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2. Correction: Oncogenic Transformation by Inhibitor-Sensitive and -Resistant EGFR Mutants

Author

Greulich, Heidi, Chen, Tzu-Hsiu, Feng, Whei, Jänne, Pasi A., Alvarez, James V., Zappaterra, Mauro, Bulmer, Sara E., Frank, David A., Hahn, William C., Sellers, William R., and Meyerson, Matthew

Subjects
Biological sciences
Abstract

Author(s): Heidi Greulich, Tzu-Hsiu Chen, Whei Feng, Pasi A. Jänne, James V. Alvarez, Mauro Zappaterra, Sara E. Bulmer, David A. Frank, William C. Hahn, William R. Sellers, Matthew Meyerson After [...]

Published
2024
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5. 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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6. Next-generation characterization of the Cancer Cell Line Encyclopedia

Author

Ghandi, Mahmoud, Huang, Franklin W, Jané-Valbuena, Judit, Kryukov, Gregory V, Lo, Christopher C, McDonald, E Robert, Barretina, Jordi, Gelfand, Ellen T, Bielski, Craig M, Li, Haoxin, Hu, Kevin, Andreev-Drakhlin, Alexander Y, Kim, Jaegil, Hess, Julian M, Haas, Brian J, Aguet, François, Weir, Barbara A, Rothberg, Michael V, Paolella, Brenton R, Lawrence, Michael S, Akbani, Rehan, Lu, Yiling, Tiv, Hong L, Gokhale, Prafulla C, de Weck, Antoine, Mansour, Ali Amin, Oh, Coyin, Shih, Juliann, Hadi, Kevin, Rosen, Yanay, Bistline, Jonathan, Venkatesan, Kavitha, Reddy, Anupama, Sonkin, Dmitriy, Liu, Manway, Lehar, Joseph, Korn, Joshua M, Porter, Dale A, Jones, Michael D, Golji, Javad, Caponigro, Giordano, Taylor, Jordan E, Dunning, Caitlin M, Creech, Amanda L, Warren, Allison C, McFarland, James M, Zamanighomi, Mahdi, Kauffmann, Audrey, Stransky, Nicolas, Imielinski, Marcin, Maruvka, Yosef E, Cherniack, Andrew D, Tsherniak, Aviad, Vazquez, Francisca, Jaffe, Jacob D, Lane, Andrew A, Weinstock, David M, Johannessen, Cory M, Morrissey, Michael P, Stegmeier, Frank, Schlegel, Robert, Hahn, William C, Getz, Gad, Mills, Gordon B, Boehm, Jesse S, Golub, Todd R, Garraway, Levi A, and Sellers, William R

Subjects
Genetics, Human Genome, Lung, Cancer, Biotechnology, Lung Cancer, Aetiology, 2.1 Biological and endogenous factors, Good Health and Well Being, Antineoplastic Agents, Biomarkers, Tumor, Cell Line, Tumor, DNA Methylation, Drug Resistance, Neoplasm, Ethnicity, Gene Editing, Histones, Humans, MicroRNAs, Molecular Targeted Therapy, Neoplasms, Protein Array Analysis, RNA Splicing, General Science & Technology
Abstract

Large panels of comprehensively characterized human cancer models, including the Cancer Cell Line Encyclopedia (CCLE), have provided a rigorous framework with which to study genetic variants, candidate targets, and small-molecule and biological therapeutics and to identify new marker-driven cancer dependencies. To improve our understanding of the molecular features that contribute to cancer phenotypes, including drug responses, here we have expanded the characterizations of cancer cell lines to include genetic, RNA splicing, DNA methylation, histone H3 modification, microRNA expression and reverse-phase protein array data for 1,072 cell lines from individuals of various lineages and ethnicities. Integration of these data with functional characterizations such as drug-sensitivity, short hairpin RNA knockdown and CRISPR-Cas9 knockout data reveals potential targets for cancer drugs and associated biomarkers. Together, this dataset and an accompanying public data portal provide a resource for the acceleration of cancer research using model cancer cell lines.

Published
2019

10. Paralog knockout profiling identifies DUSP4 and DUSP6 as a digenic dependence in MAPK pathway-driven cancers

Author

Ito, Takahiro, Young, Michael J., Li, Ruitong, Jain, Sidharth, Wernitznig, Andreas, Krill-Burger, John M., Lemke, Christopher T., Monducci, Davide, Rodriguez, Diego J., Chang, Liang, Dutta, Sanjukta, Pal, Debjani, Paolella, Brenton R., Rothberg, Michael V., Root, David E., Johannessen, Cory M., Parida, Laxmi, Getz, Gad, Vazquez, Francisca, Doench, John G., Zamanighomi, Mahdi, and Sellers, William R.

Published
2021
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11. Molecular basis for substrate recruitment to the PRMT5 methylosome

Author

Mulvaney, Kathleen M., Blomquist, Christa, Acharya, Nischal, Li, Ruitong, Ranaghan, Matthew J., O’Keefe, Meghan, Rodriguez, Diego J., Young, Michael J., Kesar, Devishi, Pal, Debjani, Stokes, Matthew, Nelson, Alissa J., Jain, Sidharth S., Yang, Annan, Mullin-Bernstein, Zachary, Columbus, Josie, Bozal, Fazli K., Skepner, Adam, Raymond, Donald, LaRussa, Salvatore, McKinney, David C., Freyzon, Yelena, Baidi, Yossef, Porter, Dale, Aguirre, Andrew J., Ianari, Alessandra, McMillan, Brian, and Sellers, William R.

Published
2021
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14. Facilitating a culture of responsible and effective sharing of cancer genome data

Author

Siu, Lillian L, Lawler, Mark, Haussler, David, Knoppers, Bartha Maria, Lewin, Jeremy, Vis, Daniel J, Liao, Rachel G, Andre, Fabrice, Banks, Ian, Barrett, J Carl, Caldas, Carlos, Camargo, Anamaria Aranha, Fitzgerald, Rebecca C, Mao, Mao, Mattison, John E, Pao, William, Sellers, William R, Sullivan, Patrick, Teh, Bin Tean, Ward, Robyn L, ZenKlusen, Jean Claude, Sawyers, Charles L, and Voest, Emile E

Subjects
Health Services and Systems, Health Sciences, Cancer, Cancer Genomics, Biotechnology, Human Genome, Genetics, Precision Medicine, Networking and Information Technology R&D (NITRD), Good Health and Well Being, Computational Biology, Culture, Databases, Genetic, Genome, Humans, Information Dissemination, Neoplasms, Medical and Health Sciences, Immunology, Biomedical and clinical sciences, Health sciences
Abstract

Rapid and affordable tumor molecular profiling has led to an explosion of clinical and genomic data poised to enhance the diagnosis, prognostication and treatment of cancer. A critical point has now been reached at which the analysis and storage of annotated clinical and genomic information in unconnected silos will stall the advancement of precision cancer care. Information systems must be harmonized to overcome the multiple technical and logistical barriers to data sharing. Against this backdrop, the Global Alliance for Genomic Health (GA4GH) was established in 2013 to create a common framework that enables responsible, voluntary and secure sharing of clinical and genomic data. This Perspective from the GA4GH Clinical Working Group Cancer Task Team highlights the data-aggregation challenges faced by the field, suggests potential collaborative solutions and describes how GA4GH can catalyze a harmonized data-sharing culture.

Published
2016

15. Quantitative Proteomics of the Cancer Cell Line Encyclopedia

Author

Nusinow, David P., Szpyt, John, Ghandi, Mahmoud, Rose, Christopher M., McDonald, E. Robert, III, Kalocsay, Marian, Jané-Valbuena, Judit, Gelfand, Ellen, Schweppe, Devin K., Jedrychowski, Mark, Golji, Javad, Porter, Dale A., Rejtar, Tomas, Wang, Y. Karen, Kryukov, Gregory V., Stegmeier, Frank, Erickson, Brian K., Garraway, Levi A., Sellers, William R., and Gygi, Steven P.

Published
2020
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16. A highly multiplexed quantitative phosphosite assay for biology and preclinical studies

Author

Keshishian, Hasmik, McDonald, III, E Robert, Mundt, Filip, Melanson, Randy, Krug, Karsten, Porter, Dale A, Wallace, Luke, Forestier, Dominique, Rabasha, Bokang, Marlow, Sara E, Jane‐Valbuena, Judit, Todres, Ellen, Specht, Harrison, Robinson, Margaret Lea, Jean Beltran, Pierre M, Babur, Ozgun, Olive, Meagan E, Golji, Javad, Kuhn, Eric, Burgess, Michael, MacMullan, Melanie A, Rejtar, Tomas, Wang, Karen, Mani, DR, Satpathy, Shankha, Gillette, Michael A, Sellers, William R, and Carr, Steven A

Published
2021
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17. TRPS1 Is a Lineage-Specific Transcriptional Dependency in Breast Cancer

Author

Witwicki, Robert M., Ekram, Muhammad B., Qiu, Xintao, Janiszewska, Michalina, Shu, Shaokun, Kwon, Mijung, Trinh, Anne, Frias, Elizabeth, Ramadan, Nadire, Hoffman, Greg, Yu, Kristine, Xie, Yingtian, McAllister, Gregory, McDonald, Rob, Golji, Javad, Schlabach, Michael, deWeck, Antoine, Keen, Nicholas, Chan, Ho Man, Ruddy, David, Rejtar, Tomas, Sovath, Sosathya, Silver, Serena, Sellers, William R., Jagani, Zainab, Hogarty, Michael D., Roberts, Charles, Brown, Myles, Stegmaier, Kimberly, Long, Henry, Shivdasani, Ramesh A., Pellman, David, and Polyak, Kornelia

Published
2018
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18. The landscape of cancer cell line metabolism

Author

Li, Haoxin, Ning, Shaoyang, Ghandi, Mahmoud, Kryukov, Gregory V., Gopal, Shuba, Deik, Amy, Souza, Amanda, Pierce, Kerry, Keskula, Paula, Hernandez, Desiree, Ann, Julie, Shkoza, Dojna, Apfel, Verena, Zou, Yilong, Vazquez, Francisca, Barretina, Jordi, Pagliarini, Raymond A., Galli, Giorgio G., Root, David E., Hahn, William C., Tsherniak, Aviad, Giannakis, Marios, Schreiber, Stuart L., Clish, Clary B., Garraway, Levi A., and Sellers, William R.

Published
2019
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19. K-RAS mutant pancreatic tumors show higher sensitivity to MEK than to PI3K inhibition in vivo.

Author

Hofmann, Irmgard, Weiss, Andreas, Elain, Gaelle, Schwaederle, Maria, Sterker, Dario, Romanet, Vincent, Schmelzle, Tobias, Lai, Albert, Brachmann, Saskia M, Bentires-Alj, Mohamed, Roberts, Thomas M, Sellers, William R, Hofmann, Francesco, and Maira, Sauveur-Michel

Subjects
Cell Line, Tumor, Animals, Humans, Mice, Mice, Nude, Pancreatic Neoplasms, Sulfonamides, Indazoles, Benzimidazoles, ras Proteins, Mitogen-Activated Protein Kinase Kinases, Extracellular Signal-Regulated MAP Kinases, Proto-Oncogene Proteins, Protein Kinase Inhibitors, Xenograft Model Antitumor Assays, Cell Proliferation, Phosphorylation, Mutation, Models, Biological, Female, Proto-Oncogene Proteins p21(ras), Proto-Oncogene Proteins c-akt, Gene Knockdown Techniques, Phosphatidylinositol 3-Kinases, HEK293 Cells, Phosphoinositide-3 Kinase Inhibitors, Cell Line, Tumor, Nude, Models, Biological, General Science & Technology
Abstract

Activating K-RAS mutations occur at a frequency of 90% in pancreatic cancer, and to date no therapies exist targeting this oncogene. K-RAS signals via downstream effector pathways such as the MAPK and the PI3K signaling pathways, and much effort has been focused on developing drugs targeting components of these pathways. To better understand the requirements for K-RAS and its downstream signaling pathways MAPK and PI3K in pancreatic tumor maintenance, we established an inducible K-RAS knock down system that allowed us to ablate K-RAS in established tumors. Knock down of K-RAS resulted in impaired tumor growth in all pancreatic xenograft models tested, demonstrating that K-RAS expression is indeed required for tumor maintenance of K-RAS mutant pancreatic tumors. We further examined signaling downstream of K-RAS, and detected a robust reduction of pERK levels upon K-RAS knock down. In contrast, no effect on pAKT levels could be observed due to almost undetectable basal expression levels. To investigate the requirement of the MAPK and the PI3K pathways on tumor maintenance, three selected pancreatic xenograft models were tested for their response to MEK or PI3K inhibition. Tumors of all three models regressed upon MEK inhibition, but showed less pronounced response to PI3K inhibition. The effect of MEK inhibition on pancreatic xenografts could be enhanced further by combined application of a PI3K inhibitor. These data provide further rationale for testing combinations of MEK and PI3K inhibitors in clinical trials comprising a patient population with pancreatic cancer harboring mutations in K-RAS.

Published
2012

20. p63 Regulates Commitment to the Prostate Cell Lineage

Author

Signoretti, Sabina, Pires, Maira M., Lindauer, Meghan, Horner, James W., Grisanzio, Chiara, Dhar, Sonya, Majumder, Pradip, McKeon, Frank, Kantoff, Philip W., Sellers, William R., Loda, Massimo, and Witte, Owen N.

Published
2005

21. Subtype-specific genomic alterations define new targets for soft-tissue sarcoma therapy

Author

Barretina, Jordi, Taylor, Barry S, Banerji, Shantanu, Ramos, Alexis H, Lagos-Quintana, Mariana, DeCarolis, Penelope L, Shah, Kinjal, Socci, Nicholas D, Weir, Barbara A, Ho, Alan, Chiang, Derek Y, Reva, Boris, Mermel, Craig H, Getz, Gad, Antipin, Yevgenyi, Beroukhim, Rameen, Major, John E, Hatton, Charles, Nicoletti, Richard, Hanna, Megan, Sharpe, Ted, Fennell, Tim J, Cibulskis, Kristian, Onofrio, Robert C, Saito, Tsuyoshi, Shukla, Neerav, Lau, Christopher, Nelander, Sven, Silver, Serena J, Sougnez, Carrie, Viale, Agnes, Winckler, Wendy, Maki, Robert G, Garraway, Levi A, Lash, Alex, Greulich, Heidi, Root, David E, Sellers, William R, Schwartz, Gary K, Antonescu, Cristina R, Lander, Eric S, Varmus, Harold E, Ladanyi, Marc, Sander, Chris, Meyerson, Matthew, and Singer, Samuel

Subjects
Pediatric, Biotechnology, Cancer, Human Genome, Genetics, Adult, Aged, Female, Genes, Tumor Suppressor, Genome, Histiocytoma, Malignant Fibrous, Humans, Liposarcoma, Male, Middle Aged, Mutation, Sarcoma, Biological Sciences, Medical and Health Sciences, Developmental Biology
Abstract

Soft-tissue sarcomas, which result in approximately 10,700 diagnoses and 3,800 deaths per year in the United States, show remarkable histologic diversity, with more than 50 recognized subtypes. However, knowledge of their genomic alterations is limited. We describe an integrative analysis of DNA sequence, copy number and mRNA expression in 207 samples encompassing seven major subtypes. Frequently mutated genes included TP53 (17% of pleomorphic liposarcomas), NF1 (10.5% of myxofibrosarcomas and 8% of pleomorphic liposarcomas) and PIK3CA (18% of myxoid/round-cell liposarcomas, or MRCs). PIK3CA mutations in MRCs were associated with Akt activation and poor clinical outcomes. In myxofibrosarcomas and pleomorphic liposarcomas, we found both point mutations and genomic deletions affecting the tumor suppressor NF1. Finally, we found that short hairpin RNA (shRNA)-based knockdown of several genes amplified in dedifferentiated liposarcoma, including CDK4 and YEATS4, decreased cell proliferation. Our study yields a detailed map of molecular alterations across diverse sarcoma subtypes and suggests potential subtype-specific targets for therapy.

Published
2010

23. 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

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

Author

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

Published
2017
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27. Epidermal Growth Factor Receptor Activation in Glioblastoma through Novel Missense Mutations in the Extracellular Domain.

Author

Lee, Jeffrey C, Vivanco, Igor, Beroukhim, Rameen, Huang, Julie H Y, Feng, Whei L, Debiasi, Ralph M, Yoshimoto, Koji, King, Jennifer C, Nghiemphu, Phioanh, Yuza, Yuki, Xu, Qing, Greulich, Heidi, Thomas, Roman K, Paez, J Guillermo, Peck, Timothy C, Linhart, David J, Glatt, Karen A, Getz, Gad, Onofrio, Robert, Ziaugra, Liuda, Levine, Ross L, Gabriel, Stacey, Kawaguchi, Tomohiro, O'neill, Keith, Khan, Haumith, Liau, Linda M, Nelson, Stanley F, Rao, P Nagesh, Mischel, Paul, Pieper, Russell O, Cloughesy, Tim, Leahy, Daniel J, Sellers, William R, Sawyers, Charles L, Meyerson, Matthew, and Mellinghoff, Ingo K

Abstract

BACKGROUND: Protein tyrosine kinases are important regulators of cellular homeostasis with tightly controlled catalytic activity. Mutations in kinase-encoding genes can relieve the autoinhibitory constraints on kinase activity, can promote malignant transformation, and appear to be a major determinant of response to kinase inhibitor therapy. Missense mutations in the EGFR kinase domain, for example, have recently been identified in patients who showed clinical responses to EGFR kinase inhibitor therapy. METHODS AND FINDINGS: Encouraged by the promising clinical activity of epidermal growth factor receptor (EGFR) kinase inhibitors in treating glioblastoma in humans, we have sequenced the complete EGFR coding sequence in glioma tumor samples and cell lines. We identified novel missense mutations in the extracellular domain of EGFR in 13.6% (18/132) of glioblastomas and 12.5% (1/8) of glioblastoma cell lines. These EGFR mutations were associated with increased EGFR gene dosage and conferred anchorage-independent growth and tumorigenicity to NIH-3T3 cells. Cells transformed by expression of these EGFR mutants were sensitive to small-molecule EGFR kinase inhibitors. CONCLUSIONS: Our results suggest extracellular missense mutations as a novel mechanism for oncogenic EGFR activation and may help identify patients who can benefit from EGFR kinase inhibitors for treatment of glioblastoma.

Published
2006

29. Abstract B037: Hit-finding by Cysteine-Scanning (HCS): A method for finding druggable pockets

Author

van Tienen, Laurens Moore, primary, Bayoumi, Shadwa, additional, Muneeruddin, Khaja, additional, Leymarie, Nancy, additional, Kornfilt, David, additional, Bian, Yuemin, additional, Kesar, Devishi, additional, Li, Ruitong, additional, Atack, Thomas, additional, Popa, Alexandra-Mariela, additional, Jandova, Zuzana, additional, Trollmann, Philipp, additional, Bergner, Andreas, additional, Rumpel, Klaus, additional, Kessler, Dirk, additional, and Sellers, William R., additional

Published
2023
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31. Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5

Author

Mavrakis, Konstantinos J., McDonald, E. Robert, Schlabach, Michael R., Billy, Eric, Hoffman, Gregory R., deWeck, Antoine, Ruddy, David A., Venkatesan, Kavitha, Yu, Jianjun, McAllister, Gregg, Stump, Mark, deBeaumont, Rosalie, Ho, Samuel, Yue, Yingzi, Liu, Yue, Yan-Neale, Yan, Yang, Guizhi, Lin, Fallon, Yin, Hong, Gao, Hui, Kipp, D. Randal, Zhao, Songping, McNamara, Joshua T., Sprague, Elizabeth R., Zheng, Bing, Lin, Ying, Cho, Young Shin, Gu, Justin, Crawford, Kenneth, Ciccone, David, Vitari, Alberto C., Lai, Albert, Capka, Vladimir, Hurov, Kristen, Porter, Jeffery A., Tallarico, John, Mickanin, Craig, Lees, Emma, Pagliarini, Raymond, Keen, Nicholas, Schmelzle, Tobias, Hofmann, Francesco, Stegmeier, Frank, and Sellers, William R.

Published
2016

33. Data from Discovery and Optimization of HKT288, a Cadherin-6–Targeting ADC for the Treatment of Ovarian and Renal Cancers

Author

Bialucha, Carl U., primary, Collins, Scott D., primary, Li, Xiao, primary, Saxena, Parmita, primary, Zhang, Xiamei, primary, Dürr, Clemens, primary, Lafont, Bruno, primary, Prieur, Pierric, primary, Shim, Yeonju, primary, Mosher, Rebecca, primary, Lee, David, primary, Ostrom, Lance, primary, Hu, Tiancen, primary, Bilic, Sanela, primary, Rajlic, Ivana Liric, primary, Capka, Vladimir, primary, Jiang, Wei, primary, Wagner, Joel P., primary, Elliott, GiNell, primary, Veloso, Artur, primary, Piel, Jessica C., primary, Flaherty, Meghan M., primary, Mansfield, Keith G., primary, Meseck, Emily K., primary, Rubic-Schneider, Tina, primary, London, Anne Serdakowski, primary, Tschantz, William R., primary, Kurz, Markus, primary, Nguyen, Duc, primary, Bourret, Aaron, primary, Meyer, Matthew J., primary, Faris, Jason E., primary, Janatpour, Mary J., primary, Chan, Vivien W., primary, Yoder, Nicholas C., primary, Catcott, Kalli C., primary, McShea, Molly A., primary, Sun, Xiuxia, primary, Gao, Hui, primary, Williams, Juliet, primary, Hofmann, Francesco, primary, Engelman, Jeffrey A., primary, Ettenberg, Seth A., primary, Sellers, William R., primary, and Lees, Emma, primary

Published
2023
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34. Supplementary Figure Legends 1-5 from FGFR Genetic Alterations Predict for Sensitivity to NVP-BGJ398, a Selective Pan-FGFR Inhibitor

Author

Guagnano, Vito, primary, Kauffmann, Audrey, primary, Wöhrle, Simon, primary, Stamm, Christelle, primary, Ito, Moriko, primary, Barys, Louise, primary, Pornon, Astrid, primary, Yao, Yao, primary, Li, Fang, primary, Zhang, Yun, primary, Chen, Zhi, primary, Wilson, Christopher J., primary, Bordas, Vincent, primary, Le Douget, Mickaël, primary, Gaither, L. Alex, primary, Borawski, Jason, primary, Monahan, John E., primary, Venkatesan, Kavitha, primary, Brümmendorf, Thomas, primary, Thomas, David M., primary, Garcia-Echeverria, Carlos, primary, Hofmann, Francesco, primary, Sellers, William R., primary, and Graus-Porta, Diana, primary

Published
2023
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35. Supplementary Figure 4 from Characterization of the Mechanism of Action of the Pan Class I PI3K Inhibitor NVP-BKM120 across a Broad Range of Concentrations

Author

Brachmann, Saskia M., primary, Kleylein-Sohn, Julia, primary, Gaulis, Swann, primary, Kauffmann, Audrey, primary, Blommers, Marcel J.J., primary, Kazic-Legueux, Malika, primary, Laborde, Laurent, primary, Hattenberger, Marc, primary, Stauffer, Fabian, primary, Vaxelaire, Juliane, primary, Romanet, Vincent, primary, Henry, Chrystèle, primary, Murakami, Masato, primary, Guthy, Daniel Alexander, primary, Sterker, Dario, primary, Bergling, Sebastian, primary, Wilson, Christopher, primary, Brümmendorf, Thomas, primary, Fritsch, Christine, primary, Garcia-Echeverria, Carlos, primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Maira, Sauveur-Michel, primary

Published
2023
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36. Supplementary Figure 2 from Characterization of the Mechanism of Action of the Pan Class I PI3K Inhibitor NVP-BKM120 across a Broad Range of Concentrations

Author

Brachmann, Saskia M., primary, Kleylein-Sohn, Julia, primary, Gaulis, Swann, primary, Kauffmann, Audrey, primary, Blommers, Marcel J.J., primary, Kazic-Legueux, Malika, primary, Laborde, Laurent, primary, Hattenberger, Marc, primary, Stauffer, Fabian, primary, Vaxelaire, Juliane, primary, Romanet, Vincent, primary, Henry, Chrystèle, primary, Murakami, Masato, primary, Guthy, Daniel Alexander, primary, Sterker, Dario, primary, Bergling, Sebastian, primary, Wilson, Christopher, primary, Brümmendorf, Thomas, primary, Fritsch, Christine, primary, Garcia-Echeverria, Carlos, primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Maira, Sauveur-Michel, primary

Published
2023
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37. Supplementary Table S2 from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

Author

Andraos, Rita, primary, Qian, Zhiyan, primary, Bonenfant, Débora, primary, Rubert, Joëlle, primary, Vangrevelinghe, Eric, primary, Scheufler, Clemens, primary, Marque, Fanny, primary, Régnier, Catherine H., primary, De Pover, Alain, primary, Ryckelynck, Hugues, primary, Bhagwat, Neha, primary, Koppikar, Priya, primary, Goel, Aviva, primary, Wyder, Lorenza, primary, Tavares, Gisele, primary, Baffert, Fabienne, primary, Pissot-Soldermann, Carole, primary, Manley, Paul W., primary, Gaul, Christoph, primary, Voshol, Hans, primary, Levine, Ross L., primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Radimerski, Thomas, primary

Published
2023
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38. Data from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

Author

Andraos, Rita, primary, Qian, Zhiyan, primary, Bonenfant, Débora, primary, Rubert, Joëlle, primary, Vangrevelinghe, Eric, primary, Scheufler, Clemens, primary, Marque, Fanny, primary, Régnier, Catherine H., primary, De Pover, Alain, primary, Ryckelynck, Hugues, primary, Bhagwat, Neha, primary, Koppikar, Priya, primary, Goel, Aviva, primary, Wyder, Lorenza, primary, Tavares, Gisele, primary, Baffert, Fabienne, primary, Pissot-Soldermann, Carole, primary, Manley, Paul W., primary, Gaul, Christoph, primary, Voshol, Hans, primary, Levine, Ross L., primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Radimerski, Thomas, primary

Published
2023
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39. 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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40. Supplementary Figure 2 from Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials

Author

Fritsch, Christine, primary, Huang, Alan, primary, Chatenay-Rivauday, Christian, primary, Schnell, Christian, primary, Reddy, Anupama, primary, Liu, Manway, primary, Kauffmann, Audrey, primary, Guthy, Daniel, primary, Erdmann, Dirk, primary, De Pover, Alain, primary, Furet, Pascal, primary, Gao, Hui, primary, Ferretti, Stephane, primary, Wang, Youzhen, primary, Trappe, Joerg, primary, Brachmann, Saskia M., primary, Maira, Sauveur-Michel, primary, Wilson, Christopher, primary, Boehm, Markus, primary, Garcia-Echeverria, Carlos, primary, Chene, Patrick, primary, Wiesmann, Marion, primary, Cozens, Robert, primary, Lehar, Joseph, primary, Schlegel, Robert, primary, Caravatti, Giorgio, primary, Hofmann, Francesco, primary, and Sellers, William R., primary

Published
2023
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41. Supplementary Figures, Methods, and References from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

Author

Andraos, Rita, primary, Qian, Zhiyan, primary, Bonenfant, Débora, primary, Rubert, Joëlle, primary, Vangrevelinghe, Eric, primary, Scheufler, Clemens, primary, Marque, Fanny, primary, Régnier, Catherine H., primary, De Pover, Alain, primary, Ryckelynck, Hugues, primary, Bhagwat, Neha, primary, Koppikar, Priya, primary, Goel, Aviva, primary, Wyder, Lorenza, primary, Tavares, Gisele, primary, Baffert, Fabienne, primary, Pissot-Soldermann, Carole, primary, Manley, Paul W., primary, Gaul, Christoph, primary, Voshol, Hans, primary, Levine, Ross L., primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Radimerski, Thomas, primary

Published
2023
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42. Supplementary Figure 3 from Characterization of the Mechanism of Action of the Pan Class I PI3K Inhibitor NVP-BKM120 across a Broad Range of Concentrations

Author

Brachmann, Saskia M., primary, Kleylein-Sohn, Julia, primary, Gaulis, Swann, primary, Kauffmann, Audrey, primary, Blommers, Marcel J.J., primary, Kazic-Legueux, Malika, primary, Laborde, Laurent, primary, Hattenberger, Marc, primary, Stauffer, Fabian, primary, Vaxelaire, Juliane, primary, Romanet, Vincent, primary, Henry, Chrystèle, primary, Murakami, Masato, primary, Guthy, Daniel Alexander, primary, Sterker, Dario, primary, Bergling, Sebastian, primary, Wilson, Christopher, primary, Brümmendorf, Thomas, primary, Fritsch, Christine, primary, Garcia-Echeverria, Carlos, primary, Sellers, William R., primary, Hofmann, Francesco, primary, and Maira, Sauveur-Michel, primary

Published
2023
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43. Supplementary Figure 7 from Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor

Author

Maira, Sauveur-Michel, primary, Pecchi, Sabina, primary, Huang, Alan, primary, Burger, Matthew, primary, Knapp, Mark, primary, Sterker, Dario, primary, Schnell, Christian, primary, Guthy, Daniel, primary, Nagel, Tobi, primary, Wiesmann, Marion, primary, Brachmann, Saskia, primary, Fritsch, Christine, primary, Dorsch, Marion, primary, Chène, Patrick, primary, Shoemaker, Kevin, primary, De Pover, Alain, primary, Menezes, Daniel, primary, Martiny-Baron, Georg, primary, Fabbro, Doriano, primary, Wilson, Christopher J., primary, Schlegel, Robert, primary, Hofmann, Francesco, primary, García-Echeverría, Carlos, primary, Sellers, William R., primary, and Voliva, Charles F., primary

Published
2023
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44. Supplementary Figure 3 from Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials

Author

Fritsch, Christine, primary, Huang, Alan, primary, Chatenay-Rivauday, Christian, primary, Schnell, Christian, primary, Reddy, Anupama, primary, Liu, Manway, primary, Kauffmann, Audrey, primary, Guthy, Daniel, primary, Erdmann, Dirk, primary, De Pover, Alain, primary, Furet, Pascal, primary, Gao, Hui, primary, Ferretti, Stephane, primary, Wang, Youzhen, primary, Trappe, Joerg, primary, Brachmann, Saskia M., primary, Maira, Sauveur-Michel, primary, Wilson, Christopher, primary, Boehm, Markus, primary, Garcia-Echeverria, Carlos, primary, Chene, Patrick, primary, Wiesmann, Marion, primary, Cozens, Robert, primary, Lehar, Joseph, primary, Schlegel, Robert, primary, Caravatti, Giorgio, primary, Hofmann, Francesco, primary, and Sellers, William R., primary

Published
2023
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45. Supplementary Figure Legends, Supplementary Table Legends, and Supplementary Tables 1 through 7 from Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials

Author

Fritsch, Christine, primary, Huang, Alan, primary, Chatenay-Rivauday, Christian, primary, Schnell, Christian, primary, Reddy, Anupama, primary, Liu, Manway, primary, Kauffmann, Audrey, primary, Guthy, Daniel, primary, Erdmann, Dirk, primary, De Pover, Alain, primary, Furet, Pascal, primary, Gao, Hui, primary, Ferretti, Stephane, primary, Wang, Youzhen, primary, Trappe, Joerg, primary, Brachmann, Saskia M., primary, Maira, Sauveur-Michel, primary, Wilson, Christopher, primary, Boehm, Markus, primary, Garcia-Echeverria, Carlos, primary, Chene, Patrick, primary, Wiesmann, Marion, primary, Cozens, Robert, primary, Lehar, Joseph, primary, Schlegel, Robert, primary, Caravatti, Giorgio, primary, Hofmann, Francesco, primary, and Sellers, William R., primary

Published
2023
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46. Supplementary Figure Legends from Discovery and Optimization of HKT288, a Cadherin-6–Targeting ADC for the Treatment of Ovarian and Renal Cancers

Author

Bialucha, Carl U., primary, Collins, Scott D., primary, Li, Xiao, primary, Saxena, Parmita, primary, Zhang, Xiamei, primary, Dürr, Clemens, primary, Lafont, Bruno, primary, Prieur, Pierric, primary, Shim, Yeonju, primary, Mosher, Rebecca, primary, Lee, David, primary, Ostrom, Lance, primary, Hu, Tiancen, primary, Bilic, Sanela, primary, Rajlic, Ivana Liric, primary, Capka, Vladimir, primary, Jiang, Wei, primary, Wagner, Joel P., primary, Elliott, GiNell, primary, Veloso, Artur, primary, Piel, Jessica C., primary, Flaherty, Meghan M., primary, Mansfield, Keith G., primary, Meseck, Emily K., primary, Rubic-Schneider, Tina, primary, London, Anne Serdakowski, primary, Tschantz, William R., primary, Kurz, Markus, primary, Nguyen, Duc, primary, Bourret, Aaron, primary, Meyer, Matthew J., primary, Faris, Jason E., primary, Janatpour, Mary J., primary, Chan, Vivien W., primary, Yoder, Nicholas C., primary, Catcott, Kalli C., primary, McShea, Molly A., primary, Sun, Xiuxia, primary, Gao, Hui, primary, Williams, Juliet, primary, Hofmann, Francesco, primary, Engelman, Jeffrey A., primary, Ettenberg, Seth A., primary, Sellers, William R., primary, and Lees, Emma, primary

Published
2023
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48. Supplementary Table 5 from FGFR Genetic Alterations Predict for Sensitivity to NVP-BGJ398, a Selective Pan-FGFR Inhibitor

Author

Guagnano, Vito, primary, Kauffmann, Audrey, primary, Wöhrle, Simon, primary, Stamm, Christelle, primary, Ito, Moriko, primary, Barys, Louise, primary, Pornon, Astrid, primary, Yao, Yao, primary, Li, Fang, primary, Zhang, Yun, primary, Chen, Zhi, primary, Wilson, Christopher J., primary, Bordas, Vincent, primary, Le Douget, Mickaël, primary, Gaither, L. Alex, primary, Borawski, Jason, primary, Monahan, John E., primary, Venkatesan, Kavitha, primary, Brümmendorf, Thomas, primary, Thomas, David M., primary, Garcia-Echeverria, Carlos, primary, Hofmann, Francesco, primary, Sellers, William R., primary, and Graus-Porta, Diana, primary

Published
2023
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49. Supplementary Figure 3 from Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor

Author

Maira, Sauveur-Michel, primary, Pecchi, Sabina, primary, Huang, Alan, primary, Burger, Matthew, primary, Knapp, Mark, primary, Sterker, Dario, primary, Schnell, Christian, primary, Guthy, Daniel, primary, Nagel, Tobi, primary, Wiesmann, Marion, primary, Brachmann, Saskia, primary, Fritsch, Christine, primary, Dorsch, Marion, primary, Chène, Patrick, primary, Shoemaker, Kevin, primary, De Pover, Alain, primary, Menezes, Daniel, primary, Martiny-Baron, Georg, primary, Fabbro, Doriano, primary, Wilson, Christopher J., primary, Schlegel, Robert, primary, Hofmann, Francesco, primary, García-Echeverría, Carlos, primary, Sellers, William R., primary, and Voliva, Charles F., primary

Published
2023
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50. 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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