Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 38

1.

Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation.

Lu AZ, Abo R, Ren Y, Gui B, Mo JR, Blackwell D, Wigle T, Keilhack H, Niepel M.

Biochem Pharmacol. 2019 Sep;167:97-106. doi: 10.1016/j.bcp.2019.05.007. Epub 2019 May 7.

2.

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
3.

EZH2 Modifies Sunitinib Resistance in Renal Cell Carcinoma by Kinome Reprogramming.

Adelaiye-Ogala R, Budka J, Damayanti NP, Arrington J, Ferris M, Hsu CC, Chintala S, Orillion A, Miles KM, Shen L, Elbanna M, Ciamporcero E, Arisa S, Pettazzoni P, Draetta GF, Seshadri M, Hancock B, Radovich M, Kota J, Buck M, Keilhack H, McCarthy BP, Persohn SA, Territo PR, Zang Y, Irudayaraj J, Tao WA, Hollenhorst P, Pili R.

Cancer Res. 2017 Dec 1;77(23):6651-6666. doi: 10.1158/0008-5472.CAN-17-0899. Epub 2017 Oct 4.

4.

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.

5.

In Vitro Long-Term Proliferation Assays to Study Antiproliferative Effects of PARP Inhibitors on Cancer Cells.

Keilhack H, Chang P.

Methods Mol Biol. 2017;1608:321-336. doi: 10.1007/978-1-4939-6993-7_21.

PMID:
28695519
6.

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.

7.

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.

8.

Initial testing (stage 1) of tazemetostat (EPZ-6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program.

Kurmasheva RT, Sammons M, Favours E, Wu J, Kurmashev D, Cosmopoulos K, Keilhack H, Klaus CR, Houghton PJ, Smith MA.

Pediatr Blood Cancer. 2017 Mar;64(3). doi: 10.1002/pbc.26218. Epub 2016 Aug 24.

9.

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.

10.

Reply to "Uveal melanoma cells are resistant to EZH2 inhibition regardless of BAP1 status".

LaFave LM, Béguelin W, Koche R, Teater M, Spitzer B, Chramiec A, Papalexi E, Keller MD, Hricik T, Konstantinoff K, Micol JB, Durham B, Knutson SK, Campbell JE, Blum G, Shi X, Doud EH, Krivtsov AV, Chung YR, Khodos I, de Stanchina E, Ouerfelli O, Adusumilli PS, Thomas PM, Kelleher NL, Luo M, Keilhack H, Abdel-Wahab O, Melnick A, Armstrong SA, Levine RL.

Nat Med. 2016 Jun 7;22(6):578-9. doi: 10.1038/nm.4094. No abstract available.

PMID:
27270773
11.

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
12.

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
13.

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.

14.

Loss of BAP1 function leads to EZH2-dependent transformation.

LaFave LM, Béguelin W, Koche R, Teater M, Spitzer B, Chramiec A, Papalexi E, Keller MD, Hricik T, Konstantinoff K, Micol JB, Durham B, Knutson SK, Campbell JE, Blum G, Shi X, Doud EH, Krivtsov AV, Chung YR, Khodos I, de Stanchina E, Ouerfelli O, Adusumilli PS, Thomas PM, Kelleher NL, Luo M, Keilhack H, Abdel-Wahab O, Melnick A, Armstrong SA, Levine RL.

Nat Med. 2015 Nov;21(11):1344-9. doi: 10.1038/nm.3947. Epub 2015 Oct 5.

15.

Small molecule inhibitors of EZH2: the emerging translational landscape.

Keilhack H, Smith JJ.

Epigenomics. 2015;7(3):337-41. doi: 10.2217/epi.15.14. No abstract available.

PMID:
26077423
16.

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.

17.

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.

18.

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
19.

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.

20.

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.

21.

Evidence of mTOR Activation by an AKT-Independent Mechanism Provides Support for the Combined Treatment of PTEN-Deficient Prostate Tumors with mTOR and AKT Inhibitors.

Zhang W, Haines BB, Efferson C, Zhu J, Ware C, Kunii K, Tammam J, Angagaw M, Hinton MC, Keilhack H, Paweletz CP, Zhang T, Winter C, Sathyanarayanan S, Cheng J, Zawel L, Fawell S, Gilliland G, Majumder PK.

Transl Oncol. 2012 Dec;5(6):422-9. Epub 2012 Dec 1.

22.

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
23.

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.

24.

PDK1 attenuation fails to prevent tumor formation in PTEN-deficient transgenic mouse models.

Ellwood-Yen K, Keilhack H, Kunii K, Dolinski B, Connor Y, Hu K, Nagashima K, O'Hare E, Erkul Y, Di Bacco A, Gargano D, Shomer NH, Angagaw M, Leccese E, Andrade P, Hurd M, Shin MK, Vogt TF, Northrup A, Bobkova EV, Kasibhatla S, Bronson RT, Scott ML, Draetta G, Richon V, Kohl N, Blume-Jensen P, Andersen JN, Kraus M.

Cancer Res. 2011 Apr 15;71(8):3052-65. doi: 10.1158/0008-5472.CAN-10-2282.

25.

Regulation of brown fat adipogenesis by protein tyrosine phosphatase 1B.

Matsuo K, Bettaieb A, Nagata N, Matsuo I, Keilhack H, Haj FG.

PLoS One. 2011 Jan 31;6(1):e16446. doi: 10.1371/journal.pone.0016446.

26.

Differential regulation of endoplasmic reticulum stress by protein tyrosine phosphatase 1B and T cell protein tyrosine phosphatase.

Bettaieb A, Liu S, Xi Y, Nagata N, Matsuo K, Matsuo I, Chahed S, Bakke J, Keilhack H, Tiganis T, Haj FG.

J Biol Chem. 2011 Mar 18;286(11):9225-35. doi: 10.1074/jbc.M110.186148. Epub 2011 Jan 7.

27.

Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor.

Nagashima K, Shumway SD, Sathyanarayanan S, Chen AH, Dolinski B, Xu Y, Keilhack H, Nguyen T, Wiznerowicz M, Li L, Lutterbach BA, Chi A, Paweletz C, Allison T, Yan Y, Munshi SK, Klippel A, Kraus M, Bobkova EV, Deshmukh S, Xu Z, Mueller U, Szewczak AA, Pan BS, Richon V, Pollock R, Blume-Jensen P, Northrup A, Andersen JN.

J Biol Chem. 2011 Feb 25;286(8):6433-48. doi: 10.1074/jbc.M110.156463. Epub 2010 Nov 30.

28.

Sensitive multiplexed analysis of kinase activities and activity-based kinase identification.

Kubota K, Anjum R, Yu Y, Kunz RC, Andersen JN, Kraus M, Keilhack H, Nagashima K, Krauss S, Paweletz C, Hendrickson RC, Feldman AS, Wu CL, Rush J, Villén J, Gygi SP.

Nat Biotechnol. 2009 Oct;27(10):933-40. doi: 10.1038/nbt.1566. Epub 2009 Oct 4.

29.

Comparative expression analysis of four breast cancer subtypes versus matched normal tissue from the same patients.

Martini PG, Taylor DM, Bienkowska J, Jackson J, McAllister G, Keilhack H, Campbell RK.

J Steroid Biochem Mol Biol. 2008 Apr;109(3-5):207-11. doi: 10.1016/j.jsbmb.2008.03.020. Epub 2008 Mar 14.

PMID:
18424034
30.

Diverse biochemical properties of Shp2 mutants. Implications for disease phenotypes.

Keilhack H, David FS, McGregor M, Cantley LC, Neel BG.

J Biol Chem. 2005 Sep 2;280(35):30984-93. Epub 2005 Jun 29.

31.

Prognostic, therapeutic, and mechanistic implications of a mouse model of leukemia evoked by Shp2 (PTPN11) mutations.

Mohi MG, Williams IR, Dearolf CR, Chan G, Kutok JL, Cohen S, Morgan K, Boulton C, Shigematsu H, Keilhack H, Akashi K, Gilliland DG, Neel BG.

Cancer Cell. 2005 Feb;7(2):179-91.

32.

Activating mutations of the noonan syndrome-associated SHP2/PTPN11 gene in human solid tumors and adult acute myelogenous leukemia.

Bentires-Alj M, Paez JG, David FS, Keilhack H, Halmos B, Naoki K, Maris JM, Richardson A, Bardelli A, Sugarbaker DJ, Richards WG, Du J, Girard L, Minna JD, Loh ML, Fisher DE, Velculescu VE, Vogelstein B, Meyerson M, Sellers WR, Neel BG.

Cancer Res. 2004 Dec 15;64(24):8816-20.

33.

Identification of Src phosphorylation sites in the catenin p120ctn.

Mariner DJ, Anastasiadis P, Keilhack H, Böhmer FD, Wang J, Reynolds AB.

J Biol Chem. 2001 Jul 27;276(30):28006-13. Epub 2001 May 29.

34.

Negative regulation of Ros receptor tyrosine kinase signaling. An epithelial function of the SH2 domain protein tyrosine phosphatase SHP-1.

Keilhack H, Müller M, Böhmer SA, Frank C, Weidner KM, Birchmeier W, Ligensa T, Berndt A, Kosmehl H, Günther B, Müller T, Birchmeier C, Böhmer FD.

J Cell Biol. 2001 Jan 22;152(2):325-34.

35.

The protein-tyrosine phosphatase SHP-1 binds to and dephosphorylates p120 catenin.

Keilhack H, Hellman U, van Hengel J, van Roy F, Godovac-Zimmermann J, Böhmer FD.

J Biol Chem. 2000 Aug 25;275(34):26376-84.

36.

Binding of phosphatidic acid to the protein-tyrosine phosphatase SHP-1 as a basis for activity modulation.

Frank C, Keilhack H, Opitz F, Zschörnig O, Böhmer FD.

Biochemistry. 1999 Sep 14;38(37):11993-2002.

PMID:
10508402
37.

Phosphotyrosine 1173 mediates binding of the protein-tyrosine phosphatase SHP-1 to the epidermal growth factor receptor and attenuation of receptor signaling.

Keilhack H, Tenev T, Nyakatura E, Godovac-Zimmermann J, Nielsen L, Seedorf K, Böhmer FD.

J Biol Chem. 1998 Sep 18;273(38):24839-46.

38.

Both SH2 domains are involved in interaction of SHP-1 with the epidermal growth factor receptor but cannot confer receptor-directed activity to SHP-1/SHP-2 chimera.

Tenev T, Keilhack H, Tomic S, Stoyanov B, Stein-Gerlach M, Lammers R, Krivtsov AV, Ullrich A, Böhmer FD.

J Biol Chem. 1997 Feb 28;272(9):5966-73.

Supplemental Content

Loading ...
Support Center