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Items: 1 to 50 of 207

1.

RNA-modifying proteins as anticancer drug targets.

Boriack-Sjodin PA, Ribich S, Copeland RA.

Nat Rev Drug Discov. 2018 May 18. doi: 10.1038/nrd.2018.71. [Epub ahead of print] Review.

PMID:
29773918
2.

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.

3.

Protein methyltransferase inhibitors as precision cancer therapeutics: a decade of discovery.

Copeland RA.

Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748). pii: 20170080. doi: 10.1098/rstb.2017.0080. Review.

4.

Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study.

Italiano A, Soria JC, Toulmonde M, Michot JM, Lucchesi C, Varga A, Coindre JM, Blakemore SJ, Clawson A, Suttle B, McDonald AA, Woodruff M, Ribich S, Hedrick E, Keilhack H, Thomson B, Owa T, Copeland RA, Ho PTC, Ribrag V.

Lancet Oncol. 2018 May;19(5):649-659. doi: 10.1016/S1470-2045(18)30145-1. Epub 2018 Apr 9.

PMID:
29650362
5.

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.

Drew AE, Moradei O, Jacques SL, Rioux N, Boriack-Sjodin AP, Allain C, Scott MP, Jin L, Raimondi A, Handler JL, Ott HM, Kruger RG, McCabe MT, Sneeringer C, Riera T, Shapiro G, Waters NJ, Mitchell LH, Duncan KW, Moyer MP, Copeland RA, Smith J, Chesworth R, Ribich SA.

Sci Rep. 2017 Dec 21;7(1):17993. doi: 10.1038/s41598-017-18446-z.

6.

The Elements of Translational Chemical Biology.

Copeland RA, Boriack-Sjodin PA.

Cell Chem Biol. 2018 Feb 15;25(2):128-134. doi: 10.1016/j.chembiol.2017.11.003. Epub 2017 Dec 7. Review.

PMID:
29233521
7.

Drug Discovery and Chemical Biology of Cancer Epigenetics.

Ribich S, Harvey D, Copeland RA.

Cell Chem Biol. 2017 Sep 21;24(9):1120-1147. doi: 10.1016/j.chembiol.2017.08.020. Review.

PMID:
28938089
8.

EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL.

Brach D, Johnston-Blackwell D, Drew A, Lingaraj T, Motwani V, Warholic NM, Feldman I, Plescia C, Smith JJ, Copeland RA, Keilhack H, Chan-Penebre E, Knutson SK, Ribich SA, Raimondi A, Thomenius MJ.

Mol Cancer Ther. 2017 Nov;16(11):2586-2597. doi: 10.1158/1535-7163.MCT-16-0840. Epub 2017 Aug 23.

PMID:
28835384
9.

Mechanisms of Pinometostat (EPZ-5676) Treatment-Emergent Resistance in MLL-Rearranged Leukemia.

Campbell CT, Haladyna JN, Drubin DA, Thomson TM, Maria MJ, Yamauchi T, Waters NJ, Olhava EJ, Pollock RM, Smith JJ, Copeland RA, Blakemore SJ, Bernt KM, Daigle SR.

Mol Cancer Ther. 2017 Aug;16(8):1669-1679. doi: 10.1158/1535-7163.MCT-16-0693. Epub 2017 Apr 20.

PMID:
28428443
10.

Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models.

Chan-Penebre E, Armstrong K, Drew A, Grassian AR, Feldman I, Knutson SK, Kuplast-Barr K, Roche M, Campbell J, Ho P, Copeland RA, Chesworth R, Smith JJ, Keilhack H, Ribich SA.

Mol Cancer Ther. 2017 May;16(5):850-860. doi: 10.1158/1535-7163.MCT-16-0678. Epub 2017 Mar 14.

11.

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.

12.

Drug-target interaction kinetics: underutilized in drug optimization?

Copeland RA.

Future Med Chem. 2016 Dec;8(18):2173-2175. Epub 2016 Nov 15. No abstract available.

PMID:
27845591
13.

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 JS, Kuntz KK, Ribich S, Minoshima Y, Matsui J, Copeland RA, Tanaka S, Keilhack H.

PLoS One. 2016 Jul 8;11(7):e0158888. doi: 10.1371/journal.pone.0158888. eCollection 2016. Erratum in: PLoS One. 2017 Jan 13;12 (1):e0170539.

14.

Characterization of Inhibitor Binding Through Multiple Inhibitor Analysis: A Novel Local Fitting Method.

Riera TV, Wigle TJ, Copeland RA.

Methods Mol Biol. 2016;1439:33-45. doi: 10.1007/978-1-4939-3673-1_2.

PMID:
27316986
15.

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.

Duncan KW, Rioux N, Boriack-Sjodin PA, Munchhof MJ, Reiter LA, Majer CR, Jin L, Johnston LD, Chan-Penebre E, Kuplast KG, Porter Scott M, Pollock RM, Waters NJ, Smith JJ, Moyer MP, Copeland RA, Chesworth R.

ACS Med Chem Lett. 2015 Dec 2;7(2):162-6. doi: 10.1021/acsmedchemlett.5b00380. eCollection 2016 Feb 11.

16.

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.

17.

Epigenetic Medicinal Chemistry.

Copeland RA.

ACS Med Chem Lett. 2015 Dec 10;7(2):124-7. doi: 10.1021/acsmedchemlett.5b00462. eCollection 2016 Feb 11.

18.

CARM1 Preferentially Methylates H3R17 over H3R26 through a Random Kinetic Mechanism.

Jacques SL, Aquino KP, Gureasko J, Boriack-Sjodin PA, Porter Scott M, Copeland RA, Riera TV.

Biochemistry. 2016 Mar 22;55(11):1635-44. doi: 10.1021/acs.biochem.5b01071. Epub 2016 Feb 5.

PMID:
26848779
19.

PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and Disease.

Kadoch C, Copeland RA, Keilhack H.

Biochemistry. 2016 Mar 22;55(11):1600-14. doi: 10.1021/acs.biochem.5b01191. Epub 2016 Feb 17. Review.

PMID:
26836503
20.

Characterization of the Enzymatic Activity of SETDB1 and Its 1:1 Complex with ATF7IP.

Basavapathruni A, Gureasko J, Porter Scott M, Hermans W, Godbole A, Leland PA, Boriack-Sjodin PA, Wigle TJ, Copeland RA, Riera TV.

Biochemistry. 2016 Mar 22;55(11):1645-51. doi: 10.1021/acs.biochem.5b01202. Epub 2016 Feb 11.

PMID:
26813693
21.

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.

PMID:
26769278
22.

The Biochemistry of Chromatin Remodeling.

Copeland RA.

Biochemistry. 2016 Mar 22;55(11):1555-6. doi: 10.1021/acs.biochem.6b00014. Epub 2016 Jan 22. No abstract available.

PMID:
26745206
23.

The drug-target residence time model: a 10-year retrospective.

Copeland RA.

Nat Rev Drug Discov. 2016 Feb;15(2):87-95. doi: 10.1038/nrd.2015.18. Epub 2015 Dec 18. Review.

PMID:
26678621
24.

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.

25.

Structural Insights into Ternary Complex Formation of Human CARM1 with Various Substrates.

Boriack-Sjodin PA, Jin L, Jacques SL, Drew A, Sneeringer C, Scott MP, Moyer MP, Ribich S, Moradei O, Copeland RA.

ACS Chem Biol. 2016 Mar 18;11(3):763-71. doi: 10.1021/acschembio.5b00773. Epub 2015 Nov 23.

PMID:
26551522
26.

Corrigendum: The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Nov;11(11):887. doi: 10.1038/nchembio1115-887c. No abstract available.

PMID:
26485080
27.

Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor.

Rioux N, Duncan KW, Lantz RJ, Miao X, Chan-Penebre E, Moyer MP, Munchhof MJ, Copeland RA, Chesworth R, Waters NJ.

Xenobiotica. 2016;46(3):268-77.

PMID:
26294260
28.

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. No abstract available. Erratum in: Nat Chem Biol. 2015 Nov;11(11):887. Nat Chem Biol. 2015 Aug;11(8):541. Roth, Brian [Corrected to Roth, Bryan] and Frederiksen, Mathias [Added].

29.

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.

Mitchell LH, Drew AE, Ribich SA, Rioux N, Swinger KK, Jacques SL, Lingaraj T, Boriack-Sjodin PA, Waters NJ, Wigle TJ, Moradei O, Jin L, Riera T, Porter-Scott M, Moyer MP, Smith JJ, Chesworth R, Copeland RA.

ACS Med Chem Lett. 2015 Apr 6;6(6):655-9. doi: 10.1021/acsmedchemlett.5b00071. eCollection 2015 Jun 11.

30.

Drug-target interactions: Stay tuned.

Copeland RA.

Nat Chem Biol. 2015 Jul;11(7):451-2. doi: 10.1038/nchembio.1831. Epub 2015 May 25. No abstract available.

PMID:
26006012
31.

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.

32.

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.

Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K, Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O, Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland RA, Chesworth R, Duncan KW.

Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27.

PMID:
25915199
33.

Structural and Kinetic Characterization of a Novel N-acetylated Aliphatic Amine Metabolite of the PRMT Inhibitor, EPZ011652.

Rioux N, Mitchell LH, Tiller P, Plant K, Shaw J, Frost K, Ribich S, Moyer MP, Copeland RA, Chesworth R, Waters NJ.

Drug Metab Dispos. 2015 Jul;43(7):936-43. doi: 10.1124/dmd.115.064014. Epub 2015 Apr 17.

34.

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.

PMID:
25755264
35.

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.

36.

Small molecule control of chromatin remodeling.

Finley A, Copeland RA.

Chem Biol. 2014 Sep 18;21(9):1196-210. doi: 10.1016/j.chembiol.2014.07.024. Review.

37.

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.

PMID:
25154026
38.

O2(b(1)Σ(+)(g), υ = 0, 1) relative yields in O((1)D) + O2 energy transfer.

Pejaković DA, Copeland RA, Slanger TG, Kalogerakis KS.

J Chem Phys. 2014 Jul 14;141(2):024303. doi: 10.1063/1.4885721.

PMID:
25028015
39.

DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells.

Klaus CR, Iwanowicz D, Johnston D, Campbell CA, Smith JJ, Moyer MP, Copeland RA, Olhava EJ, Scott MP, Pollock RM, Daigle SR, Raimondi A.

J Pharmacol Exp Ther. 2014 Sep;350(3):646-56. doi: 10.1124/jpet.114.214577. Epub 2014 Jul 3.

40.

Targeting epigenetic regulators for cancer therapy.

Wee S, Dhanak D, Li H, Armstrong SA, Copeland RA, Sims R, Baylin SB, Liu XS, Schweizer L.

Ann N Y Acad Sci. 2014 Feb;1309:30-6. doi: 10.1111/nyas.12356. Review.

PMID:
24571255
41.

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.

42.

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.

Basavapathruni A, Olhava EJ, Daigle SR, Therkelsen CA, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Dovletoglou A, Richon VM, Pollock RM, Copeland RA, Moyer MP, Chesworth R, Pearson PG, Waters NJ.

Biopharm Drug Dispos. 2014 May;35(4):237-52. doi: 10.1002/bdd.1889. Epub 2014 Feb 14.

PMID:
24415392
43.

Molecular pathways: protein methyltransferases in cancer.

Copeland RA.

Clin Cancer Res. 2013 Dec 1;19(23):6344-50. doi: 10.1158/1078-0432.CCR-13-0223. Epub 2013 Aug 19. Review.

44.

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.

Daigle SR, Olhava EJ, Therkelsen CA, Basavapathruni A, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Waters NJ, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM.

Blood. 2013 Aug 8;122(6):1017-25. doi: 10.1182/blood-2013-04-497644. Epub 2013 Jun 25.

45.

Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys²⁷ methylation by human polycomb repressive complex 2 and vSET.

Swalm BM, Hallenbeck KK, Majer CR, Jin L, Scott MP, Moyer MP, Copeland RA, Wigle TJ.

Biochem J. 2013 Jul 15;453(2):241-7. doi: 10.1042/BJ20130439.

PMID:
23679895
46.

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.

47.

Drugging the human methylome: an emerging modality for reversible control of aberrant gene transcription.

Wigle TJ, Copeland RA.

Curr Opin Chem Biol. 2013 Jun;17(3):369-78. doi: 10.1016/j.cbpa.2013.03.035. Epub 2013 Apr 23. Review.

PMID:
23619004
48.

Targeting genetic alterations in protein methyltransferases for personalized cancer therapeutics.

Copeland RA, Moyer MP, Richon VM.

Oncogene. 2013 Feb 21;32(8):939-46. doi: 10.1038/onc.2012.552. Epub 2012 Nov 19. Review.

49.

Socioeconomic disparities in cataract surgery.

Desai N, Copeland RA.

Curr Opin Ophthalmol. 2013 Jan;24(1):74-8. doi: 10.1097/ICU.0b013e32835a93da. Review.

PMID:
23108314
50.

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.

PMID:
23023262

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