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2. Integrated CRISPR screening and drug profiling identifies combination opportunities for EGFR, ALK, and BRAF/MEK inhibitors

Author

Tiedt, Ralph, King, Frederick J., Stamm, Christelle, Niederst, Matthew J., Delach, Scott, Zumstein-Mecker, Sabine, Meltzer, Jodi, Mulford, Iain J., Labrot, Emma, Engstler, Barbara Schacher, Baltschukat, Sabrina, Kerr, Grainne, Golji, Javad, Wyss, Daniel, Schnell, Christian, Ainscow, Edward, Engelman, Jeffrey A., Sellers, William R., Barretina, Jordi, Caponigro, Giordano, and Porta, Diana Graus

Published
2023
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3. BET bromodomain inhibitors regulate keratinocyte plasticity

Author

Schutzius, Gabi, Kolter, Christian, Bergling, Sebastian, Tortelli, Federico, Fuchs, Florian, Renner, Steffen, Guagnano, Vito, Cotesta, Simona, Rueeger, Heinrich, Faller, Michael, Bouchez, Laure, Salathe, Adrian, Nigsch, Florian, Richards, Shola M., Louis, Malvina, Gruber, Viktoria, Aebi, Alexandra, Turner, Jonathan, Grandjean, Frederic, Li, Jun, Dimitri, Chris, Thomas, Jason R., Schirle, Markus, Blank, Jutta, Drueckes, Peter, Vaupel, Andrea, Tiedt, Ralph, Manley, Paul W., Klopp, Julia, Hemmig, Rene, Zink, Florence, Leroy, Nelly, Carbone, Walter, Roma, Guglielmo, Keller, Caroline Gubser, Dales, Natalie, Beyerbach, Armin, Zimmerlin, Alfred, Bonenfant, Debora, Terranova, Remi, Berwick, Amy, Sahambi, Sukhdeep, Reynolds, Aimee, Jennings, Lori L., Ruffner, Heinz, Tarsa, Peter, Bouwmeester, Tewis, Driver, Vickie, Frederiksen, Mathias, Lohmann, Felix, and Kirkland, Susan

Published
2021
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4. A phase 1b study of the MET inhibitor capmatinib combined with cetuximab in patients with MET-positive colorectal cancer who had progressed following anti-EGFR monoclonal antibody treatment

Author

Delord, Jean-Pierre, Argilés, Guillem, Fayette, Jerôme, Wirth, Lori, Kasper, Stefan, Siena, Salvatore, Mesia, Ricard, Berardi, Rossana, Cervantes, Andrés, Dekervel, Jeroen, Zhao, Sylvia, Sun, Yongjian, Hao, Huai-Xiang, Tiedt, Ralph, Vicente, Sergio, Myers, Andrea, and Siu, Lillian L.

Published
2020
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5. A Phase Ib/II, open-label, multicenter study of INC280 (capmatinib) alone and in combination with buparlisib (BKM120) in adult patients with recurrent glioblastoma

Author

van den Bent, Martin, Azaro, Analia, De Vos, Filip, Sepulveda, Juan, Yung, W. K. Alfred, Wen, Patrick Y., Lassman, Andrew B., Joerger, Markus, Tabatabai, Ghazaleh, Rodon, Jordi, Tiedt, Ralph, Zhao, Sylvia, Kirsilae, Tiina, Cheng, Yi, Vicente, Sergio, Balbin, O. Alejandro, Zhang, Hefei, and Wick, Wolfgang

Published
2020
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6. Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf−/− mouse model

Author

Chapeau, Emilie A., Gembarska, Agnieszka, Durand, Eric Y., Mandon, Emeline, Estadieu, Claire, Romanet, Vincent, Wiesmann, Marion, Tiedt, Ralph, Lehar, Joseph, deWeck, Antoine, Rad, Roland, Barys, Louise, Jeay, Sebastien, Ferretti, Stephane, Kauffmann, Audrey, Sutter, Esther, Grevot, Armelle, Moulin, Pierre, Murakami, Masato, Sellers, William R., Hofmann, Francesco, and Jensen, Michael Rugaard

Published
2017

7. Abstract 3449: Development of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for the treatment of lung cancers with MYC-induced translational addiction

Author

Gavory, Gerald, primary, Ghandi, Mahmoud, additional, d’Alessandro, Anne-Cecile, additional, Bonenfant, Debora, additional, Cabanski, Maciej, additional, Cantagallo, Lisa, additional, Chicas, Agustin, additional, Chen, Qian, additional, Diesslin, Anna, additional, King, Christopher, additional, Massafra, Vittoria, additional, Narayan, Rajiv, additional, Osmont, Arnaud, additional, Peck, Dave, additional, Ortiz, Carolina Perdomo, additional, Schillo, Martin, additional, Singh, Ambika, additional, Tiedt, Ralph, additional, Tortoioli, Simone, additional, Buonamici, Silvia, additional, Janku, Filip, additional, Wallace, Owen, additional, and Fasching, Bernhard, additional

Published
2023
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8. Supplementary Methods from Rescue Screens with Secreted Proteins Reveal Compensatory Potential of Receptor Tyrosine Kinases in Driving Cancer Growth

Author

Harbinski, Fred, primary, Craig, Vanessa J., primary, Sanghavi, Sneha, primary, Jeffery, Douglas, primary, Liu, Lijuan, primary, Sheppard, Kelly Ann, primary, Wagner, Sabrina, primary, Stamm, Christelle, primary, Buness, Andreas, primary, Chatenay-Rivauday, Christian, primary, Yao, Yao, primary, He, Feng, primary, Lu, Chris X., primary, Guagnano, Vito, primary, Metz, Thomas, primary, Finan, Peter M., primary, Hofmann, Francesco, primary, Sellers, William R., primary, Porter, Jeffrey A., primary, Myer, Vic E., primary, Graus-Porta, Diana, primary, Wilson, Christopher J., primary, Buckler, Alan, primary, and Tiedt, Ralph, primary

Published
2023
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9. Supplementary Figures 1-5 from Rescue Screens with Secreted Proteins Reveal Compensatory Potential of Receptor Tyrosine Kinases in Driving Cancer Growth

Author

Harbinski, Fred, primary, Craig, Vanessa J., primary, Sanghavi, Sneha, primary, Jeffery, Douglas, primary, Liu, Lijuan, primary, Sheppard, Kelly Ann, primary, Wagner, Sabrina, primary, Stamm, Christelle, primary, Buness, Andreas, primary, Chatenay-Rivauday, Christian, primary, Yao, Yao, primary, He, Feng, primary, Lu, Chris X., primary, Guagnano, Vito, primary, Metz, Thomas, primary, Finan, Peter M., primary, Hofmann, Francesco, primary, Sellers, William R., primary, Porter, Jeffrey A., primary, Myer, Vic E., primary, Graus-Porta, Diana, primary, Wilson, Christopher J., primary, Buckler, Alan, primary, and Tiedt, Ralph, primary

Published
2023
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10. Supplementary Table 1 from Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion–Positive Cholangiocarcinoma

Author

Goyal, Lipika, primary, Saha, Supriya K., primary, Liu, Leah Y., primary, Siravegna, Giulia, primary, Leshchiner, Ignaty, primary, Ahronian, Leanne G., primary, Lennerz, Jochen K., primary, Vu, Phuong, primary, Deshpande, Vikram, primary, Kambadakone, Avinash, primary, Mussolin, Benedetta, primary, Reyes, Stephanie, primary, Henderson, Laura, primary, Sun, Jiaoyuan Elisabeth, primary, Van Seventer, Emily E., primary, Gurski, Joseph M., primary, Baltschukat, Sabrina, primary, Schacher-Engstler, Barbara, primary, Barys, Louise, primary, Stamm, Christelle, primary, Furet, Pascal, primary, Ryan, David P., primary, Stone, James R., primary, Iafrate, A. John, primary, Getz, Gad, primary, Porta, Diana Graus, primary, Tiedt, Ralph, primary, Bardelli, Alberto, primary, Juric, Dejan, primary, Corcoran, Ryan B., primary, Bardeesy, Nabeel, primary, and Zhu, Andrew X., primary

Published
2023
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11. Data from Rescue Screens with Secreted Proteins Reveal Compensatory Potential of Receptor Tyrosine Kinases in Driving Cancer Growth

Author

Harbinski, Fred, primary, Craig, Vanessa J., primary, Sanghavi, Sneha, primary, Jeffery, Douglas, primary, Liu, Lijuan, primary, Sheppard, Kelly Ann, primary, Wagner, Sabrina, primary, Stamm, Christelle, primary, Buness, Andreas, primary, Chatenay-Rivauday, Christian, primary, Yao, Yao, primary, He, Feng, primary, Lu, Chris X., primary, Guagnano, Vito, primary, Metz, Thomas, primary, Finan, Peter M., primary, Hofmann, Francesco, primary, Sellers, William R., primary, Porter, Jeffrey A., primary, Myer, Vic E., primary, Graus-Porta, Diana, primary, Wilson, Christopher J., primary, Buckler, Alan, primary, and Tiedt, Ralph, primary

Published
2023
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12. Data from Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion–Positive Cholangiocarcinoma

Author

Goyal, Lipika, primary, Saha, Supriya K., primary, Liu, Leah Y., primary, Siravegna, Giulia, primary, Leshchiner, Ignaty, primary, Ahronian, Leanne G., primary, Lennerz, Jochen K., primary, Vu, Phuong, primary, Deshpande, Vikram, primary, Kambadakone, Avinash, primary, Mussolin, Benedetta, primary, Reyes, Stephanie, primary, Henderson, Laura, primary, Sun, Jiaoyuan Elisabeth, primary, Van Seventer, Emily E., primary, Gurski, Joseph M., primary, Baltschukat, Sabrina, primary, Schacher-Engstler, Barbara, primary, Barys, Louise, primary, Stamm, Christelle, primary, Furet, Pascal, primary, Ryan, David P., primary, Stone, James R., primary, Iafrate, A. John, primary, Getz, Gad, primary, Porta, Diana Graus, primary, Tiedt, Ralph, primary, Bardelli, Alberto, primary, Juric, Dejan, primary, Corcoran, Ryan B., primary, Bardeesy, Nabeel, primary, and Zhu, Andrew X., primary

Published
2023
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13. Supplementary Figures 1 - 6 from Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion–Positive Cholangiocarcinoma

Author

Goyal, Lipika, primary, Saha, Supriya K., primary, Liu, Leah Y., primary, Siravegna, Giulia, primary, Leshchiner, Ignaty, primary, Ahronian, Leanne G., primary, Lennerz, Jochen K., primary, Vu, Phuong, primary, Deshpande, Vikram, primary, Kambadakone, Avinash, primary, Mussolin, Benedetta, primary, Reyes, Stephanie, primary, Henderson, Laura, primary, Sun, Jiaoyuan Elisabeth, primary, Van Seventer, Emily E., primary, Gurski, Joseph M., primary, Baltschukat, Sabrina, primary, Schacher-Engstler, Barbara, primary, Barys, Louise, primary, Stamm, Christelle, primary, Furet, Pascal, primary, Ryan, David P., primary, Stone, James R., primary, Iafrate, A. John, primary, Getz, Gad, primary, Porta, Diana Graus, primary, Tiedt, Ralph, primary, Bardelli, Alberto, primary, Juric, Dejan, primary, Corcoran, Ryan B., primary, Bardeesy, Nabeel, primary, and Zhu, Andrew X., primary

Published
2023
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14. Supplementary Tables 1-3 and Table 5 from Rescue Screens with Secreted Proteins Reveal Compensatory Potential of Receptor Tyrosine Kinases in Driving Cancer Growth

Author

Harbinski, Fred, primary, Craig, Vanessa J., primary, Sanghavi, Sneha, primary, Jeffery, Douglas, primary, Liu, Lijuan, primary, Sheppard, Kelly Ann, primary, Wagner, Sabrina, primary, Stamm, Christelle, primary, Buness, Andreas, primary, Chatenay-Rivauday, Christian, primary, Yao, Yao, primary, He, Feng, primary, Lu, Chris X., primary, Guagnano, Vito, primary, Metz, Thomas, primary, Finan, Peter M., primary, Hofmann, Francesco, primary, Sellers, William R., primary, Porter, Jeffrey A., primary, Myer, Vic E., primary, Graus-Porta, Diana, primary, Wilson, Christopher J., primary, Buckler, Alan, primary, and Tiedt, Ralph, primary

Published
2023
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15. Supplementary Table 4 from Rescue Screens with Secreted Proteins Reveal Compensatory Potential of Receptor Tyrosine Kinases in Driving Cancer Growth

Author

Harbinski, Fred, primary, Craig, Vanessa J., primary, Sanghavi, Sneha, primary, Jeffery, Douglas, primary, Liu, Lijuan, primary, Sheppard, Kelly Ann, primary, Wagner, Sabrina, primary, Stamm, Christelle, primary, Buness, Andreas, primary, Chatenay-Rivauday, Christian, primary, Yao, Yao, primary, He, Feng, primary, Lu, Chris X., primary, Guagnano, Vito, primary, Metz, Thomas, primary, Finan, Peter M., primary, Hofmann, Francesco, primary, Sellers, William R., primary, Porter, Jeffrey A., primary, Myer, Vic E., primary, Graus-Porta, Diana, primary, Wilson, Christopher J., primary, Buckler, Alan, primary, and Tiedt, Ralph, primary

Published
2023
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16. Supplementary Tables from Capmatinib (INC280) Is Active Against Models of Non–Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation

Author

Baltschukat, Sabrina, primary, Engstler, Barbara Schacher, primary, Huang, Alan, primary, Hao, Huai-Xiang, primary, Tam, Angela, primary, Wang, Hui Qin, primary, Liang, Jinsheng, primary, DiMare, Matthew T., primary, Bhang, Hyo-Eun Carrie, primary, Wang, Youzhen, primary, Furet, Pascal, primary, Sellers, William R., primary, Hofmann, Francesco, primary, Schoepfer, Joseph, primary, and Tiedt, Ralph, primary

Published
2023
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17. Supplementary Data from Phase Ib Study of Ribociclib plus Fulvestrant and Ribociclib plus Fulvestrant plus PI3K Inhibitor (Alpelisib or Buparlisib) for HR+ Advanced Breast Cancer

Author

Tolaney, Sara M., primary, Im, Young-Hyuck, primary, Calvo, Emiliano, primary, Lu, Yen-Shen, primary, Hamilton, Erika, primary, Forero-Torres, Andres, primary, Bachelot, Thomas, primary, Maur, Michela, primary, Fasolo, Angelica, primary, Tiedt, Ralph, primary, Nardi, Lisa, primary, Stammberger, Uz, primary, Abdelhady, Ahmed M., primary, Ruan, Shiling, primary, and Lee, Soo Chin, primary

Published
2023
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18. Supplementary Data from Capmatinib (INC280) Is Active Against Models of Non–Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation

Author

Baltschukat, Sabrina, primary, Engstler, Barbara Schacher, primary, Huang, Alan, primary, Hao, Huai-Xiang, primary, Tam, Angela, primary, Wang, Hui Qin, primary, Liang, Jinsheng, primary, DiMare, Matthew T., primary, Bhang, Hyo-Eun Carrie, primary, Wang, Youzhen, primary, Furet, Pascal, primary, Sellers, William R., primary, Hofmann, Francesco, primary, Schoepfer, Joseph, primary, and Tiedt, Ralph, primary

Published
2023
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19. Data from A Drug Resistance Screen Using a Selective MET Inhibitor Reveals a Spectrum of Mutations That Partially Overlap with Activating Mutations Found in Cancer Patients

Author

Tiedt, Ralph, primary, Degenkolbe, Elisa, primary, Furet, Pascal, primary, Appleton, Brent A., primary, Wagner, Sabrina, primary, Schoepfer, Joseph, primary, Buck, Emily, primary, Ruddy, David A., primary, Monahan, John E., primary, Jones, Michael D., primary, Blank, Jutta, primary, Haasen, Dorothea, primary, Drueckes, Peter, primary, Wartmann, Markus, primary, McCarthy, Clive, primary, Sellers, William R., primary, and Hofmann, Francesco, primary

Published
2023
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20. Supplementary Figures 1-2, Tables 1-4, Methods from A Drug Resistance Screen Using a Selective MET Inhibitor Reveals a Spectrum of Mutations That Partially Overlap with Activating Mutations Found in Cancer Patients

Author

Tiedt, Ralph, primary, Degenkolbe, Elisa, primary, Furet, Pascal, primary, Appleton, Brent A., primary, Wagner, Sabrina, primary, Schoepfer, Joseph, primary, Buck, Emily, primary, Ruddy, David A., primary, Monahan, John E., primary, Jones, Michael D., primary, Blank, Jutta, primary, Haasen, Dorothea, primary, Drueckes, Peter, primary, Wartmann, Markus, primary, McCarthy, Clive, primary, Sellers, William R., primary, and Hofmann, Francesco, primary

Published
2023
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21. Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition

Author

Fassl, Anne, Brain, Christopher, Abu-Remaileh, Monther, Stukan, Iga, Butter, Deborah, Stepien, Piotr, Feit, Avery S., Bergholz, Johann, Michowski, Wojciech, Otto, Tobias, Sheng, Qing, Loo, Alice, Michael, Walter, Tiedt, Ralph, DeAngelis, Carmine, Schiff, Rachel, Jiang, Baishan, Jovanovic, Bojana, Nowak, Karolina, Ericsson, Maria, Cameron, Michael, Gray, Nathanael, Dillon, Deborah, Zhao, Jean J., Sabatini, David M., Jeselsohn, Rinath, Brown, Myles, Polyak, Kornelia, Sicinski, Piotr, Fassl, Anne, Brain, Christopher, Abu-Remaileh, Monther, Stukan, Iga, Butter, Deborah, Stepien, Piotr, Feit, Avery S., Bergholz, Johann, Michowski, Wojciech, Otto, Tobias, Sheng, Qing, Loo, Alice, Michael, Walter, Tiedt, Ralph, DeAngelis, Carmine, Schiff, Rachel, Jiang, Baishan, Jovanovic, Bojana, Nowak, Karolina, Ericsson, Maria, Cameron, Michael, Gray, Nathanael, Dillon, Deborah, Zhao, Jean J., Sabatini, David M., Jeselsohn, Rinath, Brown, Myles, Polyak, Kornelia, and Sicinski, Piotr

Abstract

© 2020 The Authors, some rights reserved; exclusive licensee American Association for the Advancement of Science. No claim to original U.S. Government Works. Distributed under a Creative Commons Attribution NonCommercial License 4.0 (CC BY-NC). Inhibitors of cyclin-dependent kinases CDK4 and CDK6 have been approved for treatment of hormone receptor-positive breast cancers. In contrast, triple-negative breast cancers (TNBCs) are resistant to CDK4/6 inhibition. Here, we demonstrate that a subset of TNBC critically requires CDK4/6 for proliferation, and yet, these TNBC are resistant to CDK4/6 inhibition due to sequestration of CDK4/6 inhibitors into tumor cell lysosomes. This sequestration is caused by enhanced lysosomal biogenesis and increased lysosomal numbers in TNBC cells. We developed new CDK4/6 inhibitor compounds that evade the lysosomal sequestration and are efficacious against resistant TNBC. We also show that coadministration of lysosomotropic or lysosome-destabilizing compounds (an antibiotic azithromycin, an antidepressant siramesine, an antimalaria compound chloroquine) renders resistant tumor cells sensitive to currently used CDK4/6 inhibitors. Lastly, coinhibition of CDK2 arrested proliferation of CDK4/6 inhibitor-resistant cells. These observations may extend the use of CDK4/6 inhibitors to TNBCs that are refractory to current anti-CDK4/6 therapies.

Published
2022

22. Abstract P5-13-18: Upregulation of immune response biomarkers by ribociclib plus endocrine therapy (ET) in paired tumor samples from phase I studies

Author

Juric, Dejan, primary, Ma, Chong, additional, Tiedt, Ralph, additional, Yap, Yoon-Sim, additional, Chiu, Joanne, additional, Munster, Pamela, additional, Ismail-Khan, Roohi, additional, Garcia-Estevez, Laura, additional, Mayer, Ingrid A., additional, Becerra, Carlos, additional, Solovieff, Nadia, additional, Lteif, Agnes, additional, Su, Faye, additional, and Lu, Yen-Shen, additional

Published
2022
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24. Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition

Author

Fassl, Anne, Brain, Christopher, Abu-Remaileh, Monther, Stukan, Iga, Butter, Deborah, Stepien, Piotr, Feit, Avery S, Bergholz, Johann, Michowski, Wojciech, Otto, Tobias, Sheng, Qing, Loo, Alice, Michael, Walter, Tiedt, Ralph, DeAngelis, Carmine, Schiff, Rachel, Jiang, Baishan, Jovanovic, Bojana, Nowak, Karolina, Ericsson, Maria, Cameron, Michael, Gray, Nathanael, Dillon, Deborah, Zhao, Jean J, Sabatini, David M, Jeselsohn, Rinath, Brown, Myles, Polyak, Kornelia, Sicinski, Piotr, Fassl, Anne, Brain, Christopher, Abu-Remaileh, Monther, Stukan, Iga, Butter, Deborah, Stepien, Piotr, Feit, Avery S, Bergholz, Johann, Michowski, Wojciech, Otto, Tobias, Sheng, Qing, Loo, Alice, Michael, Walter, Tiedt, Ralph, DeAngelis, Carmine, Schiff, Rachel, Jiang, Baishan, Jovanovic, Bojana, Nowak, Karolina, Ericsson, Maria, Cameron, Michael, Gray, Nathanael, Dillon, Deborah, Zhao, Jean J, Sabatini, David M, Jeselsohn, Rinath, Brown, Myles, Polyak, Kornelia, and Sicinski, Piotr

Abstract

© 2020 The Authors, some rights reserved; exclusive licensee American Association for the Advancement of Science. No claim to original U.S. Government Works. Distributed under a Creative Commons Attribution NonCommercial License 4.0 (CC BY-NC). Inhibitors of cyclin-dependent kinases CDK4 and CDK6 have been approved for treatment of hormone receptor-positive breast cancers. In contrast, triple-negative breast cancers (TNBCs) are resistant to CDK4/6 inhibition. Here, we demonstrate that a subset of TNBC critically requires CDK4/6 for proliferation, and yet, these TNBC are resistant to CDK4/6 inhibition due to sequestration of CDK4/6 inhibitors into tumor cell lysosomes. This sequestration is caused by enhanced lysosomal biogenesis and increased lysosomal numbers in TNBC cells. We developed new CDK4/6 inhibitor compounds that evade the lysosomal sequestration and are efficacious against resistant TNBC. We also show that coadministration of lysosomotropic or lysosome-destabilizing compounds (an antibiotic azithromycin, an antidepressant siramesine, an antimalaria compound chloroquine) renders resistant tumor cells sensitive to currently used CDK4/6 inhibitors. Lastly, coinhibition of CDK2 arrested proliferation of CDK4/6 inhibitor-resistant cells. These observations may extend the use of CDK4/6 inhibitors to TNBCs that are refractory to current anti-CDK4/6 therapies.

Published
2021

25. A Phase Ib/II, open-label, multicenter study of INC280 (capmatinib) alone and in combination with buparlisib (BKM120) in adult patients with recurrent glioblastoma

Author

MS Medische Oncologie, Cancer, van den Bent, Martin, Azaro, Analia, De Vos, Filip, Sepulveda, Juan, Yung, W. K.Alfred, Wen, Patrick Y., Lassman, Andrew B., Joerger, Markus, Tabatabai, Ghazaleh, Rodon, Jordi, Tiedt, Ralph, Zhao, Sylvia, Kirsilae, Tiina, Cheng, Yi, Vicente, Sergio, Balbin, O. Alejandro, Zhang, Hefei, Wick, Wolfgang, MS Medische Oncologie, Cancer, van den Bent, Martin, Azaro, Analia, De Vos, Filip, Sepulveda, Juan, Yung, W. K.Alfred, Wen, Patrick Y., Lassman, Andrew B., Joerger, Markus, Tabatabai, Ghazaleh, Rodon, Jordi, Tiedt, Ralph, Zhao, Sylvia, Kirsilae, Tiina, Cheng, Yi, Vicente, Sergio, Balbin, O. Alejandro, Zhang, Hefei, and Wick, Wolfgang

Published
2020

26. Phase Ib Study of Ribociclib plus Fulvestrant and Ribociclib plus Fulvestrant plus PI3K Inhibitor (Alpelisib or Buparlisib) for HR+ Advanced Breast Cancer

Author

Tolaney, Sara M., primary, Im, Young-Hyuck, additional, Calvo, Emiliano, additional, Lu, Yen-Shen, additional, Hamilton, Erika, additional, Forero-Torres, Andres, additional, Bachelot, Thomas, additional, Maur, Michela, additional, Fasolo, Angelica, additional, Tiedt, Ralph, additional, Nardi, Lisa, additional, Stammberger, Uz, additional, Abdelhady, Ahmed M., additional, Ruan, Shiling, additional, and Lee, Soo Chin, additional

Published
2021
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27. A gain-of-function mutation of JAK2 in myeloproliferative disorders

Author

Kralovics, Robert, Passamonti, Francesco, Buser, Andreas S., Tiedt, Ralph, Passweg, Jakob R., Soon-Siong Teo, Tichelli, Andre, Cazzola, Mario, and Skoda, Radek C.

Subjects
Gene mutations -- Research, Hematopoietic growth factors -- Research, Myeloproliferative disorders -- Risk factors, Myeloproliferative disorders -- Diagnosis
Abstract

The loss of heterozygosity (LOH) on the short arm of chromosome 9 (9pLOH) in myeloproliferative disorders suggests that 9p harbors a mutation that contributes to the cause of clonal expansion of hematopoietic cells in these diseases. A high proportion of patients with myeloproliferative disorders carry a dominant gain-of-function mutation of JAK2.

Published
2005

29. Novel inhibitors of the histone methyltransferase DOT1L show potent antileukemic activity in patient-derived xenografts

Author

Perner, Florian, primary, Gadrey, Jayant Y., additional, Xiong, Yijun, additional, Hatton, Charles, additional, Eschle, Benjamin K., additional, Weiss, Andreas, additional, Stauffer, Frédéric, additional, Gaul, Christoph, additional, Tiedt, Ralph, additional, Perry, Jennifer A., additional, Armstrong, Scott A., additional, and Krivtsov, Andrei V., additional

Published
2020
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30. Abstract 1770: A new DOT1L inhibitor with in vivo activity in mouse models of MLL-translocated leukemia

Author

Weiss, Andreas, primary, Stauffer, Frederic, additional, Clemens, Clemens, additional, Möbitz, Henrik, additional, Ragot, Christian, additional, Beyer, Kim S., additional, Calkins, Keith, additional, Thoma, Claudio, additional, Guthy, Daniel, additional, Kiffe, Michael, additional, Van Eerdenbrugh, Bernard, additional, Sellers, William R., additional, Hofmann, Francesco, additional, Tiedt, Ralph, additional, and Gaul, Christoph, additional

Published
2020
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31. Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition

Author

Fassl, Anne, primary, Brain, Christopher, additional, Abu-Remaileh, Monther, additional, Stukan, Iga, additional, Butter, Deborah, additional, Stepien, Piotr, additional, Feit, Avery S., additional, Bergholz, Johann, additional, Michowski, Wojciech, additional, Otto, Tobias, additional, Sheng, Qing, additional, Loo, Alice, additional, Michael, Walter, additional, Tiedt, Ralph, additional, DeAngelis, Carmine, additional, Schiff, Rachel, additional, Jiang, Baishan, additional, Jovanovic, Bojana, additional, Nowak, Karolina, additional, Ericsson, Maria, additional, Cameron, Michael, additional, Gray, Nathanael, additional, Dillon, Deborah, additional, Zhao, Jean J., additional, Sabatini, David M., additional, Jeselsohn, Rinath, additional, Brown, Myles, additional, Polyak, Kornelia, additional, and Sicinski, Piotr, additional

Published
2020
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32. Correction: The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models

Author

Kim, Sunkyu, primary, Tiedt, Ralph, additional, Loo, Alice, additional, Horn, Thomas, additional, Delach, Scott, additional, Kovats, Steven, additional, Haas, Kristy, additional, Engstler, Barbara Schacher, additional, Cao, Alexander, additional, Pinzon-Ortiz, Maria, additional, Mulford, Iain, additional, Acker, Michael G., additional, Chopra, Rajiv, additional, Brain, Christopher, additional, Tomaso, Emmanuelle di, additional, Sellers, William R., additional, and Caponigro, Giordano, additional

Published
2020
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33. DOT1L inhibition is lethal for multiple myeloma due to perturbation of the endoplasmic reticulum stress pathway

Author

Dafflon, Caroline, primary, Gaulis, Swann, additional, Barys, Louise, additional, Kapur, Karen, additional, Cornacchione, Vanessa, additional, Schukur, Lina, additional, Bergling, Sebastian, additional, Traggiai, Elisabetta, additional, Jansky, Selina, additional, Hellmann, Leon, additional, Engstler, Barbara Schacher, additional, Kerr, Grainne, additional, Weck, Antoine de, additional, Ruddy, David A., additional, Naumann, Ulrike, additional, Stauffer, Frédéric, additional, Gaul, Christoph, additional, Lin, Ying, additional, Billy, Eric, additional, Weiss, Andreas, additional, Hofmann, Francesco, additional, Ito, Moriko, additional, and Tiedt, Ralph, additional

Published
2020
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34. New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse

Author

Stauffer, Frédéric, primary, Weiss, Andreas, additional, Scheufler, Clemens, additional, Möbitz, Henrik, additional, Ragot, Christian, additional, Beyer, Kim S., additional, Calkins, Keith, additional, Guthy, Daniel, additional, Kiffe, Michael, additional, Van Eerdenbrugh, Bernard, additional, Tiedt, Ralph, additional, and Gaul, Christoph, additional

Published
2019
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35. INC280X2201_HCC_Manuscript_Supplementary_Figure_S1 – Supplemental material for A phase II study of the efficacy and safety of the MET inhibitor capmatinib (INC280) in patients with advanced hepatocellular carcinoma

Author

Shukui Qin, Chan, Stephen Lam, Wattana Sukeepaisarnjaroen, Guohong Han, Choo, Su Pin, Virote Sriuranpong, Hongming Pan, Yau, Thomas, Yabing Guo, Minshan Chen, Zhenggang Ren, Jianming Xu, Chia-Jui Yen, Zhong-Zhe Lin, Manenti, Luigi, Gu, Yi, Yongjian Sun, Tiedt, Ralph, Hao, Lu, Wenjie Song, and Tawesak Tanwandee

Subjects
110203 Respiratory Diseases, FOS: Clinical medicine, 111702 Aged Health Care, FOS: Health sciences, 111599 Pharmacology and Pharmaceutical Sciences not elsewhere classified, 111299 Oncology and Carcinogenesis not elsewhere classified
Abstract

Supplemental material, INC280X2201_HCC_Manuscript_Supplementary_Figure_S1 for A phase II study of the efficacy and safety of the MET inhibitor capmatinib (INC280) in patients with advanced hepatocellular carcinoma by Shukui Qin, Stephen Lam Chan, Wattana Sukeepaisarnjaroen, Guohong Han, Su Pin Choo, Virote Sriuranpong, Hongming Pan, Thomas Yau, Yabing Guo, Minshan Chen, Zhenggang Ren, Jianming Xu, Chia-Jui Yen, Zhong-Zhe Lin, Luigi Manenti, Yi Gu, Yongjian Sun, Ralph Tiedt, Lu Hao, Wenjie Song and Tawesak Tanwandee in Therapeutic Advances in Medical Oncology

Published
2019
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37. A Phase Ib/II, open-label, multicenter study of INC280 (capmatinib) alone and in combination with buparlisib (BKM120) in adult patients with recurrent glioblastoma

Author

van den Bent, Martin, primary, Azaro, Analia, additional, De Vos, Filip, additional, Sepulveda, Juan, additional, Yung, W. K. Alfred, additional, Wen, Patrick Y., additional, Lassman, Andrew B., additional, Joerger, Markus, additional, Tabatabai, Ghazaleh, additional, Rodon, Jordi, additional, Tiedt, Ralph, additional, Zhao, Sylvia, additional, Kirsilae, Tiina, additional, Cheng, Yi, additional, Vicente, Sergio, additional, Balbin, O. Alejandro, additional, Zhang, Hefei, additional, and Wick, Wolfgang, additional

Published
2019
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38. A conditional inducible JAK2V617F transgenic mouse model reveals myeloproliferative disease that is reversible upon switching off transgene expression

Author

Chapeau, Emilie A., primary, Mandon, Emeline, additional, Gill, Jason, additional, Romanet, Vincent, additional, Ebel, Nicolas, additional, Powajbo, Violetta, additional, Andraos-Rey, Rita, additional, Qian, Zhiyan, additional, Kininis, Miltos, additional, Zumstein-Mecker, Sabine, additional, Ito, Moriko, additional, Hynes, Nancy E., additional, Tiedt, Ralph, additional, Hofmann, Francesco, additional, Eshkind, Leonid, additional, Bockamp, Ernesto, additional, Kinzel, Bernd, additional, Mueller, Matthias, additional, Murakami, Masato, additional, Baffert, Fabienne, additional, and Radimerski, Thomas, additional

Published
2019
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39. Capmatinib (INC280) Is Active Against Models of Non–Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation

Author

Baltschukat, Sabrina, primary, Engstler, Barbara Schacher, additional, Huang, Alan, additional, Hao, Huai-Xiang, additional, Tam, Angela, additional, Wang, Hui Qin, additional, Liang, Jinsheng, additional, DiMare, Matthew T., additional, Bhang, Hyo-Eun Carrie, additional, Wang, Youzhen, additional, Furet, Pascal, additional, Sellers, William R., additional, Hofmann, Francesco, additional, Schoepfer, Joseph, additional, and Tiedt, Ralph, additional

Published
2019
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40. A phase II study of the efficacy and safety of the MET inhibitor capmatinib (INC280) in patients with advanced hepatocellular carcinoma

Author

Qin, Shukui, primary, Chan, Stephen Lam, additional, Sukeepaisarnjaroen, Wattana, additional, Han, Guohong, additional, Choo, Su Pin, additional, Sriuranpong, Virote, additional, Pan, Hongming, additional, Yau, Thomas, additional, Guo, Yabing, additional, Chen, Minshan, additional, Ren, Zhenggang, additional, Xu, Jianming, additional, Yen, Chia-Jui, additional, Lin, Zhong-Zhe, additional, Manenti, Luigi, additional, Gu, Yi, additional, Sun, Yongjian, additional, Tiedt, Ralph, additional, Hao, Lu, additional, Song, Wenjie, additional, and Tanwandee, Tawesak, additional

Published
2019
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41. The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models

Author

Kim, Sunkyu, primary, Tiedt, Ralph, additional, Loo, Alice, additional, Horn, Thomas, additional, Delach, Scott, additional, Kovats, Steven, additional, Haas, Kristy, additional, Engstler, Barbara Schacher, additional, Cao, Alexander, additional, Pinzon-Ortiz, Maria, additional, Mulford, Iain, additional, Acker, Michael G., additional, Chopra, Rajiv, additional, Brain, Christopher, additional, di Tomaso, Emmanuelle, additional, Sellers, William R., additional, and Caponigro, Giordano, additional

Published
2018
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42. ACTR-74. A PHASE IB/II, OPEN-LABEL, MULTICENTER STUDY OF CAPMATINIB (INC280) ALONE AND IN COMBINATION WITH BUPARLISIB (BKM120) IN ADULT PATIENTS WITH RECURRENT GLIOBLASTOMA

Author

van den Bent, Martin, primary, Azaro, Analia, additional, Vos, Filip, additional, Sepulveda, Juan, additional, Yung, W K Alfred, additional, Wen, Patrick, additional, Lassman, Andrew, additional, Joerger, Markus, additional, Tabatabai, Ghazaleh, additional, Rodon, Jordi, additional, Tiedt, Ralph, additional, Zhao, Sylvia, additional, Kirsilae, Tiina, additional, Vicente, Sergio, additional, Myers, Andrea, additional, and Wick, Wolfgang, additional

Published
2017
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44. Abstract 4114: Polyclonal secondary FGFR2 mutations drive acquired resistance to FGFR inhibition in FGFR2 fusion-positive cholangiocarcinoma patients

Author

Goyal, Lipika, primary, Saha, Supriya K., additional, Liu, Leah Y., additional, Siravegna, Giulia, additional, Leshchiner, Ignaty, additional, Ahronian, Leanne G., additional, Lennerz, Jochen K., additional, Vu, Phuong, additional, Mussolin, Benedetta, additional, Reyes, Stephanie, additional, Furet, Pascal, additional, Iafrate, A. John, additional, Getz, Gad, additional, Porta, Diana G., additional, Tiedt, Ralph, additional, Bardelli, Alberto, additional, Juric, Dejan, additional, Corcoran, Ryan B., additional, Bardeesy, Nabeel, additional, and Zhu, Andrew X., additional

Published
2017
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46. Project DRIVE: A Compendium of Cancer Dependencies and Synthetic Lethal Relationships Uncovered by Large-Scale, Deep RNAi Screening

Author

McDonald, E. Robert, primary, de Weck, Antoine, additional, Schlabach, Michael R., additional, Billy, Eric, additional, Mavrakis, Konstantinos J., additional, Hoffman, Gregory R., additional, Belur, Dhiren, additional, Castelletti, Deborah, additional, Frias, Elizabeth, additional, Gampa, Kalyani, additional, Golji, Javad, additional, Kao, Iris, additional, Li, Li, additional, Megel, Philippe, additional, Perkins, Thomas A., additional, Ramadan, Nadire, additional, Ruddy, David A., additional, Silver, Serena J., additional, Sovath, Sosathya, additional, Stump, Mark, additional, Weber, Odile, additional, Widmer, Roland, additional, Yu, Jianjun, additional, Yu, Kristine, additional, Yue, Yingzi, additional, Abramowski, Dorothee, additional, Ackley, Elizabeth, additional, Barrett, Rosemary, additional, Berger, Joel, additional, Bernard, Julie L., additional, Billig, Rebecca, additional, Brachmann, Saskia M., additional, Buxton, Frank, additional, Caothien, Roger, additional, Caushi, Justina X., additional, Chung, Franklin S., additional, Cortés-Cros, Marta, additional, deBeaumont, Rosalie S., additional, Delaunay, Clara, additional, Desplat, Aurore, additional, Duong, William, additional, Dwoske, Donald A., additional, Eldridge, Richard S., additional, Farsidjani, Ali, additional, Feng, Fei, additional, Feng, JiaJia, additional, Flemming, Daisy, additional, Forrester, William, additional, Galli, Giorgio G., additional, Gao, Zhenhai, additional, Gauter, François, additional, Gibaja, Veronica, additional, Haas, Kristy, additional, Hattenberger, Marc, additional, Hood, Tami, additional, Hurov, Kristen E., additional, Jagani, Zainab, additional, Jenal, Mathias, additional, Johnson, Jennifer A., additional, Jones, Michael D., additional, Kapoor, Avnish, additional, Korn, Joshua, additional, Liu, Jilin, additional, Liu, Qiumei, additional, Liu, Shumei, additional, Liu, Yue, additional, Loo, Alice T., additional, Macchi, Kaitlin J., additional, Martin, Typhaine, additional, McAllister, Gregory, additional, Meyer, Amandine, additional, Mollé, Sandra, additional, Pagliarini, Raymond A., additional, Phadke, Tanushree, additional, Repko, Brian, additional, Schouwey, Tanja, additional, Shanahan, Frances, additional, Shen, Qiong, additional, Stamm, Christelle, additional, Stephan, Christine, additional, Stucke, Volker M., additional, Tiedt, Ralph, additional, Varadarajan, Malini, additional, Venkatesan, Kavitha, additional, Vitari, Alberto C., additional, Wallroth, Marco, additional, Weiler, Jan, additional, Zhang, Jing, additional, Mickanin, Craig, additional, Myer, Vic E., additional, Porter, Jeffery A., additional, Lai, Albert, additional, Bitter, Hans, additional, Lees, Emma, additional, Keen, Nicholas, additional, Kauffmann, Audrey, additional, Stegmeier, Frank, additional, Hofmann, Francesco, additional, Schmelzle, Tobias, additional, and Sellers, William R., additional

Published
2017
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47. Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf −/− mouse model

Author

Chapeau, Emilie A., primary, Gembarska, Agnieszka, additional, Durand, Eric Y., additional, Mandon, Emeline, additional, Estadieu, Claire, additional, Romanet, Vincent, additional, Wiesmann, Marion, additional, Tiedt, Ralph, additional, Lehar, Joseph, additional, de Weck, Antoine, additional, Rad, Roland, additional, Barys, Louise, additional, Jeay, Sebastien, additional, Ferretti, Stephane, additional, Kauffmann, Audrey, additional, Sutter, Esther, additional, Grevot, Armelle, additional, Moulin, Pierre, additional, Murakami, Masato, additional, Sellers, William R., additional, Hofmann, Francesco, additional, and Jensen, Michael Rugaard, additional

Published
2017
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48. Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion–Positive Cholangiocarcinoma

Author

Goyal, Lipika, primary, Saha, Supriya K., additional, Liu, Leah Y., additional, Siravegna, Giulia, additional, Leshchiner, Ignaty, additional, Ahronian, Leanne G., additional, Lennerz, Jochen K., additional, Vu, Phuong, additional, Deshpande, Vikram, additional, Kambadakone, Avinash, additional, Mussolin, Benedetta, additional, Reyes, Stephanie, additional, Henderson, Laura, additional, Sun, Jiaoyuan Elisabeth, additional, Van Seventer, Emily E., additional, Gurski, Joseph M., additional, Baltschukat, Sabrina, additional, Schacher-Engstler, Barbara, additional, Barys, Louise, additional, Stamm, Christelle, additional, Furet, Pascal, additional, Ryan, David P., additional, Stone, James R., additional, Iafrate, A. John, additional, Getz, Gad, additional, Porta, Diana Graus, additional, Tiedt, Ralph, additional, Bardelli, Alberto, additional, Juric, Dejan, additional, Corcoran, Ryan B., additional, Bardeesy, Nabeel, additional, and Zhu, Andrew X., additional

Published
2017
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49. Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach

Author

Möbitz, Henrik, primary, Machauer, Rainer, additional, Holzer, Philipp, additional, Vaupel, Andrea, additional, Stauffer, Frédéric, additional, Ragot, Christian, additional, Caravatti, Giorgio, additional, Scheufler, Clemens, additional, Fernandez, Cesar, additional, Hommel, Ulrich, additional, Tiedt, Ralph, additional, Beyer, Kim S., additional, Chen, Chao, additional, Zhu, Hugh, additional, and Gaul, Christoph, additional

Published
2017
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50. A conditional inducible JAK2V617F transgenic mouse model reveals myeloproliferative disease that is reversible upon switching off transgene expression.

Author

Chapeau, Emilie A., Mandon, Emeline, Gill, Jason, Romanet, Vincent, Ebel, Nicolas, Powajbo, Violetta, Andraos-Rey, Rita, Qian, Zhiyan, Kininis, Miltos, Zumstein-Mecker, Sabine, Ito, Moriko, Hynes, Nancy E., Tiedt, Ralph, Hofmann, Francesco, Eshkind, Leonid, Bockamp, Ernesto, Kinzel, Bernd, Mueller, Matthias, Murakami, Masato, and Baffert, Fabienne

Subjects
TRANSGENIC mice, HEMATOPOIETIC stem cells, POLYCYTHEMIA vera, BONE marrow cells, TRANSGENE expression, DISEASES
Abstract

Aberrant activation of the JAK/STAT pathway is thought to be the critical event in the pathogenesis of the chronic myeloproliferative neoplasms, polycythemia vera, essential thrombocythemia and primary myelofibrosis. The most frequent genetic alteration in these pathologies is the activating JAK2V617F mutation, and expression of the mutant gene in mouse models was shown to cause a phenotype resembling the human diseases. Given the body of genetic evidence, it has come as a sobering finding that JAK inhibitor therapy only modestly suppresses the JAK2V617F allele burden, despite showing clear benefits in terms of reducing splenomegaly and constitutional symptoms in patients. To gain a better understanding if JAK2V617F is required for maintenance of myeloproliferative disease once it has evolved, we generated a conditional inducible transgenic JAK2V617F mouse model using the SCL-tTA-2S tet-off system. Our model corroborates that expression of JAK2V617F in hematopoietic stem and progenitor cells recapitulates key hallmarks of human myeloproliferative neoplasms, and exhibits gender differences in disease manifestation. The disease was found to be transplantable, and importantly, reversible when transgenic JAK2V617F expression was switched off. Our results indicate that mutant JAK2V617F-specific inhibitors should result in profound disease modification by disabling the myeloproliferative clone bearing mutant JAK2. [ABSTRACT FROM AUTHOR]

Published
2019
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