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2. Vorasidenib and ivosidenib in IDH1-mutant low-grade glioma: a randomized, perioperative phase 1 trial

Author

Mellinghoff, Ingo K, Lu, Min, Wen, Patrick Y, Taylor, Jennie W, Maher, Elizabeth A, Arrillaga-Romany, Isabel, Peters, Katherine B, Ellingson, Benjamin M, Rosenblum, Marc K, Chun, Saewon, Le, Kha, Tassinari, Ania, Choe, Sung, Toubouti, Youssef, Schoenfeld, Steven, Pandya, Shuchi S, Hassan, Islam, Steelman, Lori, Clarke, Jennifer L, and Cloughesy, Timothy F

Subjects
Biomedical and Clinical Sciences, Clinical Sciences, Oncology and Carcinogenesis, Clinical Trials and Supportive Activities, Brain Cancer, Orphan Drug, Rare Diseases, Clinical Research, Genetics, Cancer, Brain Disorders, Neurosciences, 6.1 Pharmaceuticals, Evaluation of treatments and therapeutic interventions, 5.1 Pharmaceuticals, Development of treatments and therapeutic interventions, Humans, Pyridines, Isocitrate Dehydrogenase, Glioma, Mutation, Pharmaceutical Preparations, Brain Neoplasms, Medical and Health Sciences, Immunology, Biomedical and clinical sciences, Health sciences
Abstract

Vorasidenib and ivosidenib inhibit mutant forms of isocitrate dehydrogenase (mIDH) and have shown preliminary clinical activity against mIDH glioma. We evaluated both agents in a perioperative phase 1 trial to explore the mechanism of action in recurrent low-grade glioma (IGG) and select a molecule for phase 3 testing. Primary end-point was concentration of D-2-hydroxyglutarate (2-HG), the metabolic product of mIDH enzymes, measured in tumor tissue from 49 patients with mIDH1-R132H nonenhancing gliomas following randomized treatment with vorasidenib (50 mg or 10 mg once daily, q.d.), ivosidenib (500 mg q.d. or 250 mg twice daily) or no treatment before surgery. Tumor 2-HG concentrations were reduced by 92.6% (95% credible interval (CrI), 76.1-97.6) and 91.1% (95% CrI, 72.0-97.0) in patients treated with vorasidenib 50 mg q.d. and ivosidenib 500 mg q.d., respectively. Both agents were well tolerated and follow-up is ongoing. In exploratory analyses, 2-HG reduction was associated with increased DNA 5-hydroxymethylcytosine, reversal of 'proneural' and 'stemness' gene expression signatures, decreased tumor cell proliferation and immune cell activation. Vorasidenib, which showed brain penetrance and more consistent 2-HG suppression than ivosidenib, was advanced to phase 3 testing in patients with mIDH LGGs. Funded by Agios Pharmaceuticals, Inc. and Servier Pharmaceuticals LLC; ClinicalTrials.gov number NCT03343197.

Published
2023

3. Author Correction: Vorasidenib and ivosidenib in IDH1-mutant low-grade glioma: a randomized, perioperative phase 1 trial

Author

Mellinghoff, Ingo K., Lu, Min, Wen, Patrick Y., Taylor, Jennie W., Maher, Elizabeth A., Arrillaga-Romany, Isabel, Peters, Katherine B., Ellingson, Benjamin M., Rosenblum, Marc K., Chun, Saewon, Le, Kha, Tassinari, Ania, Choe, Sung, Toubouti, Youssef, Schoenfeld, Steven, Pandya, Shuchi S., Hassan, Islam, Steelman, Lori, Clarke, Jennifer L., and Cloughesy, Timothy F.

Published
2024
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4. Vorasidenib, a Dual Inhibitor of Mutant IDH1/2, in Recurrent or Progressive Glioma; Results of a First-in-Human Phase I TrialVorasidenib in Recurrent or Progressive Glioma

Author

Mellinghoff, Ingo K, Penas-Prado, Marta, Peters, Katherine B, Burris, Howard A, Maher, Elizabeth A, Janku, Filip, Cote, Gregory M, de la Fuente, Macarena I, Clarke, Jennifer L, Ellingson, Benjamin M, Chun, Saewon, Young, Robert J, Liu, Hua, Choe, Sung, Lu, Min, Le, Kha, Hassan, Islam, Steelman, Lori, Pandya, Shuchi S, Cloughesy, Timothy F, and Wen, Patrick Y

Subjects
Neurosciences, Orphan Drug, Cancer, Brain Cancer, Brain Disorders, Clinical Research, Clinical Trials and Supportive Activities, Rare Diseases, Evaluation of treatments and therapeutic interventions, 6.1 Pharmaceuticals, Adolescent, Adult, Aged, Brain Neoplasms, Diamines, Disease Progression, Female, Glioma, Humans, Isocitrate Dehydrogenase, Male, Middle Aged, Mutation, Neoplasm Recurrence, Local, Pyridines, Young Adult, Oncology and Carcinogenesis, Oncology & Carcinogenesis
Abstract

PurposeLower grade gliomas (LGGs) are malignant brain tumors. Current therapy is associated with short- and long-term toxicity. Progression to higher tumor grade is associated with contrast enhancement on MRI. The majority of LGGs harbor mutations in the genes encoding isocitrate dehydrogenase 1 or 2 (IDH1/IDH2). Vorasidenib (AG-881) is a first-in-class, brain-penetrant, dual inhibitor of the mutant IDH1 and mutant IDH2 enzymes.Patients and methodsWe conducted a multicenter, open-label, phase I, dose-escalation study of vorasidenib in 93 patients with mutant IDH1/2 (mIDH1/2) solid tumors, including 52 patients with glioma that had recurred or progressed following standard therapy. Vorasidenib was administered orally, once daily, in 28-day cycles until progression or unacceptable toxicity. Enrollment is complete; this trial is registered with ClinicalTrials.gov, NCT02481154.ResultsVorasidenib showed a favorable safety profile in the glioma cohort. Dose-limiting toxicities of elevated transaminases occurred at doses ≥100 mg and were reversible. The protocol-defined objective response rate per Response Assessment in Neuro-Oncology criteria for LGG in patients with nonenhancing glioma was 18% (one partial response, three minor responses). The median progression-free survival was 36.8 months [95% confidence interval (CI), 11.2-40.8] for patients with nonenhancing glioma and 3.6 months (95% CI, 1.8-6.5) for patients with enhancing glioma. Exploratory evaluation of tumor volumes in patients with nonenhancing glioma showed sustained tumor shrinkage in multiple patients.ConclusionsVorasidenib was well tolerated and showed preliminary antitumor activity in patients with recurrent or progressive nonenhancing mIDH LGG.

Published
2021

5. Ivosidenib in Isocitrate Dehydrogenase 1–Mutated Advanced Glioma

Author

Mellinghoff, Ingo K, Ellingson, Benjamin M, Touat, Mehdi, Maher, Elizabeth, De La Fuente, Macarena I, Holdhoff, Matthias, Cote, Gregory M, Burris, Howard, Janku, Filip, Young, Robert J, Huang, Raymond, Jiang, Liewen, Choe, Sung, Fan, Bin, Yen, Katharine, Lu, Min, Bowden, Chris, Steelman, Lori, Pandya, Shuchi S, Cloughesy, Timothy F, and Wen, Patrick Y

Subjects
Brain Cancer, Neurosciences, Clinical Trials and Supportive Activities, Clinical Research, Cancer, Genetics, Rare Diseases, Orphan Drug, Brain Disorders, Evaluation of treatments and therapeutic interventions, 6.1 Pharmaceuticals, Adult, Aged, Antineoplastic Agents, Brain Neoplasms, Dose-Response Relationship, Drug, Enzyme Inhibitors, Female, Glioma, Glycine, Humans, Isocitrate Dehydrogenase, Male, Middle Aged, Mutation, Pyridines, Young Adult, Clinical Sciences, Oncology and Carcinogenesis, Oncology & Carcinogenesis
Abstract

PurposeDiffuse gliomas are malignant brain tumors that include lower-grade gliomas (LGGs) and glioblastomas. Transformation of low-grade glioma into a higher tumor grade is typically associated with contrast enhancement on magnetic resonance imaging. Mutations in the isocitrate dehydrogenase 1 (IDH1) gene occur in most LGGs (> 70%). Ivosidenib is an inhibitor of mutant IDH1 (mIDH1) under evaluation in patients with solid tumors.MethodsWe conducted a multicenter, open-label, phase I, dose escalation and expansion study of ivosidenib in patients with mIDH1 solid tumors. Ivosidenib was administered orally daily in 28-day cycles.ResultsIn 66 patients with advanced gliomas, ivosidenib was well tolerated, with no dose-limiting toxicities reported. The maximum tolerated dose was not reached; 500 mg once per day was selected for the expansion cohort. The grade ≥ 3 adverse event rate was 19.7%; 3% (n = 2) were considered treatment related. In patients with nonenhancing glioma (n = 35), the objective response rate was 2.9%, with 1 partial response. Thirty of 35 patients (85.7%) with nonenhancing glioma achieved stable disease compared with 14 of 31 (45.2%) with enhancing glioma. Median progression-free survival was 13.6 months (95% CI, 9.2 to 33.2 months) and 1.4 months (95% CI, 1.0 to 1.9 months) for the nonenhancing and enhancing glioma cohorts, respectively. In an exploratory analysis, ivosidenib reduced the volume and growth rates of nonenhancing tumors.ConclusionIn patients with mIDH1 advanced glioma, ivosidenib 500 mg once per day was associated with a favorable safety profile, prolonged disease control, and reduced growth of nonenhancing tumors.

Published
2020

15. Molecular mechanisms mediating relapse following ivosidenib monotherapy in IDH1-mutant relapsed or refractory AML

Author

Choe, Sung, Wang, Hongfang, DiNardo, Courtney D., Stein, Eytan M., de Botton, Stéphane, Roboz, Gail J., Altman, Jessica K., Mims, Alice S., Watts, Justin M., Pollyea, Daniel A., Fathi, Amir T., Tallman, Martin S., Kantarjian, Hagop M., Stone, Richard M., Quek, Lynn, Konteatis, Zenon, Dang, Lenny, Nicolay, Brandon, Nejad, Parham, Liu, Guowen, Zhang, Vickie, Liu, Hua, Goldwasser, Meredith, Liu, Wei, Marks, Kevin, Bowden, Chris, Biller, Scott A., Attar, Eyal C., and Wu, Bin

Published
2020
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16. CTNI-51. A RANDOMIZED DOUBLE-BLIND PHASE 3 STUDY OF VORASIDENIB VS PLACEBO IN PATIENTS WITH MUTANT IDH1/2 DIFFUSE GLIOMA (INDIGO): EXPLORATORY ANALYSIS OF VARIANT ALLELE FREQUENCY AND PROGRESSION-FREE SURVIVAL

Author

Cloughesy, Timothy, primary, Mellinghoff, Ingo, additional, van den Bent, Martin, additional, Blumenthal, Deborah, additional, Touat, Mehdi, additional, Peters, Katherine, additional, Clarke, Jennifer, additional, Mendez, Joe, additional, Yust-Katz, Shlomit, additional, Mason, Warren, additional, Ducray, Francois, additional, Umemura, Yoshie, additional, Nabors, L Burt, additional, Holdhoff, Matthias, additional, Hottinger, Andreas, additional, Arakawa, Yoshiki, additional, Sepúlveda, Juan, additional, Wick, Wolfgang, additional, Soffietti, Riccardo, additional, Perry, James, additional, Giglio, Pierre, additional, de la Fuente, Macarena, additional, Maher, Elizabeth, additional, Choe, Sung, additional, Zhao, Dan, additional, Pandya, Shuchi, additional, Steelman, Lori, additional, Hassan, Islam, additional, Tron, Adriana, additional, and Wen, Patrick, additional

Published
2023
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18. Safety and activity of ivosidenib in patients with IDH1-mutant advanced cholangiocarcinoma: a phase 1 study

Author

Lowery, Maeve A, Burris, Howard A, III, Janku, Filip, Shroff, Rachna T, Cleary, James M, Azad, Nilofer S, Goyal, Lipika, Maher, Elizabeth A, Gore, Lia, Hollebecque, Antoine, Beeram, Muralidhar, Trent, Jonathan C, Jiang, Liewen, Fan, Bin, Aguado-Fraile, Elia, Choe, Sung, Wu, Bin, Gliser, Camelia, Agresta, Samuel V, Pandya, Shuchi S, Zhu, Andrew X, and Abou-Alfa, Ghassan K

Published
2019
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19. D-2-hydroxyglutarate produced by mutant IDH2 causes cardiomyopathy and neurodegeneration in mice.

Author

Akbay, Esra, Moslehi, Javid, Christensen, Camilla, Saha, Supriya, Tchaicha, Jeremy, Ramkissoon, Shakti, Stewart, Kelly, Carretero, Julian, Kikuchi, Eiki, Zhang, Haikuo, Cohoon, Travis, Murray, Stuart, Liu, Wei, Uno, Kazumasa, Fisch, Sudeshna, Jones, Kristen, Gurumurthy, Sushma, Gliser, Camelia, Choe, Sung, Keenan, Marie, Son, Jaekyoung, Stanley, Illana, Losman, Julie, Padera, Robert, Bronson, Roderick, Asara, John, Abdel-Wahab, Omar, Amrein, Philip, Fathi, Amir, Danial, Nika, Kimmelman, Alec, Kung, Andrew, Ligon, Keith, Yen, Katharine, Kaelin, William, Bardeesy, Nabeel, and Wong, Kwok-Kin

Subjects
D-2HG, D2HGA, IDH2, cardiomyopathy, glycogen, myopathy, vacuolar leukoencephalopathy, Animals, Cardiomyopathies, Cell Line, Gene Expression Profiling, Gene Expression Regulation, Developmental, Glutarates, Heart, Humans, Isocitrate Dehydrogenase, Mice, Mice, Inbred BALB C, Mice, Nude, Mutation, Neurodegenerative Diseases
Abstract

Mutations in isocitrate dehydrogenase 1 and 2 (IDH1/2) have been discovered in several cancer types and cause the neurometabolic syndrome D2-hydroxyglutaric aciduria (D2HGA). The mutant enzymes exhibit neomorphic activity resulting in production of D2-hydroxyglutaric acid (D-2HG). To study the pathophysiological consequences of the accumulation of D-2HG, we generated transgenic mice with conditionally activated IDH2(R140Q) and IDH2(R172K) alleles. Global induction of mutant IDH2 expression in adults resulted in dilated cardiomyopathy, white matter abnormalities throughout the central nervous system (CNS), and muscular dystrophy. Embryonic activation of mutant IDH2 resulted in more pronounced phenotypes, including runting, hydrocephalus, and shortened life span, recapitulating the abnormalities observed in D2HGA patients. The diseased hearts exhibited mitochondrial damage and glycogen accumulation with a concordant up-regulation of genes involved in glycogen biosynthesis. Notably, mild cardiac hypertrophy was also observed in nude mice implanted with IDH2(R140Q)-expressing xenografts, suggesting that 2HG may potentially act in a paracrine fashion. Finally, we show that silencing of IDH2(R140Q) in mice with an inducible transgene restores heart function by lowering 2HG levels. Together, these findings indicate that inhibitors of mutant IDH2 may be beneficial in the treatment of D2HGA and suggest that 2HG produced by IDH mutant tumors has the potential to provoke a paraneoplastic condition.

Published
2014

20. Data from Vorasidenib, a Dual Inhibitor of Mutant IDH1/2, in Recurrent or Progressive Glioma; Results of a First-in-Human Phase I Trial

Author

Mellinghoff, Ingo K., primary, Penas-Prado, Marta, primary, Peters, Katherine B., primary, Burris, Howard A., primary, Maher, Elizabeth A., primary, Janku, Filip, primary, Cote, Gregory M., primary, de la Fuente, Macarena I., primary, Clarke, Jennifer L., primary, Ellingson, Benjamin M., primary, Chun, Saewon, primary, Young, Robert J., primary, Liu, Hua, primary, Choe, Sung, primary, Lu, Min, primary, Le, Kha, primary, Hassan, Islam, primary, Steelman, Lori, primary, Pandya, Shuchi S., primary, Cloughesy, Timothy F., primary, and Wen, Patrick Y., primary

Published
2023
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21. Supplementary Data from Vorasidenib, a Dual Inhibitor of Mutant IDH1/2, in Recurrent or Progressive Glioma; Results of a First-in-Human Phase I Trial

Author

Mellinghoff, Ingo K., primary, Penas-Prado, Marta, primary, Peters, Katherine B., primary, Burris, Howard A., primary, Maher, Elizabeth A., primary, Janku, Filip, primary, Cote, Gregory M., primary, de la Fuente, Macarena I., primary, Clarke, Jennifer L., primary, Ellingson, Benjamin M., primary, Chun, Saewon, primary, Young, Robert J., primary, Liu, Hua, primary, Choe, Sung, primary, Lu, Min, primary, Le, Kha, primary, Hassan, Islam, primary, Steelman, Lori, primary, Pandya, Shuchi S., primary, Cloughesy, Timothy F., primary, and Wen, Patrick Y., primary

Published
2023
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23. Data from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Author

Yen, Katharine, primary, Travins, Jeremy, primary, Wang, Fang, primary, David, Muriel D., primary, Artin, Erin, primary, Straley, Kimberly, primary, Padyana, Anil, primary, Gross, Stefan, primary, DeLaBarre, Byron, primary, Tobin, Erica, primary, Chen, Yue, primary, Nagaraja, Raj, primary, Choe, Sung, primary, Jin, Lei, primary, Konteatis, Zenon, primary, Cianchetta, Giovanni, primary, Saunders, Jeffrey O., primary, Salituro, Francesco G., primary, Quivoron, Cyril, primary, Opolon, Paule, primary, Bawa, Olivia, primary, Saada, Véronique, primary, Paci, Angelo, primary, Broutin, Sophie, primary, Bernard, Olivier A., primary, de Botton, Stéphane, primary, Marteyn, Benoît S., primary, Pilichowska, Monika, primary, Xu, YingXia, primary, Fang, Cheng, primary, Jiang, Fan, primary, Wei, Wentao, primary, Jin, Shengfang, primary, Silverman, Lee, primary, Liu, Wei, primary, Yang, Hua, primary, Dang, Lenny, primary, Dorsch, Marion, primary, Penard-Lacronique, Virginie, primary, Biller, Scott A., primary, and Su, Shin-San Michael, primary

Published
2023
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24. Supplementary Tables 1 - 8 from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Author

Yen, Katharine, primary, Travins, Jeremy, primary, Wang, Fang, primary, David, Muriel D., primary, Artin, Erin, primary, Straley, Kimberly, primary, Padyana, Anil, primary, Gross, Stefan, primary, DeLaBarre, Byron, primary, Tobin, Erica, primary, Chen, Yue, primary, Nagaraja, Raj, primary, Choe, Sung, primary, Jin, Lei, primary, Konteatis, Zenon, primary, Cianchetta, Giovanni, primary, Saunders, Jeffrey O., primary, Salituro, Francesco G., primary, Quivoron, Cyril, primary, Opolon, Paule, primary, Bawa, Olivia, primary, Saada, Véronique, primary, Paci, Angelo, primary, Broutin, Sophie, primary, Bernard, Olivier A., primary, de Botton, Stéphane, primary, Marteyn, Benoît S., primary, Pilichowska, Monika, primary, Xu, YingXia, primary, Fang, Cheng, primary, Jiang, Fan, primary, Wei, Wentao, primary, Jin, Shengfang, primary, Silverman, Lee, primary, Liu, Wei, primary, Yang, Hua, primary, Dang, Lenny, primary, Dorsch, Marion, primary, Penard-Lacronique, Virginie, primary, Biller, Scott A., primary, and Su, Shin-San Michael, primary

Published
2023
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25. Supplementary Table S1.4 from Metabolic and Functional Genomic Studies Identify Deoxythymidylate Kinase as a Target in LKB1-Mutant Lung Cancer

Author

Liu, Yan, primary, Marks, Kevin, primary, Cowley, Glenn S., primary, Carretero, Julian, primary, Liu, Qingsong, primary, Nieland, Thomas J.F., primary, Xu, Chunxiao, primary, Cohoon, Travis J., primary, Gao, Peng, primary, Zhang, Yong, primary, Chen, Zhao, primary, Altabef, Abigail B., primary, Tchaicha, Jeremy H., primary, Wang, Xiaoxu, primary, Choe, Sung, primary, Driggers, Edward M., primary, Zhang, Jianming, primary, Bailey, Sean T., primary, Sharpless, Norman E., primary, Hayes, D. Neil, primary, Patel, Nirali M., primary, Janne, Pasi A., primary, Bardeesy, Nabeel, primary, Engelman, Jeffrey A., primary, Manning, Brendan D., primary, Shaw, Reuben J., primary, Asara, John M., primary, Scully, Ralph, primary, Kimmelman, Alec, primary, Byers, Lauren A., primary, Gibbons, Don L., primary, Wistuba, Ignacio I., primary, Heymach, John V., primary, Kwiatkowski, David J., primary, Kim, William Y., primary, Kung, Andrew L., primary, Gray, Nathanael S., primary, Root, David E., primary, Cantley, Lewis C., primary, and Wong, Kwok-Kin, primary

Published
2023
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26. Supplementary Data Table S3 from Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase

Author

McDonald, Gabrielle, primary, Chubukov, Victor, primary, Coco, John, primary, Truskowski, Kevin, primary, Narayanaswamy, Rohini, primary, Choe, Sung, primary, Steadman, Mya, primary, Artin, Erin, primary, Padyana, Anil K., primary, Jin, Lei, primary, Ronseaux, Sebastien, primary, Locuson, Charles, primary, Fan, Zi-Peng, primary, Erdmann, Tabea, primary, Mann, Alan, primary, Hayes, Sebastian, primary, Fletcher, Mark, primary, Nellore, Kavitha, primary, Rao, Siva Sanjeeva, primary, Subramanya, Hosahalli, primary, Reddy, K. Satish, primary, Panigrahi, Sunil K., primary, Antony, Thomas, primary, Gopinath, Sreevalsam, primary, Sui, Zhihua, primary, Nagaraja, Nelamangala, primary, Dang, Lenny, primary, Lenz, Georg, primary, Hurov, Jonathan, primary, Biller, Scott A., primary, Murtie, Josh, primary, Marks, Kevin M., primary, and Ulanet, Danielle B., primary

Published
2023
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27. Data from Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase

Author

McDonald, Gabrielle, primary, Chubukov, Victor, primary, Coco, John, primary, Truskowski, Kevin, primary, Narayanaswamy, Rohini, primary, Choe, Sung, primary, Steadman, Mya, primary, Artin, Erin, primary, Padyana, Anil K., primary, Jin, Lei, primary, Ronseaux, Sebastien, primary, Locuson, Charles, primary, Fan, Zi-Peng, primary, Erdmann, Tabea, primary, Mann, Alan, primary, Hayes, Sebastian, primary, Fletcher, Mark, primary, Nellore, Kavitha, primary, Rao, Siva Sanjeeva, primary, Subramanya, Hosahalli, primary, Reddy, K. Satish, primary, Panigrahi, Sunil K., primary, Antony, Thomas, primary, Gopinath, Sreevalsam, primary, Sui, Zhihua, primary, Nagaraja, Nelamangala, primary, Dang, Lenny, primary, Lenz, Georg, primary, Hurov, Jonathan, primary, Biller, Scott A., primary, Murtie, Josh, primary, Marks, Kevin M., primary, and Ulanet, Danielle B., primary

Published
2023
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28. Supplementary Methods from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Author

Yen, Katharine, primary, Travins, Jeremy, primary, Wang, Fang, primary, David, Muriel D., primary, Artin, Erin, primary, Straley, Kimberly, primary, Padyana, Anil, primary, Gross, Stefan, primary, DeLaBarre, Byron, primary, Tobin, Erica, primary, Chen, Yue, primary, Nagaraja, Raj, primary, Choe, Sung, primary, Jin, Lei, primary, Konteatis, Zenon, primary, Cianchetta, Giovanni, primary, Saunders, Jeffrey O., primary, Salituro, Francesco G., primary, Quivoron, Cyril, primary, Opolon, Paule, primary, Bawa, Olivia, primary, Saada, Véronique, primary, Paci, Angelo, primary, Broutin, Sophie, primary, Bernard, Olivier A., primary, de Botton, Stéphane, primary, Marteyn, Benoît S., primary, Pilichowska, Monika, primary, Xu, YingXia, primary, Fang, Cheng, primary, Jiang, Fan, primary, Wei, Wentao, primary, Jin, Shengfang, primary, Silverman, Lee, primary, Liu, Wei, primary, Yang, Hua, primary, Dang, Lenny, primary, Dorsch, Marion, primary, Penard-Lacronique, Virginie, primary, Biller, Scott A., primary, and Su, Shin-San Michael, primary

Published
2023
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29. Data from Metabolic and Functional Genomic Studies Identify Deoxythymidylate Kinase as a Target in LKB1-Mutant Lung Cancer

Author

Liu, Yan, primary, Marks, Kevin, primary, Cowley, Glenn S., primary, Carretero, Julian, primary, Liu, Qingsong, primary, Nieland, Thomas J.F., primary, Xu, Chunxiao, primary, Cohoon, Travis J., primary, Gao, Peng, primary, Zhang, Yong, primary, Chen, Zhao, primary, Altabef, Abigail B., primary, Tchaicha, Jeremy H., primary, Wang, Xiaoxu, primary, Choe, Sung, primary, Driggers, Edward M., primary, Zhang, Jianming, primary, Bailey, Sean T., primary, Sharpless, Norman E., primary, Hayes, D. Neil, primary, Patel, Nirali M., primary, Janne, Pasi A., primary, Bardeesy, Nabeel, primary, Engelman, Jeffrey A., primary, Manning, Brendan D., primary, Shaw, Reuben J., primary, Asara, John M., primary, Scully, Ralph, primary, Kimmelman, Alec, primary, Byers, Lauren A., primary, Gibbons, Don L., primary, Wistuba, Ignacio I., primary, Heymach, John V., primary, Kwiatkowski, David J., primary, Kim, William Y., primary, Kung, Andrew L., primary, Gray, Nathanael S., primary, Root, David E., primary, Cantley, Lewis C., primary, and Wong, Kwok-Kin, primary

Published
2023
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30. Supplementary Figures from Isoform Switching as a Mechanism of Acquired Resistance to Mutant Isocitrate Dehydrogenase Inhibition

Author

Harding, James J., primary, Lowery, Maeve A., primary, Shih, Alan H., primary, Schvartzman, Juan M., primary, Hou, Shengqi, primary, Famulare, Christopher, primary, Patel, Minal, primary, Roshal, Mikhail, primary, Do, Richard K., primary, Zehir, Ahmet, primary, You, Daoqi, primary, Selcuklu, S. Duygu, primary, Viale, Agnes, primary, Tallman, Martin S., primary, Hyman, David M., primary, Reznik, Ed, primary, Finley, Lydia W.S., primary, Papaemmanuil, Elli, primary, Tosolini, Alessandra, primary, Frattini, Mark G., primary, MacBeth, Kyle J., primary, Liu, Guowen, primary, Fan, Bin, primary, Choe, Sung, primary, Wu, Bin, primary, Janjigian, Yelena Y., primary, Mellinghoff, Ingo K., primary, Diaz, Luis A., primary, Levine, Ross L., primary, Abou-Alfa, Ghassan K., primary, Stein, Eytan M., primary, and Intlekofer, Andrew M., primary

Published
2023
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31. Supplementary Figures S1- S10 from Metabolic and Functional Genomic Studies Identify Deoxythymidylate Kinase as a Target in LKB1-Mutant Lung Cancer

Author

Liu, Yan, primary, Marks, Kevin, primary, Cowley, Glenn S., primary, Carretero, Julian, primary, Liu, Qingsong, primary, Nieland, Thomas J.F., primary, Xu, Chunxiao, primary, Cohoon, Travis J., primary, Gao, Peng, primary, Zhang, Yong, primary, Chen, Zhao, primary, Altabef, Abigail B., primary, Tchaicha, Jeremy H., primary, Wang, Xiaoxu, primary, Choe, Sung, primary, Driggers, Edward M., primary, Zhang, Jianming, primary, Bailey, Sean T., primary, Sharpless, Norman E., primary, Hayes, D. Neil, primary, Patel, Nirali M., primary, Janne, Pasi A., primary, Bardeesy, Nabeel, primary, Engelman, Jeffrey A., primary, Manning, Brendan D., primary, Shaw, Reuben J., primary, Asara, John M., primary, Scully, Ralph, primary, Kimmelman, Alec, primary, Byers, Lauren A., primary, Gibbons, Don L., primary, Wistuba, Ignacio I., primary, Heymach, John V., primary, Kwiatkowski, David J., primary, Kim, William Y., primary, Kung, Andrew L., primary, Gray, Nathanael S., primary, Root, David E., primary, Cantley, Lewis C., primary, and Wong, Kwok-Kin, primary

Published
2023
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32. Supplementary Data from Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase

Author

McDonald, Gabrielle, primary, Chubukov, Victor, primary, Coco, John, primary, Truskowski, Kevin, primary, Narayanaswamy, Rohini, primary, Choe, Sung, primary, Steadman, Mya, primary, Artin, Erin, primary, Padyana, Anil K., primary, Jin, Lei, primary, Ronseaux, Sebastien, primary, Locuson, Charles, primary, Fan, Zi-Peng, primary, Erdmann, Tabea, primary, Mann, Alan, primary, Hayes, Sebastian, primary, Fletcher, Mark, primary, Nellore, Kavitha, primary, Rao, Siva Sanjeeva, primary, Subramanya, Hosahalli, primary, Reddy, K. Satish, primary, Panigrahi, Sunil K., primary, Antony, Thomas, primary, Gopinath, Sreevalsam, primary, Sui, Zhihua, primary, Nagaraja, Nelamangala, primary, Dang, Lenny, primary, Lenz, Georg, primary, Hurov, Jonathan, primary, Biller, Scott A., primary, Murtie, Josh, primary, Marks, Kevin M., primary, and Ulanet, Danielle B., primary

Published
2023
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33. Supplementary Figures 1 - 11 from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Author

Yen, Katharine, primary, Travins, Jeremy, primary, Wang, Fang, primary, David, Muriel D., primary, Artin, Erin, primary, Straley, Kimberly, primary, Padyana, Anil, primary, Gross, Stefan, primary, DeLaBarre, Byron, primary, Tobin, Erica, primary, Chen, Yue, primary, Nagaraja, Raj, primary, Choe, Sung, primary, Jin, Lei, primary, Konteatis, Zenon, primary, Cianchetta, Giovanni, primary, Saunders, Jeffrey O., primary, Salituro, Francesco G., primary, Quivoron, Cyril, primary, Opolon, Paule, primary, Bawa, Olivia, primary, Saada, Véronique, primary, Paci, Angelo, primary, Broutin, Sophie, primary, Bernard, Olivier A., primary, de Botton, Stéphane, primary, Marteyn, Benoît S., primary, Pilichowska, Monika, primary, Xu, YingXia, primary, Fang, Cheng, primary, Jiang, Fan, primary, Wei, Wentao, primary, Jin, Shengfang, primary, Silverman, Lee, primary, Liu, Wei, primary, Yang, Hua, primary, Dang, Lenny, primary, Dorsch, Marion, primary, Penard-Lacronique, Virginie, primary, Biller, Scott A., primary, and Su, Shin-San Michael, primary

Published
2023
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34. Supplementary Methods from Isoform Switching as a Mechanism of Acquired Resistance to Mutant Isocitrate Dehydrogenase Inhibition

Author

Harding, James J., primary, Lowery, Maeve A., primary, Shih, Alan H., primary, Schvartzman, Juan M., primary, Hou, Shengqi, primary, Famulare, Christopher, primary, Patel, Minal, primary, Roshal, Mikhail, primary, Do, Richard K., primary, Zehir, Ahmet, primary, You, Daoqi, primary, Selcuklu, S. Duygu, primary, Viale, Agnes, primary, Tallman, Martin S., primary, Hyman, David M., primary, Reznik, Ed, primary, Finley, Lydia W.S., primary, Papaemmanuil, Elli, primary, Tosolini, Alessandra, primary, Frattini, Mark G., primary, MacBeth, Kyle J., primary, Liu, Guowen, primary, Fan, Bin, primary, Choe, Sung, primary, Wu, Bin, primary, Janjigian, Yelena Y., primary, Mellinghoff, Ingo K., primary, Diaz, Luis A., primary, Levine, Ross L., primary, Abou-Alfa, Ghassan K., primary, Stein, Eytan M., primary, and Intlekofer, Andrew M., primary

Published
2023
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35. Supplementary Methods, Figure Legends from Metabolic and Functional Genomic Studies Identify Deoxythymidylate Kinase as a Target in LKB1-Mutant Lung Cancer

Author

Liu, Yan, primary, Marks, Kevin, primary, Cowley, Glenn S., primary, Carretero, Julian, primary, Liu, Qingsong, primary, Nieland, Thomas J.F., primary, Xu, Chunxiao, primary, Cohoon, Travis J., primary, Gao, Peng, primary, Zhang, Yong, primary, Chen, Zhao, primary, Altabef, Abigail B., primary, Tchaicha, Jeremy H., primary, Wang, Xiaoxu, primary, Choe, Sung, primary, Driggers, Edward M., primary, Zhang, Jianming, primary, Bailey, Sean T., primary, Sharpless, Norman E., primary, Hayes, D. Neil, primary, Patel, Nirali M., primary, Janne, Pasi A., primary, Bardeesy, Nabeel, primary, Engelman, Jeffrey A., primary, Manning, Brendan D., primary, Shaw, Reuben J., primary, Asara, John M., primary, Scully, Ralph, primary, Kimmelman, Alec, primary, Byers, Lauren A., primary, Gibbons, Don L., primary, Wistuba, Ignacio I., primary, Heymach, John V., primary, Kwiatkowski, David J., primary, Kim, William Y., primary, Kung, Andrew L., primary, Gray, Nathanael S., primary, Root, David E., primary, Cantley, Lewis C., primary, and Wong, Kwok-Kin, primary

Published
2023
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38. A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition

Author

Mahoney, Christopher E., Pirman, David, Chubukov, Victor, Sleger, Taryn, Hayes, Sebastian, Fan, Zi Peng, Allen, Eric L., Chen, Ying, Huang, Lingling, Liu, Meina, Zhang, Yingjia, McDonald, Gabrielle, Narayanaswamy, Rohini, Choe, Sung, Chen, Yue, Gross, Stefan, Cianchetta, Giovanni, Padyana, Anil K., Murray, Stuart, Liu, Wei, Marks, Kevin M., Murtie, Joshua, Dorsch, Marion, Jin, Shengfang, Nagaraja, Nelamangala, Biller, Scott A., Roddy, Thomas, Popovici-Muller, Janeta, and Smolen, Gromoslaw A.

Published
2019
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39. Acquired resistance to IDH inhibition through trans or cis dimer-interface mutations

Author

Intlekofer, Andrew M., Shih, Alan H., Wang, Bo, Nazir, Abbas, Rustenburg, Ariën S., Albanese, Steven K., Patel, Minal, Famulare, Christopher, Correa, Fabian M., Takemoto, Naofumi, Durani, Vidushi, Liu, Hui, Taylor, Justin, Farnoud, Noushin, Papaemmanuil, Elli, Cross, Justin R., Tallman, Martin S., Arcila, Maria E., Roshal, Mikhail, Petsko, Gregory A., Wu, Bin, Choe, Sung, Konteatis, Zenon D., Biller, Scott A., Chodera, John D., Thompson, Craig B., Levine, Ross L., and Stein, Eytan M.

Published
2018
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40. Supplementary Fig. S3 from Efficacy and pharmacodynamic effects of bosutinib (SKI-606), a Src/Abl inhibitor, in freshly generated human pancreas cancer xenografts

Author

Messersmith, Wells A., primary, Rajeshkumar, N.V., primary, Tan, Aik Choon, primary, Wang, Xiao Fei, primary, Diesl, Veronica, primary, Choe, Sung E., primary, Follettie, Max, primary, Coughlin, Christina, primary, Boschelli, Frank, primary, Garcia-Garcia, Elena, primary, Lopez-Rios, Fernando, primary, Jimeno, Antonio, primary, and Hidalgo, Manuel, primary

Published
2023
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41. Data from Delineation of a Cellular Hierarchy in Lung Cancer Reveals an Oncofetal Antigen Expressed on Tumor-Initiating Cells

Author

Damelin, Marc, primary, Geles, Kenneth G., primary, Follettie, Maximillian T., primary, Yuan, Ping, primary, Baxter, Michelle, primary, Golas, Jonathon, primary, DiJoseph, John F., primary, Karnoub, Maha, primary, Huang, Shuguang, primary, Diesl, Veronica, primary, Behrens, Carmen, primary, Choe, Sung E., primary, Rios, Carol, primary, Gruzas, Janet, primary, Sridharan, Latha, primary, Dougher, Maureen, primary, Kunz, Arthur, primary, Hamann, Philip R., primary, Evans, Deborah, primary, Armellino, Douglas, primary, Khandke, Kiran, primary, Marquette, Kimberly, primary, Tchistiakova, Lioudmila, primary, Boghaert, Erwin R., primary, Abraham, Robert T., primary, Wistuba, Ignacio I., primary, and Zhou, Bin-Bing S., primary

Published
2023
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42. Supplementary Table 2 from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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43. Supplementary Methods from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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44. Supplementary Table 1 from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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45. Data from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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46. Supplementary Table 4 from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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47. Supplementary Figures 1-6, Tables 1-5, Methods from Delineation of a Cellular Hierarchy in Lung Cancer Reveals an Oncofetal Antigen Expressed on Tumor-Initiating Cells

Author

Damelin, Marc, primary, Geles, Kenneth G., primary, Follettie, Maximillian T., primary, Yuan, Ping, primary, Baxter, Michelle, primary, Golas, Jonathon, primary, DiJoseph, John F., primary, Karnoub, Maha, primary, Huang, Shuguang, primary, Diesl, Veronica, primary, Behrens, Carmen, primary, Choe, Sung E., primary, Rios, Carol, primary, Gruzas, Janet, primary, Sridharan, Latha, primary, Dougher, Maureen, primary, Kunz, Arthur, primary, Hamann, Philip R., primary, Evans, Deborah, primary, Armellino, Douglas, primary, Khandke, Kiran, primary, Marquette, Kimberly, primary, Tchistiakova, Lioudmila, primary, Boghaert, Erwin R., primary, Abraham, Robert T., primary, Wistuba, Ignacio I., primary, and Zhou, Bin-Bing S., primary

Published
2023
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48. Supplementary Table 3 from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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49. Supplementary Figures 1-3 from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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50. Supplementary Figure Legends 1-3 from Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway

Author

Crabtree, Judy S., primary, Jelinsky, Scott A., primary, Harris, Heather A., primary, Choe, Sung E., primary, Cotreau, Monette M., primary, Kimberland, Michelle L., primary, Wilson, Ewa, primary, Saraf, Kathryn A., primary, Liu, Wei, primary, McCampbell, Adrienne S., primary, Dave, Bhuvanesh, primary, Broaddus, Russell R., primary, Brown, Eugene L., primary, Kao, Wenling, primary, Skotnicki, Jerauld S., primary, Abou-Gharbia, Magid, primary, Winneker, Richard C., primary, and Walker, Cheryl L., primary

Published
2023
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