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Items: 36

1.

Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.

Vaswani RG, Gehling VS, Dakin LA, Cook AS, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT, Normant E, Bellon SF, Albrecht BK, Harmange JC, Trojer P, Audia JE, Zhang Y, Justin N, Chen S, Wilson JR, Gamblin SJ.

J Med Chem. 2016 Nov 10;59(21):9928-9941. Epub 2016 Oct 28.

2.

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.

Albrecht BK, Gehling VS, Hewitt MC, Vaswani RG, Côté A, Leblanc Y, Nasveschuk CG, Bellon S, Bergeron L, Campbell R, Cantone N, Cooper MR, Cummings RT, Jayaram H, Joshi S, Mertz JA, Neiss A, Normant E, O'Meara M, Pardo E, Poy F, Sandy P, Supko J, Sims RJ 3rd, Harmange JC, Taylor AM, Audia JE.

J Med Chem. 2016 Feb 25;59(4):1330-9. doi: 10.1021/acs.jmedchem.5b01882. Epub 2016 Feb 4.

PMID:
26815195
3.

Discovery, design, and synthesis of indole-based EZH2 inhibitors.

Gehling VS, Vaswani RG, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Dakin LA, Cook AS, Gagnon A, Harmange JC, Audia JE, Cummings RT, Normant E, Trojer P, Albrecht BK.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9. doi: 10.1016/j.bmcl.2015.06.056. Epub 2015 Jun 19.

PMID:
26189078
4.

EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.

Bradley WD, Arora S, Busby J, Balasubramanian S, Gehling VS, Nasveschuk CG, Vaswani RG, Yuan CC, Hatton C, Zhao F, Williamson KE, Iyer P, Méndez J, Campbell R, Cantone N, Garapaty-Rao S, Audia JE, Cook AS, Dakin LA, Albrecht BK, Harmange JC, Daniels DL, Cummings RT, Bryant BM, Normant E, Trojer P.

Chem Biol. 2014 Nov 20;21(11):1463-75. doi: 10.1016/j.chembiol.2014.09.017.

5.

The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors.

Wong C, Laddha SV, Tang L, Vosburgh E, Levine AJ, Normant E, Sandy P, Harris CR, Chan CS, Xu EY.

Cell Death Dis. 2014 Oct 9;5:e1450. doi: 10.1038/cddis.2014.396.

6.

Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.

Ceribelli M, Kelly PN, Shaffer AL, Wright GW, Xiao W, Yang Y, Mathews Griner LA, Guha R, Shinn P, Keller JM, Liu D, Patel PR, Ferrer M, Joshi S, Nerle S, Sandy P, Normant E, Thomas CJ, Staudt LM.

Proc Natl Acad Sci U S A. 2014 Aug 5;111(31):11365-70. doi: 10.1073/pnas.1411701111. Epub 2014 Jul 21.

7.

Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma.

Moros A, Rodríguez V, Saborit-Villarroya I, Montraveta A, Balsas P, Sandy P, Martínez A, Wiestner A, Normant E, Campo E, Pérez-Galán P, Colomer D, Roué G.

Leukemia. 2014 Oct;28(10):2049-59. doi: 10.1038/leu.2014.106. Epub 2014 Mar 18.

PMID:
24721791
8.

A phase I study of the HSP90 inhibitor retaspimycin hydrochloride (IPI-504) in patients with gastrointestinal stromal tumors or soft-tissue sarcomas.

Wagner AJ, Chugh R, Rosen LS, Morgan JA, George S, Gordon M, Dunbar J, Normant E, Grayzel D, Demetri GD.

Clin Cancer Res. 2013 Nov 1;19(21):6020-9. doi: 10.1158/1078-0432.CCR-13-0953. Epub 2013 Sep 17.

9.

Heat shock protein 90 is a promising target for effective growth inhibition of gastrointestinal neuroendocrine tumors.

Gloesenkamp C, Nitzsche B, Lim AR, Normant E, Vosburgh E, Schrader M, Ocker M, Scherübl H, Höpfner M.

Int J Oncol. 2012 May;40(5):1659-67. doi: 10.3892/ijo.2012.1328. Epub 2012 Jan 10.

PMID:
22246317
10.

Exploiting cancer cell vulnerabilities to develop a combination therapy for ras-driven tumors.

De Raedt T, Walton Z, Yecies JL, Li D, Chen Y, Malone CF, Maertens O, Jeong SM, Bronson RT, Lebleu V, Kalluri R, Normant E, Haigis MC, Manning BD, Wong KK, Macleod KF, Cichowski K.

Cancer Cell. 2011 Sep 13;20(3):400-13. doi: 10.1016/j.ccr.2011.08.014.

11.

A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refractory multiple myeloma.

Siegel D, Jagannath S, Vesole DH, Borello I, Mazumder A, Mitsiades C, Goddard J, Dunbar J, Normant E, Adams J, Grayzel D, Anderson KC, Richardson P.

Leuk Lymphoma. 2011 Dec;52(12):2308-15. doi: 10.3109/10428194.2011.600481. Epub 2011 Aug 18.

PMID:
21851215
12.

The heat shock protein 90 inhibitor IPI-504 induces KIT degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors.

Floris G, Debiec-Rychter M, Wozniak A, Stefan C, Normant E, Faa G, Machiels K, Vanleeuw U, Sciot R, Schöffski P.

Mol Cancer Ther. 2011 Oct;10(10):1897-908. doi: 10.1158/1535-7163.MCT-11-0148. Epub 2011 Aug 8.

13.

The Novel HSP90 inhibitor, IPI-493, is highly effective in human gastrostrointestinal stromal tumor xenografts carrying heterogeneous KIT mutations.

Floris G, Sciot R, Wozniak A, Van Looy T, Wellens J, Faa G, Normant E, Debiec-Rychter M, Schöffski P.

Clin Cancer Res. 2011 Sep 1;17(17):5604-14. doi: 10.1158/1078-0432.CCR-11-0562. Epub 2011 Jul 7.

14.

Antitumor activity of the Hsp90 inhibitor IPI-504 in HER2-positive trastuzumab-resistant breast cancer.

Scaltriti M, Serra V, Normant E, Guzman M, Rodriguez O, Lim AR, Slocum KL, West KA, Rodriguez V, Prudkin L, Jimenez J, Aura C, Baselga J.

Mol Cancer Ther. 2011 May;10(5):817-24. doi: 10.1158/1535-7163.MCT-10-0966. Epub 2011 Mar 7.

15.

The Hsp90 inhibitor IPI-504 rapidly lowers EML4-ALK levels and induces tumor regression in ALK-driven NSCLC models.

Normant E, Paez G, West KA, Lim AR, Slocum KL, Tunkey C, McDougall J, Wylie AA, Robison K, Caliri K, Palombella VJ, Fritz CC.

Oncogene. 2011 Jun 2;30(22):2581-6. doi: 10.1038/onc.2010.625. Epub 2011 Jan 24.

PMID:
21258415
16.

The Hsp90 inhibitor IPI-504 overcomes bortezomib resistance in mantle cell lymphoma in vitro and in vivo by down-regulation of the prosurvival ER chaperone BiP/Grp78.

Roué G, Pérez-Galán P, Mozos A, López-Guerra M, Xargay-Torrent S, Rosich L, Saborit-Villarroya I, Normant E, Campo E, Colomer D.

Blood. 2011 Jan 27;117(4):1270-9. doi: 10.1182/blood-2010-04-278853. Epub 2010 Nov 24.

17.

Hsp90 (heat shock protein 90) inhibitor occupancy is a direct determinant of client protein degradation and tumor growth arrest in vivo.

Tillotson B, Slocum K, Coco J, Whitebread N, Thomas B, West KA, MacDougall J, Ge J, Ali JA, Palombella VJ, Normant E, Adams J, Fritz CC.

J Biol Chem. 2010 Dec 17;285(51):39835-43. doi: 10.1074/jbc.M110.141580. Epub 2010 Oct 12.

18.

The antiproliferative activity of the heat shock protein 90 inhibitor IPI-504 is not dependent on NAD(P)H:quinone oxidoreductase 1 activity in vivo.

Douglas M, Lim AR, Porter JR, West K, Pink MM, Ge J, Wylie AA, Tibbits TT, Biggs K, Curtis M, Palombella VJ, Adams J, Fritz CC, Normant E.

Mol Cancer Ther. 2009 Dec;8(12):3369-78. doi: 10.1158/1535-7163.MCT-09-0568.

19.

Ansamycin inhibitors of Hsp90: nature's prototype for anti-chaperone therapy.

Porter JR, Ge J, Lee J, Normant E, West K.

Curr Top Med Chem. 2009;9(15):1386-418. Review.

PMID:
19860734
20.

IPI-504, a novel and soluble HSP-90 inhibitor, blocks the unfolded protein response in multiple myeloma cells.

Patterson J, Palombella VJ, Fritz C, Normant E.

Cancer Chemother Pharmacol. 2008 May;61(6):923-32. Epub 2007 Jul 12.

PMID:
17624530
21.

Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90.

Sydor JR, Normant E, Pien CS, Porter JR, Ge J, Grenier L, Pak RH, Ali JA, Dembski MS, Hudak J, Patterson J, Penders C, Pink M, Read MA, Sang J, Woodward C, Zhang Y, Grayzel DS, Wright J, Barrett JA, Palombella VJ, Adams J, Tong JK.

Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17408-13. Epub 2006 Nov 7.

22.

Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.

Ge J, Normant E, Porter JR, Ali JA, Dembski MS, Gao Y, Georges AT, Grenier L, Pak RH, Patterson J, Sydor JR, Tibbitts TT, Tong JK, Adams J, Palombella VJ.

J Med Chem. 2006 Jul 27;49(15):4606-15.

PMID:
16854066
23.
25.
26.
27.

Purification, cDNA cloning, functional expression, and characterization of a 26-kDa endogenous mammalian carboxypeptidase inhibitor.

Normant E, Martres MP, Schwartz JC, Gros C.

Proc Natl Acad Sci U S A. 1995 Dec 19;92(26):12225-9.

28.
29.

Seasonal and hormonal control of pulsatile LH secretion in the dairy goat (Capra hircus).

Chemineau P, Martin GB, Saumande J, Normant E.

J Reprod Fertil. 1988 May;83(1):91-8.

PMID:
3397961
31.

[Atrophic changes in the hip joint after treatment of congenital hip dislocation by the Salter method].

Normant E.

Chir Narzadow Ruchu Ortop Pol. 1980;45(5):453-8. Polish. No abstract available.

PMID:
7460671
32.

[Posterior shoulder dislocation with humeral neck fracture].

Normant E, Grabowski M.

Chir Narzadow Ruchu Ortop Pol. 1980;45(4):315-7. Polish. No abstract available.

PMID:
7428497
33.

[Effect of Salter's operation on the course of preoperative atrophy of the dislocated hip joint].

Normant E.

Chir Narzadow Ruchu Ortop Pol. 1980;45(3):233-7. Polish. No abstract available.

PMID:
7418525
34.

[Results of treatment of stable compression vertebral fractures without paraplegia].

Normant E, Czernihowski M, Dańko S, Henicz T, Hać B.

Chir Narzadow Ruchu Ortop Pol. 1980;45(1):13-8. Polish. No abstract available.

PMID:
7379615
35.

[Surgical treatment of hallux valgus in juveniles].

Borkowski Z, Ozga A, Normant EA.

Chir Narzadow Ruchu Ortop Pol. 1976;41(3):307-14. Polish. No abstract available.

PMID:
964051
36.

[Results of surgical tibia lengthening].

Normant E, Borkowski Z.

Chir Narzadow Ruchu Ortop Pol. 1975;40(6):725-9. Polish. No abstract available.

PMID:
1204389

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