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Page 1
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: marcellus r. 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
Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R. Getlik M, et al. Among authors: marcellus r. J Med Chem. 2016 Mar 24;59(6):2478-96. doi: 10.1021/acs.jmedchem.5b01630. Epub 2016 Mar 9. J Med Chem. 2016. PMID: 26958703
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: marcellus r. 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.
Identification of RSK and TTK as Modulators of Blood Vessel Morphogenesis Using an Embryonic Stem Cell-Based Vascular Differentiation Assay.
Hammoud L, Adams JR, Loch AJ, Marcellus RC, Uehling DE, Aman A, Fladd C, McKee TD, Jo CEB, Al-Awar R, Egan SE, Rossant J. Hammoud L, et al. Among authors: marcellus rc. Stem Cell Reports. 2016 Oct 11;7(4):787-801. doi: 10.1016/j.stemcr.2016.08.004. Epub 2016 Sep 8. Stem Cell Reports. 2016. PMID: 27618721 Free PMC article.
A drug discovery platform to identify compounds that inhibit EGFR triple mutants.
Saraon P, Snider J, Kalaidzidis Y, Wybenga-Groot LE, Weiss K, Rai A, Radulovich N, Drecun L, Vučković N, Vučetić A, Wong V, Thériault B, Pham NA, Park JH, Datti A, Wang J, Pathmanathan S, Aboualizadeh F, Lyakisheva A, Yao Z, Wang Y, Joseph B, Aman A, Moran MF, Prakesch M, Poda G, Marcellus R, Uehling D, Samaržija M, Jakopović M, Tsao MS, Shepherd FA, Sacher A, Leighl N, Akhmanova A, Al-Awar R, Zerial M, Stagljar I. Saraon P, et al. Among authors: marcellus r. Nat Chem Biol. 2020 May;16(5):577-586. doi: 10.1038/s41589-020-0484-2. Epub 2020 Feb 24. Nat Chem Biol. 2020. PMID: 32094923 Free PMC article.
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. Among authors: marcellus r. 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
Small molecule epigenetic screen identifies novel EZH2 and HDAC inhibitors that target glioblastoma brain tumor-initiating cells.
Grinshtein N, Rioseco CC, Marcellus R, Uehling D, Aman A, Lun X, Muto O, Podmore L, Lever J, Shen Y, Blough MD, Cairncross GJ, Robbins SM, Jones SJ, Marra MA, Al-Awar R, Senger DL, Kaplan DR. Grinshtein N, et al. Among authors: marcellus r. Oncotarget. 2016 Sep 13;7(37):59360-59376. doi: 10.18632/oncotarget.10661. Oncotarget. 2016. PMID: 27449082 Free PMC article.
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Yu W, et al. Among authors: marcellus r. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304. Nat Commun. 2012. PMID: 23250418 Free article.
An allosteric inhibitor of protein arginine methyltransferase 3.
Siarheyeva A, Senisterra G, Allali-Hassani A, Dong A, Dobrovetsky E, Wasney GA, Chau I, Marcellus R, Hajian T, Liu F, Korboukh I, Smil D, Bolshan Y, Min J, Wu H, Zeng H, Loppnau P, Poda G, Griffin C, Aman A, Brown PJ, Jin J, Al-Awar R, Arrowsmith CH, Schapira M, Vedadi M. Siarheyeva A, et al. Among authors: marcellus r. Structure. 2012 Aug 8;20(8):1425-35. doi: 10.1016/j.str.2012.06.001. Epub 2012 Jul 12. Structure. 2012. PMID: 22795084 Free article.
48 results