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Page 1
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: aman a. 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: aman a. 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.
Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.
Haftchenary S, Luchman HA, Jouk AO, Veloso AJ, Page BD, Cheng XR, Dawson SS, Grinshtein N, Shahani VM, Kerman K, Kaplan DR, Griffin C, Aman AM, Al-Awar R, Weiss S, Gunning PT. Haftchenary S, et al. ACS Med Chem Lett. 2013 Sep 8;4(11):1102-7. doi: 10.1021/ml4003138. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900612 Free PMC article.
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH. Barsyte-Lovejoy D, et al. Among authors: aman a. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. doi: 10.1073/pnas.1407358111. Epub 2014 Aug 18. Proc Natl Acad Sci U S A. 2014. PMID: 25136132 Free PMC article.
Inhibition of the Mitochondrial Protease ClpP as a Therapeutic Strategy for Human Acute Myeloid Leukemia.
Cole A, Wang Z, Coyaud E, Voisin V, Gronda M, Jitkova Y, Mattson R, Hurren R, Babovic S, Maclean N, Restall I, Wang X, Jeyaraju DV, Sukhai MA, Prabha S, Bashir S, Ramakrishnan A, Leung E, Qia YH, Zhang N, Combes KR, Ketela T, Lin F, Houry WA, Aman A, Al-Awar R, Zheng W, Wienholds E, Xu CJ, Dick J, Wang JC, Moffat J, Minden MD, Eaves CJ, Bader GD, Hao Z, Kornblau SM, Raught B, Schimmer AD. Cole A, et al. Among authors: aman a. Cancer Cell. 2015 Jun 8;27(6):864-76. doi: 10.1016/j.ccell.2015.05.004. Cancer Cell. 2015. PMID: 26058080 Free PMC article.
FV-162 is a novel, orally bioavailable, irreversible proteasome inhibitor with improved pharmacokinetics displaying preclinical efficacy with continuous daily dosing.
Wang Z, Dove P, Wang X, Shamas-Din A, Li Z, Nachman A, Oh YJ, Hurren R, Ruschak A, Climie S, Press B, Griffin C, Undzys E, Aman A, Al-awar R, Kay LE, O'Neill D, Trudel S, Slassi M, Schimmer AD. Wang Z, et al. Among authors: aman a. Cell Death Dis. 2015 Jul 9;6(7):e1815. doi: 10.1038/cddis.2015.187. Cell Death Dis. 2015. PMID: 26158521 Free PMC article.
Metformin Pharmacokinetics in Mouse Tumors: Implications for Human Therapy.
Dowling RJ, Lam S, Bassi C, Mouaaz S, Aman A, Kiyota T, Al-Awar R, Goodwin PJ, Stambolic V. Dowling RJ, et al. Among authors: aman a. Cell Metab. 2016 Apr 12;23(4):567-8. doi: 10.1016/j.cmet.2016.03.006. Cell Metab. 2016. PMID: 27076069 Free article. No abstract available.
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: aman a. Oncotarget. 2016 Sep 13;7(37):59360-59376. doi: 10.18632/oncotarget.10661. Oncotarget. 2016. PMID: 27449082 Free PMC article.
295 results