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Page 1
Inhibition of mutant IDH1 promotes cycling of acute myeloid leukemia stem cells.
Gruber E, So J, Lewis AC, Franich R, Cole R, Martelotto LG, Rogers AJ, Vidacs E, Fraser P, Stanley K, Jones L, Trigos A, Thio N, Li J, Nicolay B, Daigle S, Tron AE, Hyer ML, Shortt J, Johnstone RW, Kats LM. Gruber E, et al. Among authors: hyer ml. Cell Rep. 2022 Aug 16;40(7):111182. doi: 10.1016/j.celrep.2022.111182. Cell Rep. 2022. PMID: 35977494 Free article.
Inhibition of D-2HG leads to upregulation of a proinflammatory gene signature in a novel HLA-A2/HLA-DR1 transgenic mouse model of IDH1R132H-expressing glioma.
Chuntova P, Yamamichi A, Chen T, Narayanaswamy R, Ronseaux S, Hudson C, Tron AE, Hyer ML, Montoya M, Mende AL, Nejo T, Downey KM, Diebold D, Lu M, Nicolay B, Okada H. Chuntova P, et al. Among authors: hyer ml. J Immunother Cancer. 2022 May;10(5):e004644. doi: 10.1136/jitc-2022-004644. J Immunother Cancer. 2022. PMID: 35606087 Free PMC article.
Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia.
Barghout SH, Patel PS, Wang X, Xu GW, Kavanagh S, Halgas O, Zarabi SF, Gronda M, Hurren R, Jeyaraju DV, MacLean N, Brennan S, Hyer ML, Berger A, Traore T, Milhollen M, Smith AC, Minden MD, Pai EF, Hakem R, Schimmer AD. Barghout SH, et al. Among authors: hyer ml. Leukemia. 2019 Jan;33(1):37-51. doi: 10.1038/s41375-018-0167-0. Epub 2018 Jun 8. Leukemia. 2019. PMID: 29884901
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion.
Konteatis Z, Travins J, Gross S, Marjon K, Barnett A, Mandley E, Nicolay B, Nagaraja R, Chen Y, Sun Y, Liu Z, Yu J, Ye Z, Jiang F, Wei W, Fang C, Gao Y, Kalev P, Hyer ML, DeLaBarre B, Jin L, Padyana AK, Dang L, Murtie J, Biller SA, Sui Z, Marks KM. Konteatis Z, et al. Among authors: hyer ml. J Med Chem. 2021 Apr 22;64(8):4430-4449. doi: 10.1021/acs.jmedchem.0c01895. Epub 2021 Apr 8. J Med Chem. 2021. PMID: 33829783 Free article.
MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage.
Kalev P, Hyer ML, Gross S, Konteatis Z, Chen CC, Fletcher M, Lein M, Aguado-Fraile E, Frank V, Barnett A, Mandley E, Goldford J, Chen Y, Sellers K, Hayes S, Lizotte K, Quang P, Tuncay Y, Clasquin M, Peters R, Weier J, Simone E, Murtie J, Liu W, Nagaraja R, Dang L, Sui Z, Biller SA, Travins J, Marks KM, Marjon K. Kalev P, et al. Among authors: hyer ml. Cancer Cell. 2021 Feb 8;39(2):209-224.e11. doi: 10.1016/j.ccell.2020.12.010. Epub 2021 Jan 14. Cancer Cell. 2021. PMID: 33450196 Free article.
Ubiquitin-activating enzyme inhibition induces an unfolded protein response and overcomes drug resistance in myeloma.
Zhuang J, Shirazi F, Singh RK, Kuiatse I, Wang H, Lee HC, Berkova Z, Berger A, Hyer M, Chattopadhyay N, Syed S, Shi JQ, Yu J, Shinde V, Tirrell S, Jones RJ, Wang Z, Davis RE, Orlowski RZ. Zhuang J, et al. Blood. 2019 Apr 4;133(14):1572-1584. doi: 10.1182/blood-2018-06-859686. Epub 2019 Feb 8. Blood. 2019. PMID: 30737236 Free PMC article.
Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads.
Li M, Konteatis Z, Nagaraja N, Chen Y, Zhou S, Ma G, Gross S, Marjon K, Hyer ML, Mandley E, Lein M, Padyana AK, Jin L, Tong S, Peters R, Murtie J, Travins J, Medeiros M, Liu P, Frank V, Judd ET, Biller SA, Marks KM, Sui Z, Reznik SK. Li M, et al. Among authors: hyer ml. J Med Chem. 2022 Mar 24;65(6):4600-4615. doi: 10.1021/acs.jmedchem.1c01595. Epub 2022 Mar 16. J Med Chem. 2022. PMID: 35293760
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Duffey MO, Vos TJ, Adams R, Alley J, Anthony J, Barrett C, Bharathan I, Bowman D, Bump NJ, Chau R, Cullis C, Driscoll DL, Elder A, Forsyth N, Frazer J, Guo J, Guo L, Hyer ML, Janowick D, Kulkarni B, Lai SJ, Lasky K, Li G, Li J, Liao D, Little J, Peng B, Qian MG, Reynolds DJ, Rezaei M, Scott MP, Sells TB, Shinde V, Shi QJ, Sintchak MD, Soucy F, Sprott KT, Stroud SG, Nestor M, Visiers I, Weatherhead G, Ye Y, D'Amore N. Duffey MO, et al. Among authors: hyer ml. J Med Chem. 2012 Jan 12;55(1):197-208. doi: 10.1021/jm2011172. Epub 2011 Dec 5. J Med Chem. 2012. PMID: 22070629
Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.
Manfredi MG, Ecsedy JA, Chakravarty A, Silverman L, Zhang M, Hoar KM, Stroud SG, Chen W, Shinde V, Huck JJ, Wysong DR, Janowick DA, Hyer ML, Leroy PJ, Gershman RE, Silva MD, Germanos MS, Bolen JB, Claiborne CF, Sells TB. Manfredi MG, et al. Among authors: hyer ml. Clin Cancer Res. 2011 Dec 15;17(24):7614-24. doi: 10.1158/1078-0432.CCR-11-1536. Epub 2011 Oct 20. Clin Cancer Res. 2011. PMID: 22016509
30 results