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Items: 1 to 50 of 101

1.

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
2.

CCR 20th Anniversary Commentary: Vorinostat-Gateway to Epigenetic Therapy.

Kelly WK, Marks P, Richon VM.

Clin Cancer Res. 2015 May 15;21(10):2198-200. doi: 10.1158/1078-0432.CCR-14-2556.

3.

Redox-Mediated Suberoylanilide Hydroxamic Acid Sensitivity in Breast Cancer.

Chiaradonna F, Barozzi I, Miccolo C, Bucci G, Palorini R, Fornasari L, Botrugno OA, Pruneri G, Masullo M, Passafaro A, Galimberti VE, Fantin VR, Richon VM, Pece S, Viale G, Di Fiore PP, Draetta G, Pelicci PG, Minucci S, Chiocca S.

Antioxid Redox Signal. 2015 Jul 1;23(1):15-29. doi: 10.1089/ars.2014.6189. Epub 2015 May 27.

4.

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.

5.

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
6.

Drug discovery in rare indications: opportunities and challenges.

Richon VM.

Hematology Am Soc Hematol Educ Program. 2013;2013:19-23. doi: 10.1182/asheducation-2013.1.19. Review.

PMID:
24319157
7.

Molecular and biologic analysis of histone deacetylase inhibitors with diverse specificities.

Newbold A, Matthews GM, Bots M, Cluse LA, Clarke CJ, Banks KM, Cullinane C, Bolden JE, Christiansen AJ, Dickins RA, Miccolo C, Chiocca S, Kral AM, Ozerova ND, Miller TA, Methot JL, Richon VM, Secrist JP, Minucci S, Johnstone RW.

Mol Cancer Ther. 2013 Dec;12(12):2709-21. doi: 10.1158/1535-7163.MCT-13-0626. Epub 2013 Oct 3.

8.

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.

9.

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.

10.

Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l.

Deshpande AJ, Chen L, Fazio M, Sinha AU, Bernt KM, Banka D, Dias S, Chang J, Olhava EJ, Daigle SR, Richon VM, Pollock RM, Armstrong SA.

Blood. 2013 Mar 28;121(13):2533-41. doi: 10.1182/blood-2012-11-465120. Epub 2013 Jan 29.

11.

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.

12.

Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l.

Chen L, Deshpande AJ, Banka D, Bernt KM, Dias S, Buske C, Olhava EJ, Daigle SR, Richon VM, Pollock RM, Armstrong SA.

Leukemia. 2013 Apr;27(4):813-22. doi: 10.1038/leu.2012.327. Epub 2012 Nov 9.

13.

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
14.

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.

PMID:
22978415
15.

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.

16.

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.

17.

MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L.

Bernt KM, Zhu N, Sinha AU, Vempati S, Faber J, Krivtsov AV, Feng Z, Punt N, Daigle A, Bullinger L, Pollock RM, Richon VM, Kung AL, Armstrong SA.

Cancer Cell. 2011 Jul 12;20(1):66-78. doi: 10.1016/j.ccr.2011.06.010.

18.

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.

19.

Chemogenetic analysis of human protein methyltransferases.

Richon VM, Johnston D, Sneeringer CJ, Jin L, Majer CR, Elliston K, Jerva LF, Scott MP, Copeland RA.

Chem Biol Drug Des. 2011 Aug;78(2):199-210. doi: 10.1111/j.1747-0285.2011.01135.x. Epub 2011 Jun 16.

PMID:
21564555
20.

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.

21.

Targeting histone deacetylases: development of vorinostat for the treatment of cancer.

Richon VM.

Epigenomics. 2010 Jun;2(3):457-65. doi: 10.2217/epi.10.20. Review.

PMID:
22121904
22.

Nonclinical safety assessment of the histone deacetylase inhibitor vorinostat.

Kerr JS, Galloway S, Lagrutta A, Armstrong M, Miller T, Richon VM, Andrews PA.

Int J Toxicol. 2010 Jan-Feb;29(1):3-19. doi: 10.1177/1091581809352111. Epub 2009 Nov 10.

PMID:
19903873
23.

Vorinostat inhibits brain metastatic colonization in a model of triple-negative breast cancer and induces DNA double-strand breaks.

Palmieri D, Lockman PR, Thomas FC, Hua E, Herring J, Hargrave E, Johnson M, Flores N, Qian Y, Vega-Valle E, Taskar KS, Rudraraju V, Mittapalli RK, Gaasch JA, Bohn KA, Thorsheim HR, Liewehr DJ, Davis S, Reilly JF, Walker R, Bronder JL, Feigenbaum L, Steinberg SM, Camphausen K, Meltzer PS, Richon VM, Smith QR, Steeg PS.

Clin Cancer Res. 2009 Oct 1;15(19):6148-57. doi: 10.1158/1078-0432.CCR-09-1039. Epub 2009 Sep 29.

24.

Protein methyltransferases as a target class for drug discovery.

Copeland RA, Solomon ME, Richon VM.

Nat Rev Drug Discov. 2009 Sep;8(9):724-32. doi: 10.1038/nrd2974. Review.

PMID:
19721445
25.

Vorinostat in solid and hematologic malignancies.

Siegel D, Hussein M, Belani C, Robert F, Galanis E, Richon VM, Garcia-Vargas J, Sanz-Rodriguez C, Rizvi S.

J Hematol Oncol. 2009 Jul 27;2:31. doi: 10.1186/1756-8722-2-31. Review.

26.

Inhibition of NOTCH signaling by gamma secretase inhibitor engages the RB pathway and elicits cell cycle exit in T-cell acute lymphoblastic leukemia cells.

Rao SS, O'Neil J, Liberator CD, Hardwick JS, Dai X, Zhang T, Tyminski E, Yuan J, Kohl NE, Richon VM, Van der Ploeg LH, Carroll PM, Draetta GF, Look AT, Strack PR, Winter CG.

Cancer Res. 2009 Apr 1;69(7):3060-8. doi: 10.1158/0008-5472.CAN-08-4295. Epub 2009 Mar 24.

27.

Phase II trial of vorinostat in recurrent glioblastoma multiforme: a north central cancer treatment group study.

Galanis E, Jaeckle KA, Maurer MJ, Reid JM, Ames MM, Hardwick JS, Reilly JF, Loboda A, Nebozhyn M, Fantin VR, Richon VM, Scheithauer B, Giannini C, Flynn PJ, Moore DF Jr, Zwiebel J, Buckner JC.

J Clin Oncol. 2009 Apr 20;27(12):2052-8. doi: 10.1200/JCO.2008.19.0694. Epub 2009 Mar 23. Erratum in: J Clin Oncol. 2009 Jul 1;27(19):3262-3.

28.

Development of vorinostat: current applications and future perspectives for cancer therapy.

Richon VM, Garcia-Vargas J, Hardwick JS.

Cancer Lett. 2009 Aug 8;280(2):201-10. doi: 10.1016/j.canlet.2009.01.002. Epub 2009 Jan 31. Review.

PMID:
19181442
29.

Control of cell growth and survival by enzymes of the fatty acid synthesis pathway in HCT-116 colon cancer cells.

Zhan Y, Ginanni N, Tota MR, Wu M, Bays NW, Richon VM, Kohl NE, Bachman ES, Strack PR, Krauss S.

Clin Cancer Res. 2008 Sep 15;14(18):5735-42. doi: 10.1158/1078-0432.CCR-07-5074.

30.

A new path to the cancer epigenome.

Richon VM.

Nat Biotechnol. 2008 Jun;26(6):655-6. doi: 10.1038/nbt0608-655. No abstract available.

PMID:
18536689
31.

Constitutive activation of signal transducers and activators of transcription predicts vorinostat resistance in cutaneous T-cell lymphoma.

Fantin VR, Loboda A, Paweletz CP, Hendrickson RC, Pierce JW, Roth JA, Li L, Gooden F, Korenchuk S, Hou XS, Harrington EA, Randolph S, Reilly JF, Ware CM, Kadin ME, Frankel SR, Richon VM.

Cancer Res. 2008 May 15;68(10):3785-94. doi: 10.1158/0008-5472.CAN-07-6091.

32.

Mechanisms of resistance to histone deacetylase inhibitors and their therapeutic implications.

Fantin VR, Richon VM.

Clin Cancer Res. 2007 Dec 15;13(24):7237-42. Review.

33.

Phase 1 study of the histone deacetylase inhibitor vorinostat (suberoylanilide hydroxamic acid [SAHA]) in patients with advanced leukemias and myelodysplastic syndromes.

Garcia-Manero G, Yang H, Bueso-Ramos C, Ferrajoli A, Cortes J, Wierda WG, Faderl S, Koller C, Morris G, Rosner G, Loboda A, Fantin VR, Randolph SS, Hardwick JS, Reilly JF, Chen C, Ricker JL, Secrist JP, Richon VM, Frankel SR, Kantarjian HM.

Blood. 2008 Feb 1;111(3):1060-6. Epub 2007 Oct 25.

PMID:
17962510
34.

Analysis of the apoptotic and therapeutic activities of histone deacetylase inhibitors by using a mouse model of B cell lymphoma.

Lindemann RK, Newbold A, Whitecross KF, Cluse LA, Frew AJ, Ellis L, Williams S, Wiegmans AP, Dear AE, Scott CL, Pellegrini M, Wei A, Richon VM, Marks PA, Lowe SW, Smyth MJ, Johnstone RW.

Proc Natl Acad Sci U S A. 2007 May 8;104(19):8071-6. Epub 2007 Apr 30.

35.

Suberoylanilide hydroxamic acid (vorinostat) represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer cell proliferation.

Marrocco DL, Tilley WD, Bianco-Miotto T, Evdokiou A, Scher HI, Rifkind RA, Marks PA, Richon VM, Butler LM.

Mol Cancer Ther. 2007 Jan;6(1):51-60. Epub 2007 Jan 11.

36.

Phase 2 trial of oral vorinostat (suberoylanilide hydroxamic acid, SAHA) for refractory cutaneous T-cell lymphoma (CTCL).

Duvic M, Talpur R, Ni X, Zhang C, Hazarika P, Kelly C, Chiao JH, Reilly JF, Ricker JL, Richon VM, Frankel SR.

Blood. 2007 Jan 1;109(1):31-9. Epub 2006 Sep 7. Erratum in: Blood. 2007 Jun 15;109(12):5086.

37.
38.

Antileukemia activity of the combination of an anthracycline with a histone deacetylase inhibitor.

Sanchez-Gonzalez B, Yang H, Bueso-Ramos C, Hoshino K, Quintas-Cardama A, Richon VM, Garcia-Manero G.

Blood. 2006 Aug 15;108(4):1174-82. Epub 2006 May 4.

39.

Novel histone deacetylase inhibitors in the treatment of thyroid cancer.

Mitsiades CS, Poulaki V, McMullan C, Negri J, Fanourakis G, Goudopoulou A, Richon VM, Marks PA, Mitsiades N.

Clin Cancer Res. 2005 May 15;11(10):3958-65.

40.

Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer.

Kelly WK, O'Connor OA, Krug LM, Chiao JH, Heaney M, Curley T, MacGregore-Cortelli B, Tong W, Secrist JP, Schwartz L, Richardson S, Chu E, Olgac S, Marks PA, Scher H, Richon VM.

J Clin Oncol. 2005 Jun 10;23(17):3923-31. Epub 2005 May 16.

41.

Identification and functional significance of genes regulated by structurally different histone deacetylase inhibitors.

Peart MJ, Smyth GK, van Laar RK, Bowtell DD, Richon VM, Marks PA, Holloway AJ, Johnstone RW.

Proc Natl Acad Sci U S A. 2005 Mar 8;102(10):3697-702. Epub 2005 Feb 28.

42.

Modulation of renal disease in MRL/lpr mice by suberoylanilide hydroxamic acid.

Reilly CM, Mishra N, Miller JM, Joshi D, Ruiz P, Richon VM, Marks PA, Gilkeson GS.

J Immunol. 2004 Sep 15;173(6):4171-8.

43.

Histone deacetylase inhibitors.

Marks PA, Richon VM, Miller T, Kelly WK.

Adv Cancer Res. 2004;91:137-68. Review.

PMID:
15327890
44.

Histone deacetylase inhibitors: development as cancer therapy.

Marks PA, Richon VM, Kelly WK, Chiao JH, Miller T.

Novartis Found Symp. 2004;259:269-81; discussion 281-8.

PMID:
15171260
45.

Histone deacetylase inhibitors: assays to assess effectiveness in vitro and in vivo.

Richon VM, Zhou X, Secrist JP, Cordon-Cardo C, Kelly WK, Drobnjak M, Marks PA.

Methods Enzymol. 2004;376:199-205. Review. No abstract available.

PMID:
14975307
46.

HDAC inhibitors for the treatment of cancer.

Secrist JP, Zhou X, Richon VM.

Curr Opin Investig Drugs. 2003 Dec;4(12):1422-7. Review.

PMID:
14763127
47.

Histone deacetylase (HDAC) inhibitor activation of p21WAF1 involves changes in promoter-associated proteins, including HDAC1.

Gui CY, Ngo L, Xu WS, Richon VM, Marks PA.

Proc Natl Acad Sci U S A. 2004 Feb 3;101(5):1241-6. Epub 2004 Jan 20.

48.

Transcriptional signature of histone deacetylase inhibition in multiple myeloma: biological and clinical implications.

Mitsiades CS, Mitsiades NS, McMullan CJ, Poulaki V, Shringarpure R, Hideshima T, Akiyama M, Chauhan D, Munshi N, Gu X, Bailey C, Joseph M, Libermann TA, Richon VM, Marks PA, Anderson KC.

Proc Natl Acad Sci U S A. 2004 Jan 13;101(2):540-5. Epub 2003 Dec 26.

49.

Histone deacetylase inhibitors induce growth suppression and cell death in human rhabdomyosarcoma in vitro.

Kutko MC, Glick RD, Butler LM, Coffey DC, Rifkind RA, Marks PA, Richon VM, LaQuaglia MP.

Clin Cancer Res. 2003 Nov 15;9(15):5749-55.

50.

Phase I clinical trial of histone deacetylase inhibitor: suberoylanilide hydroxamic acid administered intravenously.

Kelly WK, Richon VM, O'Connor O, Curley T, MacGregor-Curtelli B, Tong W, Klang M, Schwartz L, Richardson S, Rosa E, Drobnjak M, Cordon-Cordo C, Chiao JH, Rifkind R, Marks PA, Scher H.

Clin Cancer Res. 2003 Sep 1;9(10 Pt 1):3578-88.

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