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Page 1
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: brandt m. ACS Chem Biol. 2014 Mar 21;9(3):622-9. doi: 10.1021/cb4008748. Epub 2013 Dec 31. ACS Chem Biol. 2014. PMID: 24304166
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. Among authors: brandt m. J Biomol Screen. 2012 Dec;17(10):1279-92. doi: 10.1177/1087057112453765. Epub 2012 Aug 17. J Biomol Screen. 2012. PMID: 22904200
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: brandt m. Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10. Nature. 2012. PMID: 23051747
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: brandt m. 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.
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: brandt m. Nat Chem Biol. 2014 Mar;10(3):181-7. doi: 10.1038/nchembio.1427. Epub 2014 Jan 5. Nat Chem Biol. 2014. PMID: 24390428
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: brandt m. J Biomol Screen. 2007 Sep;12(6):881-90. doi: 10.1177/1087057107304113. Epub 2007 Jun 19. J Biomol Screen. 2007. PMID: 17579124
Development of a high-throughput screen to detect inhibitors of TRPS1 sumoylation.
Brandt M, Szewczuk LM, Zhang H, Hong X, McCormick PM, Lewis TS, Graham TI, Hung ST, Harper-Jones AD, Kerrigan JJ, Wang DY, Dul E, Hou W, Ho TF, Meek TD, Cheung MH, Johanson KO, Jones CS, Schwartz B, Kumar S, Oliff AI, Kirkpatrick RB. Brandt M, et al. Assay Drug Dev Technol. 2013 Jun;11(5):308-25. doi: 10.1089/adt.2012.501. Assay Drug Dev Technol. 2013. PMID: 23772552
Baculovirus production of fully-active phosphoinositide 3-kinase alpha as a p85alpha-p110alpha fusion for X-ray crystallographic analysis with ATP competitive enzyme inhibitors.
Sinnamon RH, McDevitt P, Pietrak BL, Leydon VR, Xue Y, Lehr R, Qi H, Burns M, Elkins P, Ward P, Vincentini G, Fisher D, Grimes M, Brandt M, Auger KR, Ho T, Johanson K, Jones CS, Schwartz B, Sweitzer TD, Kirkpatrick RB. Sinnamon RH, et al. Among authors: brandt m. Protein Expr Purif. 2010 Oct;73(2):167-76. doi: 10.1016/j.pep.2010.05.002. Epub 2010 May 10. Protein Expr Purif. 2010. PMID: 20457255
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.
Hirst DJ, Brandt M, Bruton G, Christodoulou E, Cutler L, Deeks N, Goodacre JD, Jack T, Lindon M, Miah A, Page K, Parr N, Shukla L, Sims M, Thomas P, Thorpe J, Holmes DS. Hirst DJ, et al. Among authors: brandt m. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127533. doi: 10.1016/j.bmcl.2020.127533. Epub 2020 Sep 10. Bioorg Med Chem Lett. 2020. PMID: 32919012
1,656 results