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Items: 25


Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.

Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA.

PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018.


Identification of a peptide inhibitor for the histone methyltransferase WHSC1.

Morrison MJ, Boriack-Sjodin PA, Swinger KK, Wigle TJ, Sadalge D, Kuntz KW, Scott MP, Janzen WP, Chesworth R, Duncan KW, Harvey DM, Lampe JW, Mitchell LH, Copeland RA.

PLoS One. 2018 May 9;13(5):e0197082. doi: 10.1371/journal.pone.0197082. eCollection 2018.


Correction: Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma.

Kawano S, Grassian AR, Tsuda M, Knutson SK, Warholic NM, Kuznetsov G, Xu S, Xiao Y, Pollock RM, Smith JJ, Kuntz KW, Ribich S, Minoshima Y, Matsui J, Copeland RA, Tanaka S, Keilhack H.

PLoS One. 2017 Jan 13;12(1):e0170539. doi: 10.1371/journal.pone.0170539. eCollection 2017.


Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Mitchell LH, Boriack-Sjodin PA, Smith S, Thomenius M, Rioux N, Munchhof M, Mills JE, Klaus C, Totman J, Riera TV, Raimondi A, Jacques SL, West K, Foley M, Waters NJ, Kuntz KW, Wigle TJ, Scott MP, Copeland RA, Smith JJ, Chesworth R.

ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. doi: 10.1021/acsmedchemlett.5b00272. eCollection 2016 Feb 11.


The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.

Kuntz KW, Campbell JE, Keilhack H, Pollock RM, Knutson SK, Porter-Scott M, Richon VM, Sneeringer CJ, Wigle TJ, Allain CJ, Majer CR, Moyer MP, Copeland RA, Chesworth R.

J Med Chem. 2016 Feb 25;59(4):1556-64. doi: 10.1021/acs.jmedchem.5b01501. Epub 2016 Jan 27.


A Medium-Throughput Single Cell CRISPR-Cas9 Assay to Assess Gene Essentiality.

Grassian AR, Scales TME, Knutson SK, Kuntz KW, McCarthy NJ, Lowe CE, Moore JD, Copeland RA, Keilhack H, Smith JJ, Wickenden JA, Ribich S.

Biol Proced Online. 2015 Nov 14;17:15. doi: 10.1186/s12575-015-0028-4. eCollection 2015.


EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

Campbell JE, Kuntz KW, Knutson SK, Warholic NM, Keilhack H, Wigle TJ, Raimondi A, Klaus CR, Rioux N, Yokoi A, Kawano S, Minoshima Y, Choi HW, Porter Scott M, Waters NJ, Smith JJ, Chesworth R, Moyer MP, Copeland RA.

ACS Med Chem Lett. 2015 Mar 4;6(5):491-5. doi: 10.1021/acsmedchemlett.5b00037. eCollection 2015 May 14.


A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening.

Wigle TJ, Swinger KK, Campbell JE, Scholle MD, Sherrill J, Admirand EA, Boriack-Sjodin PA, Kuntz KW, Chesworth R, Moyer MP, Scott MP, Copeland RA.

J Biomol Screen. 2015 Jul;20(6):810-20. doi: 10.1177/1087057115575689. Epub 2015 Mar 9.


Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas.

Knutson SK, Warholic NM, Johnston LD, Klaus CR, Wigle TJ, Iwanowicz D, Littlefield BA, Porter-Scott M, Smith JJ, Moyer MP, Copeland RA, Pollock RM, Kuntz KW, Raimondi A, Keilhack H.

PLoS One. 2014 Dec 10;9(12):e111840. doi: 10.1371/journal.pone.0111840. eCollection 2014.


Reaction coupling between wild-type and disease-associated mutant EZH2.

Swalm BM, Knutson SK, Warholic NM, Jin L, Kuntz KW, Keilhack H, Smith JJ, Pollock RM, Moyer MP, Scott MP, Copeland RA, Wigle TJ.

ACS Chem Biol. 2014 Nov 21;9(11):2459-64. doi: 10.1021/cb500548b. Epub 2014 Aug 28.


Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.

Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H.

Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21.


Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.

Knutson SK, Warholic NM, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Porter Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM, Kuntz KW, Keilhack H.

Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. doi: 10.1073/pnas.1303800110. Epub 2013 Apr 25.


A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.

Knutson SK, Wigle TJ, Warholic NM, Sneeringer CJ, Allain CJ, Klaus CR, Sacks JD, Raimondi A, Majer CR, Song J, Scott MP, Jin L, Smith JJ, Olhava EJ, Chesworth R, Moyer MP, Richon VM, Copeland RA, Keilhack H, Pollock RM, Kuntz KW.

Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30.


Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L.

Basavapathruni A, Jin L, Daigle SR, Majer CR, Therkelsen CA, Wigle TJ, Kuntz KW, Chesworth R, Pollock RM, Scott MP, Moyer MP, Richon VM, Copeland RA, Olhava EJ.

Chem Biol Drug Des. 2012 Dec;80(6):971-80. doi: 10.1111/cbdd.12050. Epub 2012 Oct 9.


A687V EZH2 is a gain-of-function mutation found in lymphoma patients.

Majer CR, Jin L, Scott MP, Knutson SK, Kuntz KW, Keilhack H, Smith JJ, Moyer MP, Richon VM, Copeland RA, Wigle TJ.

FEBS Lett. 2012 Sep 21;586(19):3448-51. doi: 10.1016/j.febslet.2012.07.066. Epub 2012 Jul 28.


The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states.

Wigle TJ, Knutson SK, Jin L, Kuntz KW, Pollock RM, Richon VM, Copeland RA, Scott MP.

FEBS Lett. 2011 Oct 3;585(19):3011-4. doi: 10.1016/j.febslet.2011.08.018. Epub 2011 Aug 17.


Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.

Daigle SR, Olhava EJ, Therkelsen CA, Majer CR, Sneeringer CJ, Song J, Johnston LD, Scott MP, Smith JJ, Xiao Y, Jin L, Kuntz KW, Chesworth R, Moyer MP, Bernt KM, Tseng JC, Kung AL, Armstrong SA, Copeland RA, Richon VM, Pollock RM.

Cancer Cell. 2011 Jul 12;20(1):53-65. doi: 10.1016/j.ccr.2011.06.009.


Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas.

Sneeringer CJ, Scott MP, Kuntz KW, Knutson SK, Pollock RM, Richon VM, Copeland RA.

Proc Natl Acad Sci U S A. 2010 Dec 7;107(49):20980-5. doi: 10.1073/pnas.1012525107. Epub 2010 Nov 15.


Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.

Emmitte KA, Adjabeng GM, Andrews CW, Alberti JG, Bambal R, Chamberlain SD, Davis-Ward RG, Dickson HD, Hassler DF, Hornberger KR, Jackson JR, Kuntz KW, Lansing TJ, Mook RA Jr, Nailor KE, Pobanz MA, Smith SC, Sung CM, Cheung M.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1694-7. doi: 10.1016/j.bmcl.2009.01.094. Epub 2009 Jan 31. Erratum in: Bioorg Med Chem Lett. 2009 May 1;19(9):2604. Adjebang, George M [corrected to Adjabeng, George M].


Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).

Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA Jr, Moorthy GS, Dickerson SH, Hassell AM, Leesnitzer MA, Shewchuk LM, Groy A, Rowand JL, Anderson K, Atkins CL, Yang J, Sabbatini P, Kumar R.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004-8. doi: 10.1016/j.bmcl.2008.11.058. Epub 2008 Nov 20.


Discovery of thiophene inhibitors of polo-like kinase.

Emmitte KA, Andrews CW, Badiang JG, Davis-Ward RG, Dickson HD, Drewry DH, Emerson HK, Epperly AH, Hassler DF, Knick VB, Kuntz KW, Lansing TJ, Linn JA, Mook RA Jr, Nailor KE, Salovich JM, Spehar GM, Cheung M.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):1018-21. doi: 10.1016/j.bmcl.2008.11.041. Epub 2008 Nov 18.


Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.

Cheung M, Kuntz KW, Pobanz M, Salovich JM, Wilson BJ, Andrews CW 3rd, Shewchuk LM, Epperly AH, Hassler DF, Leesnitzer MA, Smith JL, Smith GK, Lansing TJ, Mook RA Jr.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6214-7. doi: 10.1016/j.bmcl.2008.09.100. Epub 2008 Oct 2.


Total synthesis of anti-HIV agent chloropeptin I.

Deng H, Jung JK, Liu T, Kuntz KW, Snapper ML, Hoveyda AH.

J Am Chem Soc. 2003 Jul 30;125(30):9032-4.


Mechanism of enantioselective Ti-catalyzed Strecker reaction: peptide-based metal complexes as bifunctional catalysts.

Josephsohn NS, Kuntz KW, Snapper ML, Hoveyda AH.

J Am Chem Soc. 2001 Nov 28;123(47):11594-9.


Combinatorial catalyst discovery.

Kuntz KW, Snapper ML, Hoveyda AH.

Curr Opin Chem Biol. 1999 Jun;3(3):313-9. Review.


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