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Publications 2009

Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.
Ontoria JM, Altamura S, Di Marco A, Ferrigno F, Laufer R, Muraglia E, Palumbi MC, Rowley M, Scarpelli R, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P. (2009)
J Med Chem. 2009 Nov 12;52(21):6782-9.

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Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.
Ontoria JM, Rydberg EH, Di Marco S, Tomei L, Attenni B, Malancona S, Martin Hernando JI, Gennari N, Koch U, Narjes F, Rowley M, Summa V, Carroll SS, Olsen DB, De Francesco R, Altamura S, Migliaccio G, Carfì A. (2009)
J Med Chem. 2009 Aug 27;52(16):5217-27.

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Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Jones P, Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S, Monteagudo E, Ontoria JM, Orsale MV, Palumbi MC, Pesci S, Roscilli G, Scarpelli R, Schultz-Fademrecht C, Toniatti C, Rowley M. (2009)
J Med Chem. 2009 Nov 26;52(22):7170-85.

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2-(3-Thienyl)-5,6-dihydroxypyrimidine-4-carboxylic acids as inhibitors of HCV NS5B RdRp.
Pacini B, Avolio S, Ercolani C, Koch U, Migliaccio G, Narjes F, Pacini L, Tomei L, Harper S. (2009)
Bioorg Med Chem Lett. 2009 Nov 1;19(21):6245-9.

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Phosphoramidate prodrugs of 2′-C-methylcytidine for therapy of hepatitis C virus infection.
Gardelli C, Attenni B, Donghi M, Meppen M, Pacini B, Harper S, Di Marco A, Fiore F, Giuliano C, Pucci V, Laufer R, Gennari N, Marcucci I, Leone JF, Olsen DB, MacCoss M, Rowley M, Narjes F. (2009)
J Med Chem. 2009 Sep 10;52(17):5394-407.

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Engineered adenovirus serotypes for overcoming anti-vector immunity.
Dharmapuri S, Peruzzi D, Aurisicchio L. (2009)
Expert Opin Biol Ther. 2009 Oct;9(10):1279-87.

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2-D Difference in gel electrophoresis combined with Pro-Q Diamond staining: a successful approach for the identification of kinase/phosphatase targets.
Orsatti L, Forte E, Tomei L, Caterino M, Pessi A, Talamo F. (2009)
Electrophoresis. 2009 Jul;30(14):2469-76.

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Mass spectrometry study of PRL-3 phosphatase inactivation by disulfide bond formation and cysteine into glycine conversion.
Orsatti L, Innocenti F, Lo Surdo P, Talamo F, Barbato G. (2009)
Rapid Commun Mass Spectrom. 2009 Sep;23(17):2733-40.

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Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles.
Harper S, Ferrara M, Crescenzi B, Pompei M, Palumbi MC, DiMuzio JM, Donghi M, Fiore F, Koch U, Liverton NJ, Pesci S, Petrocchi A, Rowley M, Summa V, Gardelli C. (2009)
J Med Chem. 2009 Aug 13;52(15):4820-37.

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Coadministration of telomerase genetic vaccine and a novel TLR9 agonist in nonhuman primates.
Dharmapuri S, Peruzzi D, Mennuni C, Calvaruso F, Giampaoli S, Barbato G, Kandimalla ER, Agrawal S, Scarselli E, Mesiti G, Ciliberto G, La Monica N, Aurisicchio L. (2009)
Mol Ther. 2009 Oct;17(10):1804-13.

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Loss of histone deacetylase 4 causes segregation defects during mitosis of p53-deficient human tumor cells.
Cadot B, Brunetti M, Coppari S, Fedeli S, de Rinaldis E, Dello Russo C, Gallinari P, De Francesco R, Steinkühler C, Filocamo G. (2009)
Cancer Res. 2009 Aug 1;69(15):6074-82.

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Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: improving cell based activity by the quaternarization of a chiral center.
Nizi E, Orsale MV, Crescenzi B, Pescatore G, Muraglia E, Alfieri A, Gardelli C, Spieser SA, Summa V. (2009)
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4617-21.

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Metabolism-related liabilities of a potent histone deacetylase (HDAC) inhibitor and relevance of the route of administration on its metabolic fate.
Fonsi M, Fiore F, Jones P, Kinzel O, Laufer R, Rowley M, Monteagudo E. (2009)
Xenobiotica. 2009 Oct;39(10):722-37.

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Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.
Branca D, Cerretani M, Jones P, Koch U, Orvieto F, Palumbi MC, Rowley M, Toniatti C, Muraglia E. (2009)
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4042-5.

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Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.
Orvieto F, Branca D, Giomini C, Jones P, Koch U, Ontoria JM, Palumbi MC, Rowley M, Toniatti C, Muraglia E. (2009)
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4196-200.

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Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.
Dessole G, Branca D, Ferrigno F, Kinzel O, Muraglia E, Palumbi MC, Rowley M, Serafini S, Steinkühler C, Jones P. (2009)
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4191-5.

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N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors.
Petrocchi A, Jones P, Rowley M, Fiore F, Summa V. (2009)
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4245-9.

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An indirect method to measure trimerization constants using surface plasmon resonance.
Mattu M, Bendtsen C, Barbato G. (2009)
Anal Biochem. 2009 Oct 1;393(1):126-8.

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Cyclic phosphoramidates as prodrugs of 2′-C-methylcytidine.
Meppen M, Pacini B, Bazzo R, Koch U, Leone JF, Koeplinger KA, Rowley M, Altamura S, Di Marco A, Fiore F, Giuliano C, Gonzalez-Paz O, Laufer R, Pucci V, Narjes F, Gardelli C. (2009)
Eur J Med Chem. 2009 Sep;44(9):3765-70.

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Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
Kinzel O, Llauger-Bufi L, Pescatore G, Rowley M, Schultz-Fademrecht C, Monteagudo E, Fonsi M, Gonzalez Paz O, Fiore F, Steinkühler C, Jones P. (2009)
J Med Chem. 2009 Jun 11;52(11):3453-6.

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Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
Attenni B, Ontoria JM, Cruz JC, Rowley M, Schultz-Fademrecht C, Steinkühler C, Jones P. (2009)
Bioorg Med Chem Lett. 2009 Jun 1;19(11):3081-4.

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Smoothened antagonists: a promising new class of antitumor agents.
Gallinari P, Filocamo G, Jones P, Pazzaglia S, Steinkühler C. (2009)
Expert Opin Drug Discov. 2009 May;4(5):525-44.

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A peptide vaccine based on retro-inverso beta-amyloid sequences fails to elicit a cross-reactive immune response.
Bianchi E, Ingallinella P, Finotto M, Liang X, Kinney GG, Pessi A. (2009)
Adv Exp Med Biol. 2009;611:363-4.

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A strategy for selectively shielding portions of a peptide/protein from immune response while maintaining immunogenicity of contiguous epitopes.
Bianchi E, Finotto M, Ingallinella P, Citron M, Hrin R, Lu M, Geleziunas R, Miller MD, Liang X, Pessi A. (2009)
Adv Exp Med Biol. 2009;611:359-60.

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Synthetic peptide vaccines: the quest to develop peptide vaccines for influenza, HIV and Alzheimer’s disease.
Bianchi E, Ingallinella P, Finotto M, Joyce J, Liang X, Miller MD, Kinney GG, Ciliberto G, Shiver JW, Pessi A. (2009)
Adv Exp Med Biol. 2009;611:121-3.

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Phosphorous acid analogs of novel P2-P4 macrocycles as inhibitors of HCV-NS3 protease.
Pompei M, Francesco ME, Koch U, Liverton NJ, Summa V. (2009)
Bioorg Med Chem Lett. 2009 May 1;19(9):2574-8.

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Comparative expression pathway analysis of human and canine mammary tumors.
Uva P, Aurisicchio L, Watters J, Loboda A, Kulkarni A, Castle J, Palombo F, Viti V, Mesiti G, Zappulli V, Marconato L, Abramo F, Ciliberto G, Lahm A, La Monica N, de Rinaldis E. (2009)
BMC Genomics. 2009 Mar 27;10:135.

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Inhibitors of hepatitis C virus NS3/4A: alpha-ketoamide based macrocyclic inhibitors.
Avolio S, Robertson K, Hernando JI, DiMuzio J, Summa V. (2009)
Bioorg Med Chem Lett. 2009 Apr 15;19(8):2295-8.

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3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates–a new class of HIV-1 integrase inhibitors.
Donghi M, Kinzel OD, Summa V. (2009)
Bioorg Med Chem Lett. 2009 Apr 1;19(7):1930-4.

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Synthesis and evaluation of novel phosphoramidate prodrugs of 2′-methyl cytidine as inhibitors of hepatitis C virus NS5B polymerase.
Donghi M, Attenni B, Gardelli C, Marco AD, Fiore F, Giuliano C, Laufer R, Leone JF, Pucci V, Rowley M, Narjes F. (2009)
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1392-5.

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A novel chimpanzee serotype-based adenoviral vector as delivery tool for cancer vaccines.
Peruzzi D, Dharmapuri S, Cirillo A, Bruni BE, Nicosia A, Cortese R, Colloca S, Ciliberto G, La Monica N, Aurisicchio L. (2009)
Vaccine. 2009 Feb 25;27(9):1293-300.

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Discovery of pentacyclic compounds as potent inhibitors of hepatitis C virus NS5B RNA polymerase.
Habermann J, Capitò E, Ferreira Mdel R, Koch U, Narjes F. (2009)
Bioorg Med Chem Lett. 2009 Feb 1;19(3):633-8.

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An oral TLR7 agonist is a potent adjuvant of DNA vaccination in transgenic mouse tumor models.
Dharmapuri S, Aurisicchio L, Neuner P, Verdirame M, Ciliberto G, La Monica N. (2009)
Cancer Gene Ther. 2009 May;16(5):462-72.

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Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
Scarpelli R, Di Marco A, Ferrigno F, Laufer R, Marcucci I, Muraglia E, Ontoria JM, Rowley M, Serafini S, Steinkühler C, Jones P. (2008)
Bioorg Med Chem Lett. 2008 Dec 1;18(23):6078-82.

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A therapeutic cancer vaccine targeting carcinoembryonic antigen in intestinal carcinomas.
Mori F, Giannetti P, Peruzzi D, Lazzaro D, Giampaoli S, Kaufman HL, Ciliberto G, La Monica N, Aurisicchio L. (2009)
Hum Gene Ther. 2009 Feb;20(2):125-36.

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