neal W, Smeal, Tod, Smith, Graham L, Stewart, Albert E, Timofeevski, Sergei, Zhu, Huichun, Zhu, Jinjiang, Zou, Helen Y, Edwards, Martin P

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Mechanistic Effects of Autophosphorylation on Receptor Tyrosine Kinase Catalysis:  Enzymatic Characterization of Tie2 and Phospho-Tie2 von Murray, Brion W, Padrique, Ellen S, Pinko, Chris, McTigue, Michele A

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Acquired Resistance to Crizotinib from a Mutation in CD74–ROS1 von Awad, Mark M, Katayama, Ryohei, McTigue, Michele, Liu, Wei, Deng, Ya-Li, Brooun, Alexei, Friboulet, Luc, Huang, Donghui, Falk, Matthew D, Timofeevski, Sergei, Wilner, Keith D, Lockerman, Elizabeth L, Khan, Tahsin M, Mahmood, Sidra, Gainor, Justin F, Digumarthy, Subba R, Stone, James R, Mino-Kenudson, Mari, Christensen, James G, Iafrate, A. John, Engelman, Jeffrey A, Shaw, Alice T

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