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46 results on '"Walter Annette O"'

1. Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling

Author

Graham, Keith, Lienau, Philip, Bader, Benjamin, Prechtl, Stefan, Naujoks, Jan, Lesche, Ralf, Weiske, Joerg, Kuehnlenz, Julia, Brzezinka, Krzysztof, Potze, Lisette, Zanconato, Francesca, Nicke, Barbara, Montebaur, Anna, Bone, Wilhelm, Golfier, Sven, Kaulfuss, Stefan, Kopitz, Charlotte, Pilari, Sabine, Steuber, Holger, Hayat, Sikander, Kamburov, Atanas, Steffen, Andreas, Schlicker, Andreas, Buchgraber, Philipp, Braeuer, Nico, Font, Nuria Aiguabella, Heinrich, Tobias, Kuhnke, Lara, Nowak-Reppel, Katrin, Stresemann, Carlo, Steigemann, Patrick, Walter, Annette O., Blotta, Simona, Ocker, Matthias, Lakner, Ashley, von Nussbaum, Franz, Mumberg, Dominik, Eis, Knut, Piccolo, Stefano, and Lange, Martin

Published
2024
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2. Anetumab ravtansine versus vinorelbine in patients with relapsed, mesothelin-positive malignant pleural mesothelioma (ARCS-M): a randomised, open-label phase 2 trial

Author

Kindler, Hedy L, Novello, Silvia, Bearz, Alessandra, Ceresoli, Giovanni L, Aerts, Joachim G J V, Spicer, James, Taylor, Paul, Nackaerts, Kristiaan, Greystoke, Alastair, Jennens, Ross, Calabrò, Luana, Burgers, Jacobus A, Santoro, Armando, Cedrés, Susana, Serwatowski, Piotr, Ponce, Santiago, Van Meerbeeck, Jan P, Nowak, Anna K, Blumenschein, George, Jr, Siegel, Jonathan M, Kasten, Linda, Köchert, Karl, Walter, Annette O, Childs, Barrett H, Elbi, Cem, Hassan, Raffit, and Fennell, Dean A

Published
2022
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4. Supplementary Figure 8 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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5. Supplementary Figure 9 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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6. Supplementary Tables 1 through 4 and Supplementary Figures 1 through 5 from In Vitro and In Vivo Characterization of Irreversible Mutant-Selective EGFR Inhibitors That Are Wild-Type Sparing

Author

Tjin Tham Sjin, Robert, primary, Lee, Kwangho, primary, Walter, Annette O., primary, Dubrovskiy, Aleksandr, primary, Sheets, Michael, primary, Martin, Thia St., primary, Labenski, Matthew T., primary, Zhu, Zhendong, primary, Tester, Richland, primary, Karp, Russell, primary, Medikonda, Aravind, primary, Chaturvedi, Prasoon, primary, Ren, Yixuan, primary, Haringsma, Henry, primary, Etter, Jeff, primary, Raponi, Mitch, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Westlin, William F., primary, Petter, Russell C., primary, Allen, Andrew, primary, and Singh, Juswinder, primary

Published
2023
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7. Supplementary Figure 2 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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8. Data from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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9. Supplementary Materials and Methods from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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10. Supplementary Figure 7 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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11. Supplementary Figure 11 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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12. Supplementary Figure 3 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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13. Supplementary Table 2 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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14. Supplementary Table 1 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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15. Supplementary Table 3 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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16. Supplementary Materials and Methods and Supplementary Figure Legends from In Vitro and In Vivo Characterization of Irreversible Mutant-Selective EGFR Inhibitors That Are Wild-Type Sparing

Author

Tjin Tham Sjin, Robert, primary, Lee, Kwangho, primary, Walter, Annette O., primary, Dubrovskiy, Aleksandr, primary, Sheets, Michael, primary, Martin, Thia St., primary, Labenski, Matthew T., primary, Zhu, Zhendong, primary, Tester, Richland, primary, Karp, Russell, primary, Medikonda, Aravind, primary, Chaturvedi, Prasoon, primary, Ren, Yixuan, primary, Haringsma, Henry, primary, Etter, Jeff, primary, Raponi, Mitch, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Westlin, William F., primary, Petter, Russell C., primary, Allen, Andrew, primary, and Singh, Juswinder, primary

Published
2023
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17. Supplementary Figure 4 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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18. Supplementary Figure 5 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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19. Supplementary Figure 6 from Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, primary, Haringsma, Henry J., primary, Ohashi, Kadoaki, primary, Sun, Jing, primary, Lee, Kwangho, primary, Dubrovskiy, Aleksandr, primary, Labenski, Matthew, primary, Zhu, Zhendong, primary, Wang, Zhigang, primary, Sheets, Michael, primary, St Martin, Thia, primary, Karp, Russell, primary, van Kalken, Dan, primary, Chaturvedi, Prasoon, primary, Niu, Deqiang, primary, Nacht, Mariana, primary, Petter, Russell C., primary, Westlin, William, primary, Lin, Kevin, primary, Jaw-Tsai, Sarah, primary, Raponi, Mitch, primary, Van Dyke, Terry, primary, Etter, Jeff, primary, Weaver, Zoe, primary, Pao, William, primary, Singh, Juswinder, primary, Simmons, Andrew D., primary, Harding, Thomas C., primary, and Allen, Andrew, primary

Published
2023
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20. Safety and activity of anti-mesothelin antibody–drug conjugate anetumab ravtansine in combination with pegylated-liposomal doxorubicin in platinum-resistant ovarian cancer: multicenter, phase Ib dose escalation and expansion study

Author

Santin, Alessandro D, primary, Vergote, Ignace, additional, González-Martín, Antonio, additional, Moore, Kathleen, additional, Oaknin, Ana, additional, Romero, Ignacio, additional, Diab, Sami, additional, Copeland, Larry J, additional, Monk, Bradley J, additional, Coleman, Robert L, additional, Herzog, Thomas J, additional, Siegel, Jonathan, additional, Kasten, Linda, additional, Schlicker, Andreas, additional, Schulz, Anke, additional, Köchert, Karl, additional, Walter, Annette O, additional, Childs, Barrett H, additional, Elbi, Cem, additional, and Bulat, Iurie, additional

Published
2022
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21. Safety and activity of anti-mesothelin antibody-drug conjugate anetumab ravtansine in combination with pegylated-liposomal doxorubicin in platinum-resistant ovarian cancer: multicenter, phase Ib dose escalation and expansion study.

Author

Santin, Alessandro D., Vergote, Ignace, González-Martín, Antonio, Moore, Kathleen, Oaknin, Ana, Romero, Ignacio, Diab, Sami, Copeland, Larry J., Monk, Bradley J., Coleman, Robert L., Herzog, Thomas J., Siegel, Jonathan, Kasten, Linda, Schlicker, Andreas, Schulz, Anke, Köchert, Karl, Walter, Annette O., Childs, Barrett H., Elbi, Cem, and Bulat, Iurie

Published
2023
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24. First-in-Human, Multicenter, Phase I Dose-Escalation and Expansion Study of Anti-Mesothelin Antibody–Drug Conjugate Anetumab Ravtansine in Advanced or Metastatic Solid Tumors

Author

Hassan, Raffit, primary, Blumenschein, George R., additional, Moore, Kathleen N., additional, Santin, Alessandro D., additional, Kindler, Hedy L., additional, Nemunaitis, John J., additional, Seward, Shelly M., additional, Thomas, Anish, additional, Kim, Stella K., additional, Rajagopalan, Prabhu, additional, Walter, Annette O., additional, Laurent, Dirk, additional, Childs, Barrett H., additional, Sarapa, Nenad, additional, Elbi, Cem, additional, and Bendell, Johanna C., additional

Published
2020
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25. Abstract 4816: Anetumab ravtansine has monotherapy efficacy in mesothelin positive patient-derived NSCLC tumor models and in a syngeneic tumor model in immunocompetent mice

Author

Sommer, Anette, primary, Lejeune, Pascale, additional, Hoff, Sabine, additional, Walter, Annette O., additional, Berndt, Sandra, additional, Roese, Lars, additional, Schlicker, Andreas, additional, Wick, Michael J., additional, Elbi, Cem, additional, Mumberg, Dominik, additional, and Schatz, Christoph, additional

Published
2019
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26. First-in-human phase I study of the bromodomain and extraterminal motif inhibitor BAY 1238097: emerging pharmacokinetic/pharmacodynamic relationship and early termination due to unexpected toxicity

Author

Postel-Vinay, Sophie, primary, Herbschleb, Karin, additional, Massard, Christophe, additional, Woodcock, Victoria, additional, Soria, Jean-Charles, additional, Walter, Annette O., additional, Ewerton, Flavio, additional, Poelman, Martine, additional, Benson, Neil, additional, Ocker, Matthias, additional, Wilkinson, Gary, additional, and Middleton, Mark, additional

Published
2019
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27. The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5

Author

Nathan Brammeier, Walter Annette O, Duhl David, Dirksen E. Bussiere, Paul A. Barsanti, Weibo Wang, Zhi-Jie Ni, and Eric J. Martin

Subjects
Models, Molecular, Molecular model, medicine.drug_class, Clinical Biochemistry, Allosteric regulation, Kinesins, Pharmaceutical Science, Carboxamide, Crystallography, X-Ray, Biochemistry, Structure-Activity Relationship, Allosteric Regulation, Cell Line, Tumor, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Enzyme Inhibitors, Solid tumor, Molecular Biology, Binding Sites, Drug discovery, Chemistry, Organic Chemistry, High-Throughput Screening Assays, Rats, Beta Carbolines, Molecular Medicine, Kinesin, Carbolines
Abstract

A series of tetrahydro-beta-carbolines were identified by HTS as inhibitors of the kinesin Eg5. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of removing potential metabolic liabilities and improving cellular potency.

Published
2010
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28. 4-(1H-Indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors

Author

Weiping Jia, Walter Annette O, Cornelia Bellamacina, Song Lin, Mika Lindvall, Asha Yabannavar, Cynthia M. Shafer, and Thomas G. Gesner

Subjects
Indazoles, Molecular model, Stereochemistry, Chemistry, Pharmaceutical, Clinical Biochemistry, Molecular Conformation, Pharmaceutical Science, Cell Cycle Proteins, Pyrimidinones, Non-specific serine/threonine protein kinase, Protein Serine-Threonine Kinases, Biochemistry, Inhibitory Concentration 50, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, Humans, Pyrimidone, Enzyme Inhibitors, Molecular Biology, chemistry.chemical_classification, Indazole, Binding Sites, Molecular Structure, Bicyclic molecule, biology, Organic Chemistry, Enzyme, Models, Chemical, chemistry, Enzyme inhibitor, Drug Design, Benzene derivatives, biology.protein, Molecular Medicine, Caco-2 Cells
Abstract

A series of 4-(4-hydroxyphenyl)-6-phenylpyrimidin-2(1H)-ones were identified by HTS as inhibitors of CDC7. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus on removing potential metabolic liabilities and improving cellular potency.

Published
2008
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29. Phase I dose-escalation studies of roniciclib, a pan-cyclin-dependent kinase inhibitor, in advanced malignancies

Author

Bahleda, Rastislav, primary, Grilley-Olson, Juneko E, additional, Govindan, Ramaswamy, additional, Barlesi, Fabrice, additional, Greillier, Laurent, additional, Perol, Maurice, additional, Ray-Coquard, Isabelle, additional, Strumberg, Dirk, additional, Schultheis, Beate, additional, Dy, Grace K, additional, Zalcman, Gérard, additional, Weiss, Glen J, additional, Walter, Annette O, additional, Kornacker, Martin, additional, Rajagopalan, Prabhu, additional, Henderson, David, additional, Nogai, Hendrik, additional, Ocker, Matthias, additional, and Soria, Jean-Charles, additional

Published
2017
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30. Abstract 3022: BAY 1143572, a first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, shows convincing anti-tumor activity in preclinical models of acute myeloid leukemia (AML)

Author

Scholz, Arne, primary, Oellerich, Thomas, additional, Hussain, Akhtar, additional, Lindner, Sarah, additional, Luecking, Ulrich, additional, Walter, Annette O., additional, Ellinghaus, Peter, additional, Valencia, Ray, additional, von Nussbaum, Franz, additional, Mumberg, Dominik, additional, Brands, Michael, additional, Ince, Stuart, additional, Serve, Hubert, additional, and Ziegelbauer, Karl, additional

Published
2016
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31. 3D Pharmacophore Model-Assisted Discovery of Novel CDC7 Inhibitors

Author

Kent Wong, Cynthia M. Shafer, Walter Annette O, Maureen Mckenna, Song Lin, Mika Lindvall, Christopher McBride, Asha Yabannavar, and Thomas G. Gesner

Subjects
Chemistry, Docking (molecular), Organic Chemistry, Drug Discovery, Structure–activity relationship, Computational biology, Homology modeling, Pharmacophore, Biochemistry, Combinatorial chemistry, LigandScout
Abstract

A ligand-based 3D pharmacophore model for serine/threonine kinase CDC7 inhibition was created and successfully applied in the discovery of novel 2-(heteroaryl)-6,7-dihydrothieno[3,2-c]pyridin-4(5H)-ones. The pharmacophore model provided a hypothesis for lead generation missed by docking to a homology model. Medicinal chemistry exploration of the series revealed clear structure–activity relationships consistent with the pharmacophore model and pointed to further optimization opportunities.

Published
2011

32. Abstract 3524: BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models

Author

Lejeune, Pascale, primary, Sugawara, Tatsuo, additional, Gelato, Kathy A., additional, Ellinger-Ziegelbauer, Heidrun, additional, Fernandez-Montalvan, Amaury E., additional, Schmees, Norbert, additional, Siegel, Stephan, additional, Weinmann, Hilmar, additional, Gekeler, Volker, additional, Walter, Annette O., additional, Ocker, Matthias, additional, Ince, Stuart, additional, and Haendler, Bernard, additional

Published
2015
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33. Abstract DDT02-02: BAY 1143572: A first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis

Author

Scholz, Arne, primary, Luecking, Ulrich, additional, Siemeister, Gerhard, additional, Lienau, Philip, additional, Boemer, Ulf, additional, Ellinghaus, Peter, additional, Walter, Annette O., additional, Valencia, Ray, additional, Ince, Stuart, additional, von Nussbaum, Franz, additional, Mumberg, Dominik, additional, Brands, Michael, additional, and Ziegelbauer, Karl, additional

Published
2015
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34. Inhibition of Cdc7/Dbf4 kinase activity affects specific phosphorylation sites on MCM2 in cancer cells

Author

Marco Wallroth, Jamie Narberes, Sylvia Chow, Asha Yabannavar, Deborah Charych, Walter Annette O, Cynthia M. Shafer, and Mazie Y. Coyne

Subjects
Lung Neoplasms, Molecular Sequence Data, Apoptosis, Cell Cycle Proteins, Biology, Mitogen-activated protein kinase kinase, Protein Serine-Threonine Kinases, Biochemistry, Mass Spectrometry, Minichromosome maintenance, Cell Line, Tumor, Humans, Amino Acid Sequence, Kinase activity, Phosphorylation, Molecular Biology, MAPK14, Serine/threonine-specific protein kinase, MAP kinase kinase kinase, Nuclear Proteins, Minichromosome Maintenance Complex Component 2, Cell Biology, Molecular biology, Chromatin, Mutagenesis, Colonic Neoplasms, Origin recognition complex
Abstract

The Cdc7/Dbf4 kinase is required for initiation of DNA replication and also plays a role in checkpoint function in response to replication stress. Exactly how Cdc7/Dbf4 mediates those activities remains to be elucidated. Cdc7/Dbf4 physically interacts with and phosphorylates the minichromosome maintenance complex (MCM), such as MCM2, MCM4 and MCM6. Cdc7/Dbf4 activity is required for association of Cdc45 followed by recruitment of DNA polymerase on the chromatin. Using high resolution mass spectrometry, we identified six phosphorylation sites on MCM2, two of them have not been described before. We provide evidence that Cdc7/Dbf4 mediates phosphorylation on serine 108 and serine 40 on human MCM2 in vitro and in vivo in cancer cells in the absence of DNA damage. Antibodies specific to pS108 or pS40 confirmed the sites and established useful read-outs for inhibition of Cdc7/Dbf4. This report demonstrates the utility of an in vitro to in vivo workflow utilizing immunoprecipitation and mass spectrometry to map phosphorylation sites on endogenous kinase substrates. The approach can be readily generalized to identify target modulation read-outs for other potential kinase cancer targets.

Published
2008

36. Abstract CT209: A phase I study with the oral pan-CDK inhibitor BAY 1000394 in patients with advanced stage small cell lung or ovarian cancer

Author

Bahleda, Rastilav, primary, Barlesi, Fabrice, additional, Audebert, Christine, additional, Perol, Maurice, additional, Ray-Coquard, Isabelle, additional, Strumberg, Dirk, additional, Schultheis, Beate, additional, Govindan, Ramaswamy, additional, Dy, Grace K., additional, Zalcman, Gerard, additional, Walter, Annette O., additional, Kornacker, Martin, additional, Ocker, Matthias, additional, and Soria, Jean-Charles, additional

Published
2014
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37. In Vitro and In Vivo Characterization of Irreversible Mutant-Selective EGFR Inhibitors That Are Wild-Type Sparing

Author

Tjin Tham Sjin, Robert, primary, Lee, Kwangho, additional, Walter, Annette O., additional, Dubrovskiy, Aleksandr, additional, Sheets, Michael, additional, Martin, Thia St., additional, Labenski, Matthew T., additional, Zhu, Zhendong, additional, Tester, Richland, additional, Karp, Russell, additional, Medikonda, Aravind, additional, Chaturvedi, Prasoon, additional, Ren, Yixuan, additional, Haringsma, Henry, additional, Etter, Jeff, additional, Raponi, Mitch, additional, Simmons, Andrew D., additional, Harding, Thomas C., additional, Niu, Deqiang, additional, Nacht, Mariana, additional, Westlin, William F., additional, Petter, Russell C., additional, Allen, Andrew, additional, and Singh, Juswinder, additional

Published
2014
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38. Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

Author

Walter, Annette O., primary, Sjin, Robert Tjin Tham, additional, Haringsma, Henry J., additional, Ohashi, Kadoaki, additional, Sun, Jing, additional, Lee, Kwangho, additional, Dubrovskiy, Aleksandr, additional, Labenski, Matthew, additional, Zhu, Zhendong, additional, Wang, Zhigang, additional, Sheets, Michael, additional, St Martin, Thia, additional, Karp, Russell, additional, van Kalken, Dan, additional, Chaturvedi, Prasoon, additional, Niu, Deqiang, additional, Nacht, Mariana, additional, Petter, Russell C., additional, Westlin, William, additional, Lin, Kevin, additional, Jaw-Tsai, Sarah, additional, Raponi, Mitch, additional, Van Dyke, Terry, additional, Etter, Jeff, additional, Weaver, Zoe, additional, Pao, William, additional, Singh, Juswinder, additional, Simmons, Andrew D., additional, Harding, Thomas C., additional, and Allen, Andrew, additional

Published
2013
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44. Abstract 1791: CO-1686, a novel mutant-selective EGFR inhibitor, overcomes T790M mediated resistance in Non-Small Cell Lung Cancer (NSCLC)

Author

Walter, Annette O., primary, Tjin, Robert, additional, Haringsma, Henry, additional, Lin, Kevin, additional, Dubrovskiy, Alex, additional, Lee, Kwangho, additional, Martin, Thia St., additional, Karp, Russell, additional, Zhu, Zhendong, additional, Nu, Deqiang, additional, Nacht, Mariana, additional, Suda, Kenichi, additional, Mitsudomi, Tetsuya, additional, Petter, Russell C., additional, Westlin, William F., additional, Singh, Juswinder, additional, Raponi, Mitch, additional, and Allen, Andrew, additional

Published
2012
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45. Abstract C189: CO-1686, an orally available, mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), causes tumor shrinkage in non-small cell lung cancer (NSCLC) with T790M mutations.

Author

Walter, Annette O., primary, Tjin, Robert, additional, Haringsma, Henry, additional, Lin, Kevin, additional, Dubrovskiy, Alex, additional, Lee, Kwangho, additional, St. Martin, Thia, additional, Karp, Russell, additional, Zhu, Zhendong, additional, Niu, Deqiang, additional, Nacht, Mariana, additional, Petter, Russell C., additional, Westlin, William F., additional, Singh, Juswinder, additional, Raponi, Mitch, additional, and Allen, Andrew, additional

Published
2011
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