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Page 1
Wnt inhibitor screen reveals iron dependence of β-catenin signaling in cancers.
Song S, Christova T, Perusini S, Alizadeh S, Bao RY, Miller BW, Hurren R, Jitkova Y, Gronda M, Isaac M, Joseph B, Subramaniam R, Aman A, Chau A, Hogge DE, Weir SJ, Kasper J, Schimmer AD, Al-awar R, Wrana JL, Attisano L. Song S, et al. Cancer Res. 2011 Dec 15;71(24):7628-39. doi: 10.1158/0008-5472.CAN-11-2745. Epub 2011 Oct 18. Cancer Res. 2011. PMID: 22009536 Clinical Trial.
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
Ensan D, Smil D, Zepeda-Velázquez CA, Panagopoulos D, Wong JF, Williams EP, Adamson R, Bullock AN, Kiyota T, Aman A, Roberts OG, Edwards AM, O'Meara JA, Isaac MB, Al-Awar R. Ensan D, et al. Among authors: isaac mb. J Med Chem. 2020 May 14;63(9):4978-4996. doi: 10.1021/acs.jmedchem.0c00395. Epub 2020 May 5. J Med Chem. 2020. PMID: 32369358 Free PMC article.
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.
Smil D, Wong JF, Williams EP, Adamson RJ, Howarth A, McLeod DA, Mamai A, Kim S, Wilson BJ, Kiyota T, Aman A, Owen J, Poda G, Horiuchi KY, Kuznetsova E, Ma H, Hamblin JN, Cramp S, Roberts OG, Edwards AM, Uehling D, Al-Awar R, Bullock AN, O'Meara JA, Isaac MB. Smil D, et al. Among authors: isaac mb. J Med Chem. 2020 Sep 10;63(17):10061-10085. doi: 10.1021/acs.jmedchem.0c01199. Epub 2020 Aug 26. J Med Chem. 2020. PMID: 32787083 Free article.
Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma.
Uehling DE, Joseph B, Chung KC, Zhang AX, Ler S, Prakesch MA, Poda G, Grouleff J, Aman A, Kiyota T, Leung-Hagesteijn C, Konda JD, Marcellus R, Griffin C, Subramaniam R, Abibi A, Strathdee CA, Isaac MB, Al-Awar R, Tiedemann RE. Uehling DE, et al. Among authors: isaac mb. J Med Chem. 2021 Aug 12;64(15):11129-11147. doi: 10.1021/acs.jmedchem.1c00506. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34291633
Chemical Genetics Screen Identifies COPB2 Tool Compounds That Alters ER Stress Response and Induces RTK Dysregulation in Lung Cancer Cells.
Saraon P, Snider J, Schormann W, Rai A, Radulovich N, Sánchez-Osuna M, Coulombe-Huntington J, Huard C, Mohammed M, Lima-Fernandes E, Thériault B, Halabelian L, Chan M, Joshi D, Drecun L, Yao Z, Pathmanathan S, Wong V, Lyakisheva A, Aboualizadeh F, Niu L, Li F, Kiyota T, Subramanian R, Joseph B, Aman A, Prakesch M, Isaac M, Mamai A, Poda G, Vedadi M, Marcellus R, Uehling D, Leighl N, Sacher A, Samaržija M, Jakopović M, Arrowsmith C, Tyers M, Tsao MS, Andrews D, Al-Awar R, Stagljar I. Saraon P, et al. J Mol Biol. 2021 Nov 19;433(23):167294. doi: 10.1016/j.jmb.2021.167294. Epub 2021 Oct 16. J Mol Biol. 2021. PMID: 34662547
Correction to "Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma".
Uehling DE, Joseph B, Chung KC, Zhang AX, Ler S, Prakesch MA, Poda G, Grouleff J, Aman A, Kiyota T, Leung-Hagesteijn C, Konda JD, Marcellus R, Griffin C, Subramaniam R, Abibi A, Strathdee CA, Isaac MB, Al-Awar R, Tiedemann RE. Uehling DE, et al. Among authors: isaac mb. J Med Chem. 2022 Jan 13;65(1):886-887. doi: 10.1021/acs.jmedchem.1c02066. Epub 2021 Dec 28. J Med Chem. 2022. PMID: 34963044 No abstract available.
Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.
Mamai A, Chau AM, Wilson BJ, Watson ID, Joseph BB, Subramanian PR, Morshed MM, Morin JA, Prakesch MA, Lu T, Connolly P, Kuntz DA, Pomroy NC, Poda G, Nguyen K, Marcellus R, Strathdee G, Theriault B, Subramaniam R, Mohammed M, Abibi A, Chan M, Winston J, Kiyota T, Undzys E, Aman A, Austin N, Du Jardin M, Packman K, Phillippar U, Attar R, Edwards J, O'Meara J, Uehling DE, Al-Awar R, Privé GG, Isaac MB. Mamai A, et al. Among authors: isaac mb. ACS Med Chem Lett. 2023 Jan 12;14(2):199-210. doi: 10.1021/acsmedchemlett.2c00502. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793435 Free PMC article.
The Imipridone ONC213 Targets α-Ketoglutarate Dehydrogenase to Induce Mitochondrial Stress and Suppress Oxidative Phosphorylation in Acute Myeloid Leukemia.
Su Y, Carter JL, Li X, Fukuda Y, Gray A, Lynch J, Edwards H, Ma J, Schreiner P, Polin L, Kushner J, Dzinic SH, Buck SA, Pruett-Miller SM, Hege-Hurrish K, Robinson C, Qiao X, Liu S, Wu S, Wang G, Li J, Allen JE, Prabhu VV, Schimmer AD, Joshi D, Kalhor-Monfared S, Watson IDG, Marcellus R, Isaac MB, Al-Awar R, Taub JW, Lin H, Schuetz JD, Ge Y. Su Y, et al. Among authors: isaac mb. Cancer Res. 2024 Apr 1;84(7):1084-1100. doi: 10.1158/0008-5472.CAN-23-2659. Cancer Res. 2024. PMID: 38266099
Discovery of Conformationally Constrained ALK2 Inhibitors.
González-Álvarez H, Ensan D, Xin T, Wong JF, Zepeda-Velázquez CA, Cros J, Sweeney MN, Hoffer L, Kiyota T, Wilson BJ, Aman A, Roberts O, Isaac MB, Bullock AN, Smil D, Al-Awar R. González-Álvarez H, et al. Among authors: isaac mb. J Med Chem. 2024 Mar 28;67(6):4707-4725. doi: 10.1021/acs.jmedchem.3c02308. Epub 2024 Mar 18. J Med Chem. 2024. PMID: 38498998 Free PMC article.
43 results