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Downregulation of HER3 by a novel antisense oligonucleotide, EZN-3920, improves the antitumor activity of EGFR and HER2 tyrosine kinase inhibitors in animal models.

Wu Y, Zhang Y, Wang M, Li Q, Qu Z, Shi V, Kraft P, Kim S, Gao Y, Pak J, Youngster S, Horak ID, Greenberger LM.

Mol Cancer Ther. 2013 Apr;12(4):427-37. doi: 10.1158/1535-7163.MCT-12-0838. Epub 2013 Feb 8.


Reduced expression of the androgen receptor by third generation of antisense shows antitumor activity in models of prostate cancer.

Zhang Y, Castaneda S, Dumble M, Wang M, Mileski M, Qu Z, Kim S, Shi V, Kraft P, Gao Y, Pak J, Sapra P, Bandaru R, Zhao H, Vessella RL, Horak ID, Greenberger LM.

Mol Cancer Ther. 2011 Dec;10(12):2309-19. doi: 10.1158/1535-7163.MCT-11-0329. Epub 2011 Oct 25.


Endogenous knockdown of survivin improves chemotherapeutic response in ALL models.

Morrison DJ, Hogan LE, Condos G, Bhatla T, Germino N, Moskowitz NP, Lee L, Bhojwani D, Horton TM, Belitskaya-Levy I, Greenberger LM, Horak ID, Grupp SA, Teachey DT, Raetz EA, Carroll WL.

Leukemia. 2012 Feb;26(2):271-9. doi: 10.1038/leu.2011.199. Epub 2011 Aug 16.


Potent and sustained inhibition of HIF-1α and downstream genes by a polyethyleneglycol-SN38 conjugate, EZN-2208, results in anti-angiogenic effects.

Sapra P, Kraft P, Pastorino F, Ribatti D, Dumble M, Mehlig M, Wang M, Ponzoni M, Greenberger LM, Horak ID.

Angiogenesis. 2011 Sep;14(3):245-53. doi: 10.1007/s10456-011-9209-1. Epub 2011 Mar 31.


4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II.

Huang S, Li R, LaMontagne KR, Greenberger LM, Connolly PJ.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1815-8. doi: 10.1016/j.bmcl.2011.01.053. Epub 2011 Jan 21.


Down-modulation of cancer targets using locked nucleic acid (LNA)-based antisense oligonucleotides without transfection.

Zhang Y, Qu Z, Kim S, Shi V, Liao B, Kraft P, Bandaru R, Wu Y, Greenberger LM, Horak ID.

Gene Ther. 2011 Apr;18(4):326-33. doi: 10.1038/gt.2010.133. Epub 2010 Dec 23.


Tumor regression and curability of preclinical neuroblastoma models by PEGylated SN38 (EZN-2208), a novel topoisomerase I inhibitor.

Pastorino F, Loi M, Sapra P, Becherini P, Cilli M, Emionite L, Ribatti D, Greenberger LM, Horak ID, Ponzoni M.

Clin Cancer Res. 2010 Oct 1;16(19):4809-21. doi: 10.1158/1078-0432.CCR-10-1354. Epub 2010 Aug 11.


Down-modulation of survivin expression and inhibition of tumor growth in vivo by EZN-3042, a locked nucleic acid antisense oligonucleotide.

Sapra P, Wang M, Bandaru R, Zhao H, Greenberger LM, Horak ID.

Nucleosides Nucleotides Nucleic Acids. 2010 Feb;29(2):97-112. doi: 10.1080/15257771003597733.


Marked therapeutic efficacy of a novel polyethylene glycol-SN38 conjugate, EZN-2208, in xenograft models of B-cell non-Hodgkin's lymphoma.

Sapra P, Kraft P, Mehlig M, Malaby J, Zhao H, Greenberger LM, Horak ID.

Haematologica. 2009 Oct;94(10):1456-9. doi: 10.3324/haematol.2009.008276.


A highly selective, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor has potent activity in vitro and in vivo.

LaMontagne KR, Butler J, Borowski VB, Fuentes-Pesquera AR, Blevitt JM, Huang S, Li R, Connolly PJ, Greenberger LM.

Angiogenesis. 2009;12(3):287-96. doi: 10.1007/s10456-009-9151-7. Epub 2009 Jun 21.


A RNA antagonist of hypoxia-inducible factor-1alpha, EZN-2968, inhibits tumor cell growth.

Greenberger LM, Horak ID, Filpula D, Sapra P, Westergaard M, Frydenlund HF, Albaek C, Schrøder H, Ørum H.

Mol Cancer Ther. 2008 Nov;7(11):3598-608. doi: 10.1158/1535-7163.MCT-08-0510. Epub 2008 Oct 30.


A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.

Hughes TV, Xu G, Wetter SK, Connolly PJ, Emanuel SL, Karnachi P, Pollack SR, Pandey N, Adams M, Moreno-Mazza S, Middleton SA, Greenberger LM.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4896-9. doi: 10.1016/j.bmcl.2008.07.057. Epub 2008 Jul 17.


Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.

Xu G, Searle LL, Hughes TV, Beck AK, Connolly PJ, Abad MC, Neeper MP, Struble GT, Springer BA, Emanuel SL, Gruninger RH, Pandey N, Adams M, Moreno-Mazza S, Fuentes-Pesquera AR, Middleton SA, Greenberger LM.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3495-9. doi: 10.1016/j.bmcl.2008.05.024. Epub 2008 May 10.


Novel prodrugs of SN38 using multiarm poly(ethylene glycol) linkers.

Zhao H, Rubio B, Sapra P, Wu D, Reddy P, Sai P, Martinez A, Gao Y, Lozanguiez Y, Longley C, Greenberger LM, Horak ID.

Bioconjug Chem. 2008 Apr;19(4):849-59. doi: 10.1021/bc700333s. Epub 2008 Mar 28.


Novel delivery of SN38 markedly inhibits tumor growth in xenografts, including a camptothecin-11-refractory model.

Sapra P, Zhao H, Mehlig M, Malaby J, Kraft P, Longley C, Greenberger LM, Horak ID.

Clin Cancer Res. 2008 Mar 15;14(6):1888-96. doi: 10.1158/1078-0432.CCR-07-4456.


Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors.

Emanuel SL, Hughes TV, Adams M, Rugg CA, Fuentes-Pesquera A, Connolly PJ, Pandey N, Moreno-Mazza S, Butler J, Borowski V, Middleton SA, Gruninger RH, Story JR, Napier C, Hollister B, Greenberger LM.

Mol Pharmacol. 2008 Feb;73(2):338-48. Epub 2007 Nov 1.


Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.

Lin R, Chiu G, Yu Y, Connolly PJ, Li S, Lu Y, Adams M, Fuentes-Pesquera AR, Emanuel SL, Greenberger LM.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4557-61. Epub 2007 Jun 6.


Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.

Lin R, Connolly PJ, Lu Y, Chiu G, Li S, Yu Y, Huang S, Li X, Emanuel SL, Middleton SA, Gruninger RH, Adams M, Fuentes-Pesquera AR, Greenberger LM.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4297-302. Epub 2007 May 16.


Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor.

Seamon JA, Rugg CA, Emanuel S, Calcagno AM, Ambudkar SV, Middleton SA, Butler J, Borowski V, Greenberger LM.

Mol Cancer Ther. 2006 Oct;5(10):2459-67.


Synthesis and biological study of 4-aminopyrimidine-5-carboxaldehyde oximes as antiproliferative VEGFR-2 inhibitors.

Huang S, Li R, Connolly PJ, Xu G, Gaul MD, Emanuel SL, Lamontagne KR, Greenberger LM.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6063-6. Epub 2006 Sep 18.


Combination therapy for treating breast cancer using antiestrogen, ERA-923, and the mammalian target of rapamycin inhibitor, temsirolimus.

Sadler TM, Gavriil M, Annable T, Frost P, Greenberger LM, Zhang Y.

Endocr Relat Cancer. 2006 Sep;13(3):863-73.


Preclinical pharmacologic evaluation of MST-997, an orally active taxane with superior in vitro and in vivo efficacy in paclitaxel- and docetaxel-resistant tumor models.

Sampath D, Greenberger LM, Beyer C, Hari M, Liu H, Baxter M, Yang S, Rios C, Discafani C.

Clin Cancer Res. 2006 Jun 1;12(11 Pt 1):3459-69.


Paclitaxel-resistant cells have a mutation in the paclitaxel-binding region of beta-tubulin (Asp26Glu) and less stable microtubules.

Hari M, Loganzo F, Annable T, Tan X, Musto S, Morilla DB, Nettles JH, Snyder JP, Greenberger LM.

Mol Cancer Ther. 2006 Feb;5(2):270-8.


Two photoaffinity analogues of the tripeptide, hemiasterlin, exclusively label alpha-tubulin.

Nunes M, Kaplan J, Wooters J, Hari M, Minnick AA Jr, May MK, Shi C, Musto S, Beyer C, Krishnamurthy G, Qiu Y, Loganzo F, Ayral-Kaloustian S, Zask A, Greenberger LM.

Biochemistry. 2005 May 10;44(18):6844-57.


An anti-MUC1 antibody-calicheamicin conjugate for treatment of solid tumors. Choice of linker and overcoming drug resistance.

Hamann PR, Hinman LM, Beyer CF, Greenberger LM, Lin C, Lindh D, Menendez AT, Wallace R, Durr FE, Upeslacis J.

Bioconjug Chem. 2005 Mar-Apr;16(2):346-53.


Tumor cells resistant to a microtubule-depolymerizing hemiasterlin analogue, HTI-286, have mutations in alpha- or beta-tubulin and increased microtubule stability.

Poruchynsky MS, Kim JH, Nogales E, Annable T, Loganzo F, Greenberger LM, Sackett DL, Fojo T.

Biochemistry. 2004 Nov 9;43(44):13944-54.


Cells resistant to HTI-286 do not overexpress P-glycoprotein but have reduced drug accumulation and a point mutation in alpha-tubulin.

Loganzo F, Hari M, Annable T, Tan X, Morilla DB, Musto S, Zask A, Kaplan J, Minnick AA Jr, May MK, Ayral-Kaloustian S, Poruchynsky MS, Fojo T, Greenberger LM.

Mol Cancer Ther. 2004 Oct;3(10):1319-27.


Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).

Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Suayan R, Yamashita A, Cole D, Tang Z, Krishnamurthy G, Williamson R, Khafizova G, Musto S, Hernandez R, Annable T, Yang X, Discafani C, Beyer C, Greenberger LM, Loganzo F, Ayral-Kaloustian S.

J Med Chem. 2004 Sep 9;47(19):4774-86.


D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors.

Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Yamashita A, Beyer C, Krishnamurthy G, Greenberger LM, Loganzo F, Ayral-Kaloustian S.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4353-8.


Identification and validation of novel androgen-regulated genes in prostate cancer.

Velasco AM, Gillis KA, Li Y, Brown EL, Sadler TM, Achilleos M, Greenberger LM, Frost P, Bai W, Zhang Y.

Endocrinology. 2004 Aug;145(8):3913-24. Epub 2004 May 6.


Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.

Wissner A, Hamann PR, Nilakantan R, Greenberger LM, Ye F, Rapuano TA, Loganzo F.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1411-6.


Development and comparison of two nonradioactive kinase assays for I kappa B kinase.

Sadler TM, Achilleos M, Ragunathan S, Pitkin A, LaRocque J, Morin J, Annable R, Greenberger LM, Frost P, Zhang Y.

Anal Biochem. 2004 Mar 1;326(1):106-13.


MAC-321, a novel taxane with greater efficacy than paclitaxel and docetaxel in vitro and in vivo.

Sampath D, Discafani CM, Loganzo F, Beyer C, Liu H, Tan X, Musto S, Annable T, Gallagher P, Rios C, Greenberger LM.

Mol Cancer Ther. 2003 Sep;2(9):873-84.


HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

Loganzo F, Discafani CM, Annable T, Beyer C, Musto S, Hari M, Tan X, Hardy C, Hernandez R, Baxter M, Singanallore T, Khafizova G, Poruchynsky MS, Fojo T, Nieman JA, Ayral-Kaloustian S, Zask A, Andersen RJ, Greenberger LM.

Cancer Res. 2003 Apr 15;63(8):1838-45.


Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).

Wissner A, Overbeek E, Reich MF, Floyd MB, Johnson BD, Mamuya N, Rosfjord EC, Discafani C, Davis R, Shi X, Rabindran SK, Gruber BC, Ye F, Hallett WA, Nilakantan R, Shen R, Wang YF, Greenberger LM, Tsou HR.

J Med Chem. 2003 Jan 2;46(1):49-63.


Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.

Wissner A, Brawner Floyd MB, Rabindran SK, Nilakantan R, Greenberger LM, Shen R, Wang YF, Tsou HR.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2893-7.


6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.

Tsou HR, Mamuya N, Johnson BD, Reich MF, Gruber BC, Ye F, Nilakantan R, Shen R, Discafani C, DeBlanc R, Davis R, Koehn FE, Greenberger LM, Wang YF, Wissner A.

J Med Chem. 2001 Aug 16;44(17):2719-34.


Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.

Miller CP, Collini MD, Tran BD, Harris HA, Kharode YP, Marzolf JT, Moran RA, Henderson RA, Bender RH, Unwalla RJ, Greenberger LM, Yardley JP, Abou-Gharbia MA, Lyttle CR, Komm BS.

J Med Chem. 2001 May 24;44(11):1654-7. No abstract available.


4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.

Wissner A, Berger DM, Boschelli DH, Floyd MB Jr, Greenberger LM, Gruber BC, Johnson BD, Mamuya N, Nilakantan R, Reich MF, Shen R, Tsou HR, Upeslacis E, Wang YF, Wu B, Ye F, Zhang N.

J Med Chem. 2000 Aug 24;43(17):3244-56.


Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein.

Rabindran SK, Ross DD, Doyle LA, Yang W, Greenberger LM.

Cancer Res. 2000 Jan 1;60(1):47-50.


Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785).

Discafani CM, Carroll ML, Floyd MB Jr, Hollander IJ, Husain Z, Johnson BD, Kitchen D, May MK, Malo MS, Minnick AA Jr, Nilakantan R, Shen R, Wang YF, Wissner A, Greenberger LM.

Biochem Pharmacol. 1999 Apr 15;57(8):917-25.


Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C.

Rabindran SK, He H, Singh M, Brown E, Collins KI, Annable T, Greenberger LM.

Cancer Res. 1998 Dec 15;58(24):5850-8.


Identification of drug interaction sites in P-glycoprotein.

Greenberger LM.

Methods Enzymol. 1998;292:307-17. No abstract available.


Localization of the forskolin labeling sites to both halves of P-glycoprotein: similarity of the sites labeled by forskolin and prazosin.

Morris DI, Greenberger LM, Bruggemann EP, Cardarelli C, Gottesman MM, Pastan I, Seamon KB.

Mol Pharmacol. 1994 Aug;46(2):329-37.


ATP-binding cassette proteins Common denominators between ion channels, transporters, and enzymes.

Greenberger LM, Ishikawa Y.

Trends Cardiovasc Med. 1994 Jul-Aug;4(4):193-8. doi: 10.1016/1050-1738(94)90057-4.


P-glycoprotein mediates profound resistance to bisantrene.

Zhang XP, Ritke MK, Yalowich JC, Slovak ML, Ho JP, Collins KI, Annable T, Arceci RJ, Durr FE, Greenberger LM.

Oncol Res. 1994;6(7):291-301.


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