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(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: kuznetsova e. 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.
Control of the hippo pathway by Set7-dependent methylation of Yap.
Oudhoff MJ, Freeman SA, Couzens AL, Antignano F, Kuznetsova E, Min PH, Northrop JP, Lehnertz B, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Nishina H, Gold MR, Rossi FM, Gingras AC, Zaph C. Oudhoff MJ, et al. Among authors: kuznetsova e. Dev Cell. 2013 Jul 29;26(2):188-94. doi: 10.1016/j.devcel.2013.05.025. Epub 2013 Jul 11. Dev Cell. 2013. PMID: 23850191 Free article.
A Basic Post-SET Extension of NSDs Is Essential for Nucleosome Binding In Vitro.
Allali-Hassani A, Kuznetsova E, Hajian T, Wu H, Dombrovski L, Li Y, Gräslund S, Arrowsmith CH, Schapira M, Vedadi M. Allali-Hassani A, et al. Among authors: kuznetsova e. J Biomol Screen. 2014 Jul;19(6):928-35. doi: 10.1177/1087057114525854. Epub 2014 Mar 4. J Biomol Screen. 2014. PMID: 24595546
Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.
Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KVM, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G. Grebien F, et al. Among authors: kuznetsova e. Nat Chem Biol. 2015 Aug;11(8):571-578. doi: 10.1038/nchembio.1859. Epub 2015 Jul 13. Nat Chem Biol. 2015. PMID: 26167872 Free PMC article.
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: kuznetsova e. 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
Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction.
Bolshan Y, Getlik M, Kuznetsova E, Wasney GA, Hajian T, Poda G, Nguyen KT, Wu H, Dombrovski L, Dong A, Senisterra G, Schapira M, Arrowsmith CH, Brown PJ, Al-Awar R, Vedadi M, Smil D. Bolshan Y, et al. Among authors: kuznetsova e. ACS Med Chem Lett. 2013 Feb 4;4(3):353-7. doi: 10.1021/ml300467n. eCollection 2013 Mar 14. ACS Med Chem Lett. 2013. PMID: 24900672 Free PMC article.
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E, Rougie M, Jiang A, Pattenden SG, Norris JL, James LI, Roth BL, Brown PJ, Frye SV, Arrowsmith CH, Hahn KM, Wang GG, Vedadi M, Jin J. Konze KD, et al. Among authors: kuznetsova e. ACS Chem Biol. 2013;8(6):1324-34. doi: 10.1021/cb400133j. Epub 2013 Apr 24. ACS Chem Biol. 2013. PMID: 23614352 Free PMC article.
High throughput screening of purified proteins for enzymatic activity.
Proudfoot M, Kuznetsova E, Sanders SA, Gonzalez CF, Brown G, Edwards AM, Arrowsmith CH, Yakunin AF. Proudfoot M, et al. Among authors: kuznetsova e. Methods Mol Biol. 2008;426:331-41. doi: 10.1007/978-1-60327-058-8_21. Methods Mol Biol. 2008. PMID: 18542874
706 results