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Items: 39


A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment.

Hyer ML, Milhollen MA, Ciavarri J, Fleming P, Traore T, Sappal D, Huck J, Shi J, Gavin J, Brownell J, Yang Y, Stringer B, Griffin R, Bruzzese F, Soucy T, Duffy J, Rabino C, Riceberg J, Hoar K, Lublinsky A, Menon S, Sintchak M, Bump N, Pulukuri SM, Langston S, Tirrell S, Kuranda M, Veiby P, Newcomb J, Li P, Wu JT, Powe J, Dick LR, Greenspan P, Galvin K, Manfredi M, Claiborne C, Amidon BS, Bence NF.

Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474. Epub 2018 Jan 15.


Synergistic antitumor interaction between valproic acid, capecitabine and radiotherapy in colorectal cancer: critical role of p53.

Terranova-Barberio M, Pecori B, Roca MS, Imbimbo S, Bruzzese F, Leone A, Muto P, Delrio P, Avallone A, Budillon A, Di Gennaro E.

J Exp Clin Cancer Res. 2017 Dec 6;36(1):177. doi: 10.1186/s13046-017-0647-5.


Targeting Mevalonate Pathway in Cancer Treatment: Repurposing of Statins.

Iannelli F, Lombardi R, Milone MR, Pucci B, De Rienzo S, Budillon A, Bruzzese F.

Recent Pat Anticancer Drug Discov. 2017 Nov 29. doi: 10.2174/1574892812666171129141211. [Epub ahead of print]


Phase II clinical study of valproic acid plus cisplatin and cetuximab in recurrent and/or metastatic squamous cell carcinoma of Head and Neck-V-CHANCE trial.

Caponigro F, Di Gennaro E, Ionna F, Longo F, Aversa C, Pavone E, Maglione MG, Di Marzo M, Muto P, Cavalcanti E, Petrillo A, Sandomenico F, Maiolino P, D'Aniello R, Botti G, De Cecio R, Losito NS, Scala S, Trotta A, Zotti AI, Bruzzese F, Daponte A, Calogero E, Montano M, Pontone M, De Feo G, Perri F, Budillon A.

BMC Cancer. 2016 Nov 25;16(1):918.


Synergistic antitumor activity of histone deacetylase inhibitors and anti-ErbB3 antibody in NSCLC primary cultures via modulation of ErbB receptors expression.

Ciardiello C, Roca MS, Noto A, Bruzzese F, Moccia T, Vitagliano C, Di Gennaro E, Ciliberto G, Roscilli G, Aurisicchio L, Marra E, Mancini R, Budillon A, Leone A.

Oncotarget. 2016 Apr 12;7(15):19559-74. doi: 10.18632/oncotarget.7195.


Valproic acid potentiates the anticancer activity of capecitabine in vitro and in vivo in breast cancer models via induction of thymidine phosphorylase expression.

Terranova-Barberio M, Roca MS, Zotti AI, Leone A, Bruzzese F, Vitagliano C, Scogliamiglio G, Russo D, D'Angelo G, Franco R, Budillon A, Di Gennaro E.

Oncotarget. 2016 Feb 16;7(7):7715-31. doi: 10.18632/oncotarget.6802.


Vorinostat synergizes with EGFR inhibitors in NSCLC cells by increasing ROS via up-regulation of the major mitochondrial porin VDAC1 and modulation of the c-Myc-NRF2-KEAP1 pathway.

Leone A, Roca MS, Ciardiello C, Terranova-Barberio M, Vitagliano C, Ciliberto G, Mancini R, Di Gennaro E, Bruzzese F, Budillon A.

Free Radic Biol Med. 2015 Dec;89:287-99. doi: 10.1016/j.freeradbiomed.2015.07.155. Epub 2015 Sep 26.


Annexin A1 is involved in the acquisition and maintenance of a stem cell-like/aggressive phenotype in prostate cancer cells with acquired resistance to zoledronic acid.

Bizzarro V, Belvedere R, Milone MR, Pucci B, Lombardi R, Bruzzese F, Popolo A, Parente L, Budillon A, Petrella A.

Oncotarget. 2015 Sep 22;6(28):25076-92. doi: 10.18632/oncotarget.4725.


Pathophysiologically relevant in vitro tumor models for drug screening.

Das V, Bruzzese F, Konečný P, Iannelli F, Budillon A, Hajdúch M.

Drug Discov Today. 2015 Jul;20(7):848-55. doi: 10.1016/j.drudis.2015.04.004. Epub 2015 Apr 20. Review.


Proteomic analysis of zoledronic-acid resistant prostate cancer cells unveils novel pathways characterizing an invasive phenotype.

Milone MR, Pucci B, Bifulco K, Iannelli F, Lombardi R, Ciardiello C, Bruzzese F, Carriero MV, Budillon A.

Oncotarget. 2015 Mar 10;6(7):5324-41.


Mechanistic study of Uba5 enzyme and the Ufm1 conjugation pathway.

Gavin JM, Hoar K, Xu Q, Ma J, Lin Y, Chen J, Chen W, Bruzzese FJ, Harrison S, Mallender WD, Bump NJ, Sintchak MD, Bence NF, Li P, Dick LR, Gould AE, Chen JJ.

J Biol Chem. 2014 Aug 15;289(33):22648-58. doi: 10.1074/jbc.M114.573972. Epub 2014 Jun 25.


Local and systemic protumorigenic effects of cancer-associated fibroblast-derived GDF15.

Bruzzese F, Hägglöf C, Leone A, Sjöberg E, Roca MS, Kiflemariam S, Sjöblom T, Hammarsten P, Egevad L, Bergh A, Ostman A, Budillon A, Augsten M.

Cancer Res. 2014 Jul 1;74(13):3408-17. doi: 10.1158/0008-5472.CAN-13-2259. Epub 2014 Apr 29.


Panobinostat synergizes with zoledronic acid in prostate cancer and multiple myeloma models by increasing ROS and modulating mevalonate and p38-MAPK pathways.

Bruzzese F, Pucci B, Milone MR, Ciardiello C, Franco R, Chianese MI, Rocco M, Di Gennaro E, Leone A, Luciano A, Arra C, Santini D, Caraglia M, Budillon A.

Cell Death Dis. 2013 Oct 24;4:e878. doi: 10.1038/cddis.2013.406.


New perspective for an old antidiabetic drug: metformin as anticancer agent.

Leone A, Di Gennaro E, Bruzzese F, Avallone A, Budillon A.

Cancer Treat Res. 2014;159:355-76. doi: 10.1007/978-3-642-38007-5_21. Review.


Acquired resistance to zoledronic acid and the parallel acquisition of an aggressive phenotype are mediated by p38-MAP kinase activation in prostate cancer cells.

Milone MR, Pucci B, Bruzzese F, Carbone C, Piro G, Costantini S, Capone F, Leone A, Di Gennaro E, Caraglia M, Budillon A.

Cell Death Dis. 2013 May 23;4:e641. doi: 10.1038/cddis.2013.165. Erratum in: Cell Death Dis. 2014;5:e1276.


Identification and application of NEDD8 E1 inhibitors.

Bruzzese FJ, Milhollen MA, Gavin JM, Josephine HR, Brownell JE.

Methods Mol Biol. 2012;832:577-88. doi: 10.1007/978-1-61779-474-2_40.


Mechanistic studies of substrate-assisted inhibition of ubiquitin-activating enzyme by adenosine sulfamate analogues.

Chen JJ, Tsu CA, Gavin JM, Milhollen MA, Bruzzese FJ, Mallender WD, Sintchak MD, Bump NJ, Yang X, Ma J, Loke HK, Xu Q, Li P, Bence NF, Brownell JE, Dick LR.

J Biol Chem. 2011 Nov 25;286(47):40867-77. doi: 10.1074/jbc.M111.279984. Epub 2011 Oct 3.


Proteomic analysis identifies differentially expressed proteins after HDAC vorinostat and EGFR inhibitor gefitinib treatments in Hep-2 cancer cells.

Bianchi L, Bruzzese F, Leone A, Gagliardi A, Puglia M, Di Gennaro E, Rocco M, Gimigliano A, Pucci B, Armini A, Bini L, Budillon A.

Proteomics. 2011 Sep;11(18):3725-42. doi: 10.1002/pmic.201100092.


HDAC inhibitor vorinostat enhances the antitumor effect of gefitinib in squamous cell carcinoma of head and neck by modulating ErbB receptor expression and reverting EMT.

Bruzzese F, Leone A, Rocco M, Carbone C, Piro G, Caraglia M, Di Gennaro E, Budillon A.

J Cell Physiol. 2011 Sep;226(9):2378-90. doi: 10.1002/jcp.22574.


Vorinostat synergises with capecitabine through upregulation of thymidine phosphorylase.

Di Gennaro E, Piro G, Chianese MI, Franco R, Di Cintio A, Moccia T, Luciano A, de Ruggiero I, Bruzzese F, Avallone A, Arra C, Budillon A.

Br J Cancer. 2010 Nov 23;103(11):1680-91. doi: 10.1038/sj.bjc.6605969. Epub 2010 Nov 2.


Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome.

Blackburn C, Barrett C, Blank JL, Bruzzese FJ, Bump N, Dick LR, Fleming P, Garcia K, Hales P, Hu Z, Jones M, Liu JX, Sappal DS, Sintchak MD, Tsu C, Gigstad KM.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6581-6. doi: 10.1016/j.bmcl.2010.09.032. Epub 2010 Sep 15.


Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit.

Blackburn C, Gigstad KM, Hales P, Garcia K, Jones M, Bruzzese FJ, Barrett C, Liu JX, Soucy TA, Sappal DS, Bump N, Olhava EJ, Fleming P, Dick LR, Tsu C, Sintchak MD, Blank JL.

Biochem J. 2010 Sep 15;430(3):461-76. doi: 10.1042/BJ20100383. Erratum in: Biochem J. 2010 Oct 11;431(3):433.


Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer.

Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu J, Yang Y, Hales P, Bruzzese F, Liu J, Blank J, Garcia K, Tsu C, Dick L, Fleming P, Yu L, Manfredi M, Rolfe M, Bolen J.

Cancer Res. 2010 Mar 1;70(5):1970-80. doi: 10.1158/0008-5472.CAN-09-2766. Epub 2010 Feb 16. Erratum in: Cancer Res. 2010 May 1;70(9):3853. Hales, Paul [added].


Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ.

Brownell JE, Sintchak MD, Gavin JM, Liao H, Bruzzese FJ, Bump NJ, Soucy TA, Milhollen MA, Yang X, Burkhardt AL, Ma J, Loke HK, Lingaraj T, Wu D, Hamman KB, Spelman JJ, Cullis CA, Langston SP, Vyskocil S, Sells TB, Mallender WD, Visiers I, Li P, Claiborne CF, Rolfe M, Bolen JB, Dick LR.

Mol Cell. 2010 Jan 15;37(1):102-11. doi: 10.1016/j.molcel.2009.12.024.


Synergistic antitumor effect between vorinostat and topotecan in small cell lung cancer cells is mediated by generation of reactive oxygen species and DNA damage-induced apoptosis.

Bruzzese F, Rocco M, Castelli S, Di Gennaro E, Desideri A, Budillon A.

Mol Cancer Ther. 2009 Nov;8(11):3075-87. doi: 10.1158/1535-7163.MCT-09-0254. Epub 2009 Nov 3.


Development of a charcoal paper adenosine triphosphate:pyrophosphate exchange assay: kinetic characterization of NEDD8 activating enzyme.

Bruzzese FJ, Tsu CA, Ma J, Loke HK, Wu D, Li Z, Tayber O, Dick LR.

Anal Biochem. 2009 Nov 1;394(1):24-9. doi: 10.1016/j.ab.2009.07.011. Epub 2009 Jul 12.


Modulation of thymidilate synthase and p53 expression by HDAC inhibitor vorinostat resulted in synergistic antitumor effect in combination with 5FU or raltitrexed.

Di Gennaro E, Bruzzese F, Pepe S, Leone A, Delrio P, Subbarayan PR, Avallone A, Budillon A.

Cancer Biol Ther. 2009 May;8(9):782-91. Epub 2009 May 9.


Histone deacetylase inhibitors: a new wave of molecular targeted anticancer agents.

Budillon A, Di Gennaro E, Bruzzese F, Rocco M, Manzo G, Caraglia M.

Recent Pat Anticancer Drug Discov. 2007 Jun;2(2):119-34. Review.


Synergistic antitumour effect of raltitrexed and 5-fluorouracil plus folinic acid combination in human cancer cells.

Avallone A, Di Gennaro E, Bruzzese F, Laus G, Delrio P, Caraglia M, Pepe S, Comella P, Budillon A.

Anticancer Drugs. 2007 Aug;18(7):781-91.


Comparison of biochemical and biological effects of ML858 (salinosporamide A) and bortezomib.

Williamson MJ, Blank JL, Bruzzese FJ, Cao Y, Daniels JS, Dick LR, Labutti J, Mazzola AM, Patil AD, Reimer CL, Solomon MS, Stirling M, Tian Y, Tsu CA, Weatherhead GS, Zhang JX, Rolfe M.

Mol Cancer Ther. 2006 Dec;5(12):3052-61.


Synergistic antitumor activity of epidermal growth factor receptor tyrosine kinase inhibitor gefitinib and IFN-alpha in head and neck cancer cells in vitro and in vivo.

Bruzzese F, Di Gennaro E, Avallone A, Pepe S, Arra C, Caraglia M, Tagliaferri P, Budillon A.

Clin Cancer Res. 2006 Jan 15;12(2):617-25.


Multiple-target drugs: inhibitors of heat shock protein 90 and of histone deacetylase.

Budillon A, Bruzzese F, Di Gennaro E, Caraglia M.

Curr Drug Targets. 2005 May;6(3):337-51. Review.


Acetylation of proteins as novel target for antitumor therapy: review article.

Di Gennaro E, Bruzzese F, Caraglia M, Abruzzese A, Budillon A.

Amino Acids. 2004 Jul;26(4):435-41. Epub 2004 Jun 11. Review.


Critical role of both p27KIP1 and p21CIP1/WAF1 in the antiproliferative effect of ZD1839 ('Iressa'), an epidermal growth factor receptor tyrosine kinase inhibitor, in head and neck squamous carcinoma cells.

Di Gennaro E, Barbarino M, Bruzzese F, De Lorenzo S, Caraglia M, Abbruzzese A, Avallone A, Comella P, Caponigro F, Pepe S, Budillon A.

J Cell Physiol. 2003 Apr;195(1):139-50.


Inhibition of IMPDH by mycophenolic acid: dissection of forward and reverse pathways using capillary electrophoresis.

Fleming MA, Chambers SP, Connelly PR, Nimmesgern E, Fox T, Bruzzese FJ, Hoe ST, Fulghum JR, Livingston DJ, Stuver CM, Sintchak MD, Wilson KP, Thomson JA.

Biochemistry. 1996 Jun 4;35(22):6990-7.


Enthalpy of hydrogen bond formation in a protein-ligand binding reaction.

Connelly PR, Aldape RA, Bruzzese FJ, Chambers SP, Fitzgibbon MJ, Fleming MA, Itoh S, Livingston DJ, Navia MA, Thomson JA, et al.

Proc Natl Acad Sci U S A. 1994 Mar 1;91(5):1964-8.


Resonance Raman spectroscopy of chemically modified hemoglobins.

Bruzzese FJ, Dix JA, Rava RP, Cerny LC.

Biomater Artif Cells Artif Organs. 1990;18(2):143-56.


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