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Items: 42

1.

Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) Inhibitor GSK2816126 in Patients with Advanced Hematologic and Solid Tumors.

Yap TA, Winter JN, Giulino-Roth L, Longley J, Lopez J, Michot JM, Leonard JP, Ribrag V, McCabe MT, Creasy CL, Stern M, Pene Dumitrescu T, Wang X, Frey S, Carver J, Horner T, Oh C, Khaled A, Dhar A, Johnson PWM.

Clin Cancer Res. 2019 Aug 30. doi: 10.1158/1078-0432.CCR-18-4121. [Epub ahead of print]

PMID:
31471312
2.

Rational Targeting of Cooperating Layers of the Epigenome Yields Enhanced Therapeutic Efficacy against AML.

Duy C, Teater M, Garrett-Bakelman FE, Lee TC, Meydan C, Glass JL, Li M, Hellmuth JC, Mohammad HP, Smitheman KN, Shih AH, Abdel-Wahab O, Tallman MS, Guzman ML, Muench D, Grimes HL, Roboz GJ, Kruger RG, Creasy CL, Paietta EM, Levine RL, Carroll M, Melnick AM.

Cancer Discov. 2019 Jul;9(7):872-889. doi: 10.1158/2159-8290.CD-19-0106. Epub 2019 May 10.

PMID:
31076479
3.

Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer.

Mohammad HP, Barbash O, Creasy CL.

Nat Med. 2019 Mar;25(3):403-418. doi: 10.1038/s41591-019-0376-8. Epub 2019 Mar 6. Review.

PMID:
30842676
4.

Efficacy and safety of trametinib in Japanese patients with advanced biliary tract cancers refractory to gemcitabine.

Ikeda M, Ioka T, Fukutomi A, Morizane C, Kasuga A, Takahashi H, Todaka A, Okusaka T, Creasy CL, Gorman S, Felitsky DJ, Kobayashi M, Zhang F, Furuse J.

Cancer Sci. 2018 Jan;109(1):215-224. doi: 10.1111/cas.13438. Epub 2017 Dec 9.

5.

A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1.

McNulty DE, Bonnette WG, Qi H, Wang L, Ho TF, Waszkiewicz A, Kallal LA, Nagarajan RP, Stern M, Quinn AM, Creasy CL, Su DS, Graves AP, Annan RS, Sweitzer SM, Holbert MA.

SLAS Discov. 2018 Jan;23(1):34-46. doi: 10.1177/2472555217732014. Epub 2017 Sep 28.

PMID:
28957646
6.

Untangling the role of mutant histone H3 in diffuse intrinsic pontine glioma.

Creasy CL.

Nat Med. 2017 Apr 7;23(4):413-414. doi: 10.1038/nm.4320. No abstract available.

PMID:
28388610
7.

Loss of tumor suppressor KDM6A amplifies PRC2-regulated transcriptional repression in bladder cancer and can be targeted through inhibition of EZH2.

Ler LD, Ghosh S, Chai X, Thike AA, Heng HL, Siew EY, Dey S, Koh LK, Lim JQ, Lim WK, Myint SS, Loh JL, Ong P, Sam XX, Huang D, Lim T, Tan PH, Nagarajan S, Cheng CW, Ho H, Ng LG, Yuen J, Lin PH, Chuang CK, Chang YH, Weng WH, Rozen SG, Tan P, Creasy CL, Pang ST, McCabe MT, Poon SL, Teh BT.

Sci Transl Med. 2017 Feb 22;9(378). pii: eaai8312. doi: 10.1126/scitranslmed.aai8312.

PMID:
28228601
8.

The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors.

Zingg D, Debbache J, Schaefer SM, Tuncer E, Frommel SC, Cheng P, Arenas-Ramirez N, Haeusel J, Zhang Y, Bonalli M, McCabe MT, Creasy CL, Levesque MP, Boyman O, Santoro R, Shakhova O, Dummer R, Sommer L.

Nat Commun. 2015 Jan 22;6:6051. doi: 10.1038/ncomms7051.

PMID:
25609585
9.

A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation.

Ott HM, Graves AP, Pappalardi MB, Huddleston M, Halsey WS, Hughes AM, Groy A, Dul E, Jiang Y, Bai Y, Annan R, Verma SK, Knight SD, Kruger RG, Dhanak D, Schwartz B, Tummino PJ, Creasy CL, McCabe MT.

Mol Cancer Ther. 2014 Dec;13(12):3062-73. doi: 10.1158/1535-7163.MCT-13-0876. Epub 2014 Sep 24.

10.

EZH2 as a potential target in cancer therapy.

McCabe MT, Creasy CL.

Epigenomics. 2014 Jun;6(3):341-51. doi: 10.2217/epi.14.23. Review.

PMID:
25111487
11.

Epigenomic alterations define lethal CIMP-positive ependymomas of infancy.

Mack SC, Witt H, Piro RM, Gu L, Zuyderduyn S, Stütz AM, Wang X, Gallo M, Garzia L, Zayne K, Zhang X, Ramaswamy V, Jäger N, Jones DT, Sill M, Pugh TJ, Ryzhova M, Wani KM, Shih DJ, Head R, Remke M, Bailey SD, Zichner T, Faria CC, Barszczyk M, Stark S, Seker-Cin H, Hutter S, Johann P, Bender S, Hovestadt V, Tzaridis T, Dubuc AM, Northcott PA, Peacock J, Bertrand KC, Agnihotri S, Cavalli FM, Clarke I, Nethery-Brokx K, Creasy CL, Verma SK, Koster J, Wu X, Yao Y, Milde T, Sin-Chan P, Zuccaro J, Lau L, Pereira S, Castelo-Branco P, Hirst M, Marra MA, Roberts SS, Fults D, Massimi L, Cho YJ, Van Meter T, Grajkowska W, Lach B, Kulozik AE, von Deimling A, Witt O, Scherer SW, Fan X, Muraszko KM, Kool M, Pomeroy SL, Gupta N, Phillips J, Huang A, Tabori U, Hawkins C, Malkin D, Kongkham PN, Weiss WA, Jabado N, Rutka JT, Bouffet E, Korbel JO, Lupien M, Aldape KD, Bader GD, Eils R, Lichter P, Dirks PB, Pfister SM, Korshunov A, Taylor MD.

Nature. 2014 Feb 27;506(7489):445-50. doi: 10.1038/nature13108. Epub 2014 Feb 19.

12.

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.

ACS Chem Biol. 2014 Mar 21;9(3):622-9. doi: 10.1021/cb4008748. Epub 2013 Dec 31.

PMID:
24304166
13.

Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.

Wyce A, Degenhardt Y, Bai Y, Le B, Korenchuk S, Crouthame MC, McHugh CF, Vessella R, Creasy CL, Tummino PJ, Barbash O.

Oncotarget. 2013 Dec;4(12):2419-29.

14.

EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation.

Béguelin W, Popovic R, Teater M, Jiang Y, Bunting KL, Rosen M, Shen H, Yang SN, Wang L, Ezponda T, Martinez-Garcia E, Zhang H, Zheng Y, Verma SK, McCabe MT, Ott HM, Van Aller GS, Kruger RG, Liu Y, McHugh CF, Scott DW, Chung YR, Kelleher N, Shaknovich R, Creasy CL, Gascoyne RD, Wong KK, Cerchietti L, Levine RL, Abdel-Wahab O, Licht JD, Elemento O, Melnick AM.

Cancer Cell. 2013 May 13;23(5):677-92. doi: 10.1016/j.ccr.2013.04.011.

15.

The tumor suppressor Mst1 promotes changes in the cellular redox state by phosphorylation and inactivation of peroxiredoxin-1 protein.

Rawat SJ, Creasy CL, Peterson JR, Chernoff J.

J Biol Chem. 2013 Mar 22;288(12):8762-71. doi: 10.1074/jbc.M112.414524. Epub 2013 Feb 5.

16.

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.

ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13.

17.

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.

Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10.

PMID:
23051747
18.

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.

J Biomol Screen. 2012 Dec;17(10):1279-92. doi: 10.1177/1087057112453765. Epub 2012 Aug 17.

PMID:
22904200
19.

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.

Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2989-94. doi: 10.1073/pnas.1116418109. Epub 2012 Feb 8.

20.

ALDH1A1 is a novel EZH2 target gene in epithelial ovarian cancer identified by genome-wide approaches.

Li H, Bitler BG, Vathipadiekal V, Maradeo ME, Slifker M, Creasy CL, Tummino PJ, Cairns P, Birrer MJ, Zhang R.

Cancer Prev Res (Phila). 2012 Mar;5(3):484-91. doi: 10.1158/1940-6207.CAPR-11-0414. Epub 2011 Dec 5.

21.

DYRK3 dual-specificity kinase attenuates erythropoiesis during anemia.

Bogacheva O, Bogachev O, Menon M, Dev A, Houde E, Valoret EI, Prosser HM, Creasy CL, Pickering SJ, Grau E, Rance K, Livi GP, Karur V, Erickson-Miller CL, Wojchowski DM.

J Biol Chem. 2008 Dec 26;283(52):36665-75. doi: 10.1074/jbc.M807844200. Epub 2008 Oct 14.

22.

Neuroprotective role of the Reaper-related serine protease HtrA2/Omi revealed by targeted deletion in mice.

Martins LM, Morrison A, Klupsch K, Fedele V, Moisoi N, Teismann P, Abuin A, Grau E, Geppert M, Livi GP, Creasy CL, Martin A, Hargreaves I, Heales SJ, Okada H, Brandner S, Schulz JB, Mak T, Downward J.

Mol Cell Biol. 2004 Nov;24(22):9848-62.

23.

The yeast Pho80-Pho85 cyclin-CDK complex has multiple substrates.

Waters NC, Knight JP, Creasy CL, Bergman LW.

Curr Genet. 2004 Jul;46(1):1-9. Epub 2004 Apr 1.

PMID:
15057567
24.

The serine protease Omi/HtrA2 regulates apoptosis by binding XIAP through a reaper-like motif.

Martins LM, Iaccarino I, Tenev T, Gschmeissner S, Totty NF, Lemoine NR, Savopoulos J, Gray CW, Creasy CL, Dingwall C, Downward J.

J Biol Chem. 2002 Jan 4;277(1):439-44. Epub 2001 Oct 15.

25.

Oligonucleotide-mediated, PCR-independent cloning by homologous recombination.

DeMarini DJ, Creasy CL, Lu Q, Mao J, Sheardown SA, Sathe GM, Livi GP.

Biotechniques. 2001 Mar;30(3):520-3.

26.

mDYRK3 kinase is expressed selectively in late erythroid progenitor cells and attenuates colony-forming unit-erythroid development.

Geiger JN, Knudsen GT, Panek L, Pandit AK, Yoder MD, Lord KA, Creasy CL, Burns BM, Gaines P, Dillon SB, Wojchowski DM.

Blood. 2001 Feb 15;97(4):901-10.

PMID:
11159515
27.

Characterization of human HtrA2, a novel serine protease involved in the mammalian cellular stress response.

Gray CW, Ward RV, Karran E, Turconi S, Rowles A, Viglienghi D, Southan C, Barton A, Fantom KG, West A, Savopoulos J, Hassan NJ, Clinkenbeard H, Hanning C, Amegadzie B, Davis JB, Dingwall C, Livi GP, Creasy CL.

Eur J Biochem. 2000 Sep;267(18):5699-710.

28.

Expression, purification, and functional analysis of the human serine protease HtrA2.

Savopoulos JW, Carter PS, Turconi S, Pettman GR, Karran EH, Gray CW, Ward RV, Jenkins O, Creasy CL.

Protein Expr Purif. 2000 Jul;19(2):227-34.

PMID:
10873535
29.
30.

REDK, a novel human regulatory erythroid kinase.

Lord KA, Creasy CL, King AG, King C, Burns BM, Lee JC, Dillon SB.

Blood. 2000 May 1;95(9):2838-46.

PMID:
10779429
31.
32.

The Ste20-like protein kinase, Mst1, dimerizes and contains an inhibitory domain.

Creasy CL, Ambrose DM, Chernoff J.

J Biol Chem. 1996 Aug 30;271(35):21049-53.

33.
34.

Negative transcriptional regulation of PH081 expression in Saccharomyces cerevisiae.

Creasy CL, Shao D, Begman LW.

Gene. 1996 Feb 2;168(1):23-9.

PMID:
8626060
35.

Cloning and characterization of a member of the MST subfamily of Ste20-like kinases.

Creasy CL, Chernoff J.

Gene. 1995 Dec 29;167(1-2):303-6.

PMID:
8566796
36.

Fission yeast pak1+ encodes a protein kinase that interacts with Cdc42p and is involved in the control of cell polarity and mating.

Ottilie S, Miller PJ, Johnson DI, Creasy CL, Sells MA, Bagrodia S, Forsburg SL, Chernoff J.

EMBO J. 1995 Dec 1;14(23):5908-19.

37.

Structure-function relationships of the yeast cyclin-dependent kinase Pho85.

Santos RC, Waters NC, Creasy CL, Bergman LW.

Mol Cell Biol. 1995 Oct;15(10):5482-91.

38.

Identification of a mouse p21Cdc42/Rac activated kinase.

Bagrodia S, Taylor SJ, Creasy CL, Chernoff J, Cerione RA.

J Biol Chem. 1995 Sep 29;270(39):22731-7. Erratum in: J Biol Chem 1996 Jan 12;271(2):1250.

39.

Cloning and characterization of a human protein kinase with homology to Ste20.

Creasy CL, Chernoff J.

J Biol Chem. 1995 Sep 15;270(37):21695-700.

40.

Molecular analysis of the PHO81 gene of Saccharomyces cerevisiae.

Creasy CL, Madden SL, Bergman LW.

Nucleic Acids Res. 1993 Apr 25;21(8):1975-82.

41.

Molecular analysis of a temperature sensitive allele of the PHO2 gene of Saccharomyces cerevisiae.

McCarthy BJ, Creasy CL, Bergman LW.

Nucleic Acids Res. 1991 Jun 25;19(12):3463. No abstract available.

42.

Structure and expression of the PHO80 gene of Saccharomyces cerevisiae.

Madden SL, Creasy CL, Srinivas V, Fawcett W, Bergman LW.

Nucleic Acids Res. 1988 Mar 25;16(6):2625-37.

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