A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia
Krivtsov, Andrei V., Evans, Kathryn, Gadrey, Jayant Y., Eschle, Benjamin K., Hatton, Charlie, Uckelmann, Hannah J., Ross, Kenneth N., Perner, Florian, Olsen, Sarah N., Pritchard, Tara, McDermott, Lisa, Jones, Connor D., Jing, Duohui, Braytee, Ali, Chacon, Diego, Earley, Eric, McKeever, Brian M., Claremon, David, Gifford, Andrew J., Lee, Heather J., Teicher, Beverly A., Pimanda, John E., Beck, Dominik, Perry, Jennifer A., Smith, Malcolm A., McGeehan, Gerard M., Lock, Richard B., Armstrong, Scott A.
Published in Cancer cell (09.12.2019)
Published in Cancer cell (09.12.2019)
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Journal Article
The menin inhibitor revumenib in KMT2A-rearranged or NPM1-mutant leukaemia
Issa, Ghayas C., Aldoss, Ibrahim, DiPersio, John, Cuglievan, Branko, Stone, Richard, Arellano, Martha, Thirman, Michael J., Patel, Manish R., Dickens, David S., Shenoy, Shalini, Shukla, Neerav, Kantarjian, Hagop, Armstrong, Scott A., Perner, Florian, Perry, Jennifer A., Rosen, Galit, Bagley, Rebecca G., Meyers, Michael L., Ordentlich, Peter, Gu, Yu, Kumar, Vinit, Smith, Steven, McGeehan, Gerard M., Stein, Eytan M.
Published in Nature (London) (30.03.2023)
Published in Nature (London) (30.03.2023)
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Journal Article
MEN1 mutations mediate clinical resistance to menin inhibition
Perner, Florian, Stein, Eytan M., Wenge, Daniela V., Singh, Sukrit, Kim, Jeonghyeon, Apazidis, Athina, Rahnamoun, Homa, Anand, Disha, Marinaccio, Christian, Hatton, Charlie, Wen, Yanhe, Stone, Richard M., Schaller, David, Mowla, Shoron, Xiao, Wenbin, Gamlen, Holly A., Stonestrom, Aaron J., Persaud, Sonali, Ener, Elizabeth, Cutler, Jevon A., Doench, John G., McGeehan, Gerard M., Volkamer, Andrea, Chodera, John D., Nowak, Radosław P., Fischer, Eric S., Levine, Ross L., Armstrong, Scott A., Cai, Sheng F.
Published in Nature (London) (30.03.2023)
Published in Nature (London) (30.03.2023)
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Journal Article
Therapeutic targeting of preleukemia cells in a mouse model of NPM1 mutant acute myeloid leukemia
Uckelmann, Hannah J, Kim, Stephanie M, Wong, Eric M, Hatton, Charles, Giovinazzo, Hugh, Gadrey, Jayant Y, Krivtsov, Andrei V, Rücker, Frank G, Döhner, Konstanze, McGeehan, Gerard M, Levine, Ross L, Bullinger, Lars, Vassiliou, George S, Armstrong, Scott A
Published in Science (American Association for the Advancement of Science) (31.01.2020)
Published in Science (American Association for the Advancement of Science) (31.01.2020)
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Journal Article
The menin-MLL1 interaction is a molecular dependency in NUP98-rearranged AML
Heikamp, Emily B., Henrich, Jill A., Perner, Florian, Wong, Eric M., Hatton, Charles, Wen, Yanhe, Barwe, Sonali P., Gopalakrishnapillai, Anilkumar, Xu, Haiming, Uckelmann, Hannah J., Takao, Sumiko, Kazansky, Yaniv, Pikman, Yana, McGeehan, Gerard M., Kolb, Edward A., Kentsis, Alex, Armstrong, Scott A.
Published in Blood (10.02.2022)
Published in Blood (10.02.2022)
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Journal Article
Synergistic targeting of FLT3 mutations in AML via combined menin-MLL and FLT3 inhibition
Dzama, Margarita M., Steiner, Marlene, Rausch, Johanna, Sasca, Daniel, Schönfeld, Jonas, Kunz, Kerstin, Taubert, Martha C., McGeehan, Gerard M., Chen, Chun-Wei, Mupo, Annalisa, Hähnel, Patricia, Theobald, Matthias, Kindler, Thomas, Koche, Richard P., Vassiliou, George S., Armstrong, Scott A., Kühn, Michael W.M.
Published in Blood (19.11.2020)
Published in Blood (19.11.2020)
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Journal Article
Inhibition of menin, BCL-2, and FLT3 combined with a hypomethylating agent cures NPM1/FLT3 -ITD/-TKD mutant acute myeloid leukemia in a patient-derived xenograft model
Carter, Bing Z, Mak, Po Yee, Tao, Wenjing, Ostermann, Lauren B, Mak, Duncan H, Ke, Baozhen, Ordentlich, Peter, McGeehan, Gerard M, Andreeff, Michael
Published in Haematologica (Roma) (01.09.2023)
Published in Haematologica (Roma) (01.09.2023)
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Journal Article
Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c)
Fiskus, Warren, Boettcher, Steffen, Daver, Naval, Mill, Christopher P., Sasaki, Koji, Birdwell, Christine E., Davis, John A., Takahashi, Koichi, Kadia, Tapan M., DiNardo, Courtney D., Jin, Qi, Qi, Yuan, Su, Xiaoping, McGeehan, Gerard M., Khoury, Joseph D., Ebert, Benjamin L., Bhalla, Kapil N.
Published in Blood cancer journal (New York) (11.01.2022)
Published in Blood cancer journal (New York) (11.01.2022)
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Journal Article
Mezigdomide is effective alone and in combination with menin inhibition in preclinical models of KMT2A-r and NPM1c AML
Bourgeois, Wallace, Cutler, Jevon A., Aubrey, Brandon J., Wenge, Daniela V., Perner, Florian, Martucci, Cynthia, Henrich, Jill A., Klega, Kelly, Nowak, Radosław P., Donovan, Katherine A., Boileau, Meaghan, Wen, Yanhe, Hatton, Charlie, Apazidis, Athina A., Olsen, Sarah Naomi, Kirmani, Nadia, Pikman, Yana, Pollard, Jessica A., Perry, Jennifer A., Sperling, Adam S., Ebert, Benjamin L., McGeehan, Gerard M., Crompton, Brian D., Fischer, Eric S., Armstrong, Scott A.
Published in Blood (11.04.2024)
Published in Blood (11.04.2024)
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Journal Article
Causal linkage of presence of mutant NPM1 to efficacy of novel therapeutic agents against AML cells with mutant NPM1
Mill, Christopher P., Fiskus, Warren, Das, Kaberi, Davis, John A., Birdwell, Christine E., Kadia, Tapan M., DiNardo, Courtney D., Daver, Naval, Takahashi, Koichi, Sasaki, Koji, McGeehan, Gerard M., Ruan, Xinjia, Su, Xiaoping, Loghavi, Sanam, Kantarjian, Hagop, Bhalla, Kapil N.
Published in Leukemia (01.06.2023)
Published in Leukemia (01.06.2023)
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Journal Article
Targeting Menin disrupts the KMT2A/B and polycomb balance to paradoxically activate bivalent genes
Sparbier, Christina E., Gillespie, Andrea, Gomez, Juliana, Kumari, Nishi, Motazedian, Ali, Chan, Kah Lok, Bell, Charles C., Gilan, Omer, Chan, Yih-Chih, Popp, Sarah, Gough, Daniel J., Eckersley-Maslin, Melanie A., Dawson, Sarah-Jane, Lehner, Paul J., Sutherland, Kate D., Ernst, Patricia, McGeehan, Gerard M., Lam, Enid Y. N., Burr, Marian L., Dawson, Mark A.
Published in Nature cell biology (01.02.2023)
Published in Nature cell biology (01.02.2023)
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Journal Article
Menin is necessary for long term maintenance of meningioma-1 driven leukemia
Libbrecht, Clara, Xie, Hongbo M., Kingsley, Molly C., Haladyna, Jessica N., Riedel, Simone S., Alikarami, Fatemeh, Lenard, Alexandra, McGeehan, Gerard M., Ernst, Patricia, Bernt, Kathrin M.
Published in Leukemia (01.05.2021)
Published in Leukemia (01.05.2021)
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Journal Article
Targeting of epigenetic co-dependencies enhances anti-AML efficacy of Menin inhibitor in AML with MLL1-r or mutant NPM1
Fiskus, Warren, Mill, Christopher P., Birdwell, Christine, Davis, John A., Das, Kaberi, Boettcher, Steffen, Kadia, Tapan M., DiNardo, Courtney D., Takahashi, Koichi, Loghavi, Sanam, Soth, Michael J., Heffernan, Tim, McGeehan, Gerard M., Ruan, Xinjia, Su, Xiaoping, Vakoc, Christopher R., Daver, Naval, Bhalla, Kapil N.
Published in Blood cancer journal (New York) (13.04.2023)
Published in Blood cancer journal (New York) (13.04.2023)
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Journal Article
Evaluation of VTP‐50469, a menin‐MLL1 inhibitor, against Ewing sarcoma xenograft models by the pediatric preclinical testing consortium
Kurmasheva, Raushan T., Bandyopadhyay, Abhik, Favours, Edward, Pozo, Vanessa Del, Ghilu, Samson, Phelps, Doris A., McGeehan, Gerard M., Erickson, Stephen W., Smith, Malcolm A., Houghton, Peter J.
Published in Pediatric blood & cancer (01.07.2020)
Published in Pediatric blood & cancer (01.07.2020)
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Journal Article
Discovery of Potent Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 Using a Novel Growth-Based Protocol of in Silico Screening and Optimization in CONTOUR
Liu, Zhijie, Singh, Suresh B, Zheng, Yajun, Lindblom, Peter, Tice, Colin, Dong, Chengguo, Zhuang, Linghang, Zhao, Yi, Kruk, Barbara A, Lala, Deepak, Claremon, David A, McGeehan, Gerard M, Gregg, Richard D, Cain, Robert
Published in Journal of chemical information and modeling (26.08.2019)
Published in Journal of chemical information and modeling (26.08.2019)
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Journal Article
The MLL–Menin Interaction is a Therapeutic Vulnerability in NUP98‐rearranged AML
Rasouli, Milad, Blair, Helen, Troester, Selina, Szoltysek, Katarzyna, Cameron, Rachel, Ashtiani, Minoo, Krippner‐Heidenreich, Anja, Grebien, Florian, McGeehan, Gerard, Zwaan, C. Michel, Heidenreich, Olaf
Published in HemaSphere (01.08.2023)
Published in HemaSphere (01.08.2023)
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Journal Article
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists
Lotesta, Stephen D., Marcus, Andrew P., Zheng, Yajun, Leftheris, Katerina, Noto, Paul B., Meng, Shi, Kandpal, Geeta, Chen, Guozhou, Zhou, Jing, McKeever, Brian, Bukhtiyarov, Yuri, Zhao, Yi, Lala, Deepak S., Singh, Suresh B., McGeehan, Gerard M.
Published in Bioorganic & medicinal chemistry (15.03.2016)
Published in Bioorganic & medicinal chemistry (15.03.2016)
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Journal Article
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist
Zheng, Yajun, Zhuang, Linghang, Fan, Kristi Yi, Tice, Colin M, Zhao, Wei, Dong, Chengguo, Lotesta, Stephen D, Leftheris, Katerina, Lindblom, Peter R, Liu, Zhijie, Shimada, Jun, Noto, Paul B, Meng, Shi, Hardy, Andrew, Howard, Lamont, Krosky, Paula, Guo, Joan, Lipinski, Kerri, Kandpal, Geeta, Bukhtiyarov, Yuri, Zhao, Yi, Lala, Deepak, Van Orden, Rebecca, Zhou, Jing, Chen, Guozhou, Wu, Zhongren, McKeever, Brian M, McGeehan, Gerard M, Gregg, Richard E, Claremon, David A, Singh, Suresh B
Published in Journal of medicinal chemistry (14.04.2016)
Published in Journal of medicinal chemistry (14.04.2016)
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Journal Article
IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia
Aubrey, Brandon J, Cutler, Jevon A, Bourgeois, Wallace, Donovan, Katherine A, Gu, Shengqing, Hatton, Charlie, Perlee, Sarah, Perner, Florian, Rahnamoun, Homa, Theall, Alexandra C P, Henrich, Jill A, Zhu, Qian, Nowak, Radosław P, Kim, Young Joon, Parvin, Salma, Cremer, Anjali, Olsen, Sarah Naomi, Eleuteri, Nicholas A, Pikman, Yana, McGeehan, Gerard M, Stegmaier, Kimberly, Letai, Anthony, Fischer, Eric S, Liu, X Shirley, Armstrong, Scott A
Published in Nature cancer (01.05.2022)
Published in Nature cancer (01.05.2022)
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Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes
Hamilton, Bradford S., Himmelsbach, Frank, Nar, Herbert, Schuler-Metz, Annette, Krosky, Paula, Guo, Joan, Guo, Rong, Meng, Shi, Zhao, Yi, Lala, Deepak S., Zhuang, Linghang, Claremon, David A., McGeehan, Gerard M.
Published in European journal of pharmacology (05.01.2015)
Published in European journal of pharmacology (05.01.2015)
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