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Page 1
A simple assay for detection of small-molecule redox activity.
Lor LA, Schneck J, McNulty DE, Diaz E, Brandt M, Thrall SH, Schwartz B. Lor LA, et al. Among authors: diaz e. J Biomol Screen. 2007 Sep;12(6):881-90. doi: 10.1177/1087057107304113. Epub 2007 Jun 19. J Biomol Screen. 2007. PMID: 17579124
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.
Diaz E, Machutta CA, Chen S, Jiang Y, Nixon C, Hofmann G, Key D, Sweitzer S, Patel M, Wu Z, Creasy CL, Kruger RG, LaFrance L, Verma SK, Pappalardi MB, Le B, Van Aller GS, McCabe MT, Tummino PJ, Pope AJ, Thrall SH, Schwartz B, Brandt M. Diaz E, et al. J Biomol Screen. 2012 Dec;17(10):1279-92. doi: 10.1177/1087057112453765. Epub 2012 Aug 17. J Biomol Screen. 2012. PMID: 22904200
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction.
Gilmartin AG, Faitg TH, Richter M, Groy A, Seefeld MA, Darcy MG, Peng X, Federowicz K, Yang J, Zhang SY, Minthorn E, Jaworski JP, Schaber M, Martens S, McNulty DE, Sinnamon RH, Zhang H, Kirkpatrick RB, Nevins N, Cui G, Pietrak B, Diaz E, Jones A, Brandt M, Schwartz B, Heerding DA, Kumar R. Gilmartin AG, et al. Among authors: diaz e. Nat Chem Biol. 2014 Mar;10(3):181-7. doi: 10.1038/nchembio.1427. Epub 2014 Jan 5. Nat Chem Biol. 2014. PMID: 24390428
Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27).
McCabe MT, Graves AP, Ganji G, Diaz E, Halsey WS, Jiang Y, Smitheman KN, Ott HM, Pappalardi MB, Allen KE, Chen SB, Della Pietra A 3rd, Dul E, Hughes AM, Gilbert SA, Thrall SH, Tummino PJ, Kruger RG, Brandt M, Schwartz B, Creasy CL. McCabe MT, et al. Among authors: diaz e. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2989-94. doi: 10.1073/pnas.1116418109. Epub 2012 Feb 8. Proc Natl Acad Sci U S A. 2012. PMID: 22323599 Free PMC article.
Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.
Lawhorn BG, Tran T, Hong VS, Morgan LA, Le BT, Harpel MR, Jolivette L, Diaz E, Schwartz B, Gross JW, Tomaszek T, Semus S, Concha N, Smallwood A, Holt DA, Kallander LS. Lawhorn BG, et al. Among authors: diaz e. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4838-4843. doi: 10.1016/j.bmcl.2017.09.046. Epub 2017 Sep 23. Bioorg Med Chem Lett. 2017. PMID: 28985999
Long residence time inhibition of EZH2 in activated polycomb repressive complex 2.
Van Aller GS, Pappalardi MB, Ott HM, Diaz E, Brandt M, Schwartz BJ, Miller WH, Dhanak D, McCabe MT, Verma SK, Creasy CL, Tummino PJ, Kruger RG. Van Aller GS, et al. Among authors: diaz e. ACS Chem Biol. 2014 Mar 21;9(3):622-9. doi: 10.1021/cb4008748. Epub 2013 Dec 31. ACS Chem Biol. 2014. PMID: 24304166
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra A 3rd, Diaz E, LaFrance LV, Mellinger M, Duquenne C, Tian X, Kruger RG, McHugh CF, Brandt M, Miller WH, Dhanak D, Verma SK, Tummino PJ, Creasy CL. McCabe MT, et al. Among authors: diaz e. Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10. Nature. 2012. PMID: 23051747
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH. Verma SK, et al. Among authors: diaz e. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13. ACS Med Chem Lett. 2012. PMID: 24900432 Free PMC article.
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Schulte CA, Deaton DN, Diaz E, Do Y, Gampe RT, Guss JH, Hancock AP, Hobbs H, Hodgson ST, Holt J, Jeune MR, Kahler KM, Kramer HF, Le J, Mortenson PN, Musetti C, Nolte RT, Orband-Miller LA, Peckham GE, Petrov KG, Pietrak BL, Poole C, Price DJ, Saxty G, Shillings A, Smalley TL Jr, Somers DO, Stewart EL, Stuart JD, Thomson SA. Schulte CA, et al. Among authors: diaz e. Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991628
1,448 results