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At IRBM, our scientists work alongside our partners to advance scientific knowledge as well as to develop life-saving drugs. Here is a sample of the publications written by our researchers over the years.

2018

Esposito S, de Leonibus ML, Ingenito R, Bianchi E, Orsatti L, Monteagudo E. (2018) A liquid chromatography high-resolution mass spectrometry in vitro assay to assess metabolism at the injection site of subcutaneously administered therapeutic peptides.
J Pharm Biomed Anal 2018 Jul 10; 159;449-458 [Epub ahead of print]

Bresciani A, Cecchetti O, Missineo A, Pacifici PG, Tomei L, Rodems S. (2018) Development of a Broadly Applicable Assay for Measurement of Glycan-Directed Enzymatic Activity.
SLAS Discov 2018 Jun 1: 2472555218782625. doi: 10.1177/2472555218782625 [Epub ahead of print]

Di Marino S, Viceconte N, Lembo A, Summa V, Tanzilli G, Raparelli V, Truscelli G, Mangieri E, Gaudio C, Cicero DO. (2018) Early metabolic response to acute myocardial ischaemia in patients undergoing elective coronary angioplasty.
Open Heart 2018 Mar 10;5(1): e000709

Nizi E, Sferrazza A, Fabbrini D, Nardi V, Andreini M, Graziani R, Gennari N, Bresciani A, Paonessa G, Harper S. (2018) Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.
Bioorg Med Chem Lett 2018 May 15;28(9): 1540-1544.

Bresciani A, Spiezia MC, Boggio R, Cariulo C, Nordheim A, Altobelli R, Kuhlbrodt K, Dominguez C, Munoz-Sanjuan I, Wityak J, Fodale V, Marchionini DM, Weiss A. (2018) Quantifying autophagy using novel LC3B and p62 TR-FRET assays.
PLoS One 2018 Mar 19;13(3):e0194423

Speziale R, Montesano C, De Leonibus ML, Bonelli F, Fezzardi P, Beconi MG, Monteagudo E, Elbaum D, Orsatti L. (2018) Determination of acetyl coenzyme A in human whole blood by ultra-performance liquid chromatography-mass spectrometry.
J Chromatogr B Analyt Technol Biomed Life Sci 2018 April 15;1083:57-62

Elbaum D, Beconi MG, Monteagudo E, Di Marco A, Quinton MS, Lyons KA, Vaino A, Harper S. (2018) Fosmetpantotenate (RE-024), a phosphopantothenate replacement therapy for pantothenate kinase-associated neurodegeneration: Mechanism of action and efficacy in nonclinical models.
PLoS One 2018 Mar 9;13(3):e0192028

Demartis A, Lahm A, Tomei L, Beghetto E, Di Biasio V, Orvieto F, Frattolillo F, Carrington PE, Mumick S, Hawes B, Bianchi E, Palani A, Pessi A. (2018) Polypharmacy through Phage Display: Selection of Glucagon and GLP-1 Receptor Co-agonists from a Phage-Displayed Peptide Library. Sci Rep. 2018 Jan 12;8(1):585.

2017

Mori M, Kovalenko L, Malancona S, Saladini F, De Forni D, Pires M, Humbert N, Real E, Botzanowski T, Cianférani S, Giannini A, Dasso Lang MC, Cugia G, Poddesu B, Lori F, Zazzi M, Harper S, Summa V, Mely Y, Botta M. (2017) Structure-Based Identification of HIV-1 Nucleocapsid Protein Inhibitors Active against Wild-Type and Drug-Resistant HIV-1 Strains. ACS Chem Biol. 2017 Dec 28.

Cariulo C, Azzollini L, Verani M, Martufi P, Boggio R, Chiki A, Deguire SM, Cherubini M, Gines S, Marsh JL, Conforti P, Cattaneo E, Santimone I, Squitieri F, Lashuel HA, Petricca L, Caricasole A. (2017) Phosphorylation of huntingtin at residue T3 is decreased in Huntington’s disease and modulates mutant huntingtin protein conformation. Proc Natl Acad Sci U S A. 2017 Dec 12;114(50):E10809-E10818.

Fodale V, Boggio R, Daldin M, Cariulo C, Spiezia MC, Byrne LM, Leavitt BR, Wild EJ, Macdonald D, Weiss A, Bresciani A. (2017) Validation of Ultrasensitive Mutant Huntingtin Detection in Human Cerebrospinal Fluid by Single Molecule Counting Immunoassay. J Huntingtons Dis. 2017;6(4):349-361.

Poli G, Di Fabio R, Ferrante L, Summa V, Botta M. (2017) Largazole Analogues as Histone Deacetylase Inhibitors and Anticancer Agents: An Overview of Structure-Activity Relationships. ChemMedChem. 2017 Dec 7;12(23):1917-1926.

Noguera ME, Aran M, Smal C, Vazquez DS, Herrera MG, Roman EA, Alaimo N, Gallo M, Santos J. (2017) Insights on the conformational dynamics of human frataxin through modifications of loop-1. Arch Biochem Biophys. 2017 Dec 15;636:123-137.

Lania G, Bresciani A, Bisbocci M, Francone A, Colonna V, Altamura S, Baldini A. (2017) Vitamin B12 ameliorates the phenotype of a mouse model of DiGeorge syndrome. Hum Mol Genet. 2017 Nov 15;26(22):4540.

Guidi A, Lalli C, Gimmelli R, Nizi E, Andreini M, Gennari N, Saccoccia F, Harper S, Bresciani A, Ruberti G. (2017) Discovery by organism based high-throughput screening of new multi-stage compounds affecting Schistosoma mansoni viability, egg formation and production. PLoS Negl Trop Dis. 2017 Oct 6;11(10):e0005994.

Bresciani A, Missineo A, Gallo M, Cerretani M, Fezzardi P, Tomei L, Cicero DO, Altamura S, Santoprete A, Ingenito R, Bianchi E, Pacifici R, Dominguez C, Munoz-Sanjuan I, Harper S, Toledo-Sherman L, Park LC. (2017) Nuclear factor (erythroid-derived 2)-like 2 (NRF2) drug discovery: Biochemical toolbox to develop NRF2 activators by reversible binding of Kelch-like ECH-associated protein 1 (KEAP1). Arch Biochem Biophys. 2017 Oct 1;631:31-41.

Daldin M, Fodale V, Cariulo C, Azzollini L, Verani M, Martufi P, Spiezia MC, Deguire SM, Cherubini M, Macdonald D, Weiss A, Bresciani A, Vonsattel JG, Petricca L, Marsh JL, Gines S, Santimone I, Marano M, Lashuel HA, Squitieri F, Caricasole A. (2017) Polyglutamine expansion affects huntingtin conformation in multiple Huntington’s disease models. Sci Rep. 2017 Jul 11;7(1):5070.

Piras M, Testa A, Fleming IN, Dall’Angelo S, Andriu A, Menta S, Mori M, Brown GD, Forster D, Williams KJ, Zanda M. (2017) High-Affinity “Click” RGD Peptidomimetics as Radiolabeled Probes for Imaging αv β3 Integrin. ChemMedChem. 2017 Jul 20;12(14):1142-1151.

Gelmetti V, De Rosa P, Torosantucci L, Marini ES, Romagnoli A, Di Rienzo M, Arena G, Vignone D, Fimia GM, Valente EM. (2017) PINK1 and BECN1 relocalize at mitochondria-associated membranes during mitophagy and promote ER-mitochondria tethering and autophagosome formation. Autophagy. 2017 Apr 3;13(4):654-669.

Turcano L, Visaggio D, Frangipani E, Missineo A, Andreini M, Altamura S, Visca P, Bresciani A. (2017) Identification by High-Throughput Screening of Pseudomonas Acyl-Coenzyme A Synthetase Inhibitors. SLAS Discov. 2017 Aug;22(7):897-905.

Mladenović M, Patsilinakos A, Pirolli A, Sabatino M, Ragno R. (2017) Understanding the Molecular Determinant of Reversible Human Monoamine Oxidase B Inhibitors Containing 2H-Chromen-2-One Core: Structure-Based and Ligand-Based Derived Three-Dimensional Quantitative Structure-Activity Relationships Predictive Models. J Chem Inf Model. 2017 Apr 24;57(4):787-814.

Di Cesare E, Verrico A, Miele A, Giubettini M, Rovella P, Coluccia A, Famiglini V, La Regina G, Cundari E, Silvestri R, Lavia P. (2017) Mitotic cell death induction by targeting the mitotic spindle with tubulin-inhibitory indole derivative molecules. Oncotarget. 2017 Mar 21;8(12):19738-19759.

Esposito S, Mele R, Ingenito R, Bianchi E, Bonelli F, Monteagudo E, Orsatti L. (2017) An efficient liquid chromatography-high resolution mass spectrometry approach for the optimization of the metabolic stability of therapeutic peptides. Anal Bioanal Chem. 2017 Apr;409(10):2685-2696.

2016

Lania G, Bresciani A, Bisbocci M, Francone A, Colonna V, Altamura S, Baldini A. (2016) Vitamin B12 ameliorates the phenotype of a mouse model of DiGeorge syndrome. Hum Mol Genet. 2016 Oct 15;25(20):4369-4375.

Verani M, Bustamante M, Martufi P, Daldin M, Cariulo C, Azzollini L, Fodale V, Puglisi F, Weiss A, Macdonald D, Petricca L, Caricasole A. (2016) Conformational modulation mediated by polyglutamine expansion in CAG repeat expansion disease-associated proteins. Biochem Biophys Res Commun. 2016 Sep 16;478(2):949-55.

Guidi A, Lalli C, Perlas E, Bolasco G, Nibbio M, Monteagudo E, Bresciani A, Ruberti G. (2016) Discovery and Characterization of Novel Anti-schistosomal Properties of the Anti-anginal Drug, Perhexiline and Its Impact on Schistosoma mansoni Male and Female Reproductive Systems. PLoS Negl Trop Dis. 2016 Aug 12;10(8):e0004928.

Simonelli V, Leuzzi G, Basile G, D’Errico M, Fortini P, Franchitto A, Viti V, Brown AR, Parlanti E, Pascucci B, Palli D, Giuliani A, Palombo F, Sobol RW, Dogliotti E. (2016) Crosstalk between mismatch repair and base excision repair in human gastric cancer. Oncotarget. 2016 Jun 20;8(49):84827-84840.

Ontoria JM, Paonessa G, Ponzi S, Ferrigno F, Nizi E, Biancofiore I, Malancona S, Graziani R, Roberts D, Willis P, Bresciani A, Gennari N, Cecchetti O, Monteagudo E, Orsale MV, Veneziano M, Di Marco A, Cellucci A, Laufer R, Altamura S, Summa V, Harper S. (2016) Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs. ACS Med Chem Lett. 2016 Mar 5;7(5):454-9.

Filocamo G, Brunetti M, Colaceci F, Sasso R, Tanori M, Pasquali E, Alfonsi R, Mancuso M, Saran A, Lahm A, Di Marcotullio L, Steinkühler C, Pazzaglia S. (2016) MK-4101, a Potent Inhibitor of the Hedgehog Pathway, Is Highly Active against Medulloblastoma and Basal Cell Carcinoma. Mol Cancer Ther. 2016 Jun;15(6):1177-89.

Esposito S, Bracacel E, Nibbio M, Speziale R, Orsatti L, Veneziano M, Monteagudo E, Bonelli F. (2016) Use of ‘dilute-and-shoot’ liquid chromatography-high resolution mass spectrometry in preclinical research: application to a DMPK study of perhexiline in mouse plasma. J Pharm Biomed Anal. 2016 Jan 25;118:70-80.

2015

Ullman C, Mathonet P, Oleksy A, Diamandakis A, Tomei L, Demartis A, Nardi C, Sambucini S, Missineo A, Alt K, Hagemeyer CE, Harris M, Hedt A, Weis R, Gehlsen KR. (2015) High Affinity Binders to EphA2 Isolated from Abdurin Scaffold Libraries; Characterization, Binding and Tumor Targeting. PLoS One. 2015 Aug 27;10(8):e0135278.

Bustamante MB, Ansaloni A, Pedersen JF, Azzollini L, Cariulo C, Wang ZM, Petricca L, Verani M, Puglisi F, Park H, Lashuel H, Caricasole A. (2015) Detection of huntingtin exon 1 phosphorylation by Phos-Tag SDS-PAGE: Predominant phosphorylation on threonine 3 and regulation by IKKβ. Biochem Biophys Res Commun. 2015 Aug 7;463(4):1317-22.

Kalathur M, Toso A, Chen J, Revandkar A, Danzer-Baltzer C, Guccini I, Alajati A, Sarti M, Pinton S, Brambilla L, Di Mitri D, Carbone G, Garcia-Escudero R, Padova A, Magnoni L, Tarditi A, Maccari L, Malusa F, Kalathur RK, A Pinna L, Cozza G, Ruzzene M, Delaleu N, Catapano CV, Frew IJ, Alimonti A. (2015) A chemogenomic screening identifies CK2 as a target for pro-senescence therapy in PTEN-deficient tumours. Nat Commun. 2015 Jun 18;6:7227.

Orsatti L, Speziale R, Orsale MV, Caretti F, Veneziano M, Zini M, Monteagudo E, Lyons K, Beconi M, Chan K, Herbst T, Toledo-Sherman L, Munoz-Sanjuan I, Bonelli F, Dominguez C. (2015) A single-run liquid chromatography mass spectrometry method to quantify neuroactive kynurenine pathway metabolites in rat plasma. J Pharm Biomed Anal. 2015 Mar 25;107:426-31.

Lalli C, Guidi A, Gennari N, Altamura S, Bresciani A, Ruberti G. (2015) Development and validation of a luminescence-based, medium-throughput assay for drug screening in Schistosoma mansoni. PLoS Negl Trop Dis. 2015 Jan 30;9(1):e0003484.

Fodale V, Kegulian NC, Verani M, Cariulo C, Azzollini L, Petricca L, Daldin M, Boggio R, Padova A, Kuhn R, Pacifici R, Macdonald D, Schoenfeld RC, Park H, Isas JM, Langen R, Weiss A, Caricasole A. (2014, 2015) Polyglutamine- and temperature-dependent conformational rigidity in mutant huntingtin revealed by immunoassays and circular dichroism spectroscopy. PLoS One. 2014 Dec 2;9(12):e112262. Erratum in: PLoS One. 2015;10(6):e0129986.

Montagner G, Gemmo C, Fabbri E, Manicardi A, Accardo I, Bianchi N, Finotti A, Breveglieri G, Salvatori F, Borgatti M, Lampronti I, Bresciani A, Altamura S, Corradini R, Gambari R. (2015) Peptide nucleic acids targeting β-globin mRNAs selectively inhibit hemoglobin production in murine erythroleukemia cells. Int J Mol Med. 2015 Jan;35(1):51-8.

2014

Bridges KA, Toniatti C, Buser CA, Liu H, Buchholz TA, Meyn RE. (2014) Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

Neuner P, Peier AM, Talamo F, Ingallinella P, Lahm A, Barbato G, Di Marco A, Desai K, Zytko K, Qian Y, Du X, Ricci D, Monteagudo E, Laufer R, Pocai A, Bianchi E, Marsh DJ, Pessi A. (2014) Development of a neuromedin U-human serum albumin conjugate as a long-acting candidate for the treatment of obesity and diabetes. Comparison with the PEGylated peptide. J Pept Sci. 2014 Jan;20(1):7-19.

Aurisicchio L, Peruzzi D, Koo G, Wei WZ, La Monica N, Ciliberto G. (2014) Immunogenicity and therapeutic efficacy of a dual-component genetic cancer vaccine cotargeting carcinoembryonic antigen and HER2/neu in preclinical models. Hum Gene Ther. 2014 Feb;25(2):121-31.

2013

Bianchi E, Carrington PE, Ingallinella P, Finotto M, Santoprete A, Petrov A, Eiermann G, Kosinski J, Marsh DJ, Pocai A, SinhaRoy R, Pessi A. (2013) A PEGylated analog of the gut hormone oxyntomodulin with long-lasting antihyperglycemic, insulinotropic and anorexigenic activity. Bioorg Med Chem. 2013 Nov 15;21(22):7064-73.

Baxa M, Hruska-Plochan M, Juhas S, Vodicka P, Pavlok A, Juhasova J, Miyanohara A, Nejime T, Klima J, Macakova M, Marsala S, Weiss A, Kubickova S, Musilova P, Vrtel R, Sontag EM, Thompson LM, Schier J, Hansikova H, Howland DS, Cattaneo E, DiFiglia M, Marsala M, Motlik J. (2013) A transgenic minipig model of Huntington’s Disease. J Huntingtons Dis. 2013;2(1):47-68.

Huntington’s Disease Sheep Collaborative Research Group, Reid SJ, Patassini S, Handley RR, Rudiger SR, McLaughlan CJ, Osmand A, Jacobsen JC, Morton AJ, Weiss A, Waldvogel HJ, MacDonald ME, Gusella JF, Bawden CS, Faull RL, Snell RG. (2013) Further molecular characterisation of the OVT73 transgenic sheep model of Huntington’s disease identifies cortical aggregates. J Huntingtons Dis. 2013;2(3):279-95.

2012

Ingallinella P, Peier AM, Pocai A, Marco AD, Desai K, Zytko K, Qian Y, Du X, Cellucci A, Monteagudo E, Laufer R, Bianchi E, Marsh DJ, Pessi A. (2012) PEGylation of Neuromedin U yields a promising candidate for the treatment of obesity and diabetes. Bioorg Med Chem. 2012 Aug 1;20(15):4751-9.

Harper S, McCauley JA, Rudd MT, Ferrara M, DiFilippo M, Crescenzi B, Koch U, Petrocchi A, Holloway MK, Butcher JW, Romano JJ, Bush KJ, Gilbert KF, McIntyre CJ, Nguyen KT, Nizi E, Carroll SS, Ludmerer SW, Burlein C, DiMuzio JM, Graham DJ, McHale CM, Stahlhut MW, Olsen DB, Monteagudo E, Cianetti S, Giuliano C, Pucci V, Trainor N, Fandozzi CM, Rowley M, Coleman PJ, Vacca JP, Summa V, Liverton NJ. (2012) Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. ACS Med Chem Lett. 2012 Mar 2;3(4):332-6.

2011

Lo Surdo P, Bottomley MJ, Calzetta A, Settembre EC, Cirillo A, Pandit S, Ni YG, Hubbard B, Sitlani A, Carfí A. (2011) Mechanistic implications for LDL receptor degradation from the PCSK9/LDLR structure at neutral pH. EMBO Rep. 2011 Dec 1;12(12):1300-5.

Di Giovine P, Settembre EC, Bhargava AK, Luftig MA, Lou H, Cohen GH, Eisenberg RJ, Krummenacher C, Carfi A. (2011) Structure of herpes simplex virus glycoprotein D bound to the human receptor nectin-1. PLoS Pathog. 2011 Sep;7(9):e1002277.

Ontoria JM, Bufi LL, Torrisi C, Bresciani A, Giomini C, Rowley M, Serafini S, Bin H, Hao W, Steinkühler C, Jones P. (2011) Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5274-82.

Muraglia E, Ontoria JM, Branca D, Dessole G, Bresciani A, Fonsi M, Giuliano C, Llauger Bufi L, Monteagudo E, Palumbi MC, Torrisi C, Rowley M, Steinkühler C, Jones P. (2011) N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5283-8.

Malancona S, Altamura S, Filocamo G, Kinzel O, Hernando JI, Rowley M, Scarpelli R, Steinkühler C, Jones P. (2011) Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4422-8.

Kinzel O, Alfieri A, Altamura S, Brunetti M, Bufali S, Colaceci F, Ferrigno F, Filocamo G, Fonsi M, Gallinari P, Malancona S, Hernando JI, Monteagudo E, Orsale MV, Palumbi MC, Pucci V, Rowley M, Sasso R, Scarpelli R, Steinkühler C, Jones P. (2011) Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4429-35.

Dharmapuri S, Peruzzi D, Marra E, Palombo F, Bett AJ, Bartz SR, Yong M, Ciliberto G, La Monica N, Buser CA, Toniatti C, Aurisicchio L. (2011) Intratumor RNA interference of cell cycle genes slows down tumor progression. Gene Ther. 2011 Jul;18(7):727-33.

2010

Monteagudo E, Fonsi M, Chu X, Bleasby K, Evers R, Pucci V, Orsale MV, Cianetti S, Ferrara M, Harper S, Laufer R, Rowley M, Summa V. (2010) The metabolism and disposition of a potent inhibitor of hepatitis C virus NS3/4A protease. Xenobiotica. 2010 Dec;40(12):826-39.

Ferrara M, Fiore F, Summa V, Gardelli C. (2010) Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5031-4.

Peruzzi D, Gavazza A, Mesiti G, Lubas G, Scarselli E, Conforti A, Bendtsen C, Ciliberto G, La Monica N, Aurisicchio L. (2010) A vaccine targeting telomerase enhances survival of dogs affected by B-cell lymphoma. Mol Ther. 2010 Aug;18(8):1559-67.

Cipriani B. (2009) Immunological markers of cancer vaccine efficacy and their clinical relevance. Biomark Med. 2009 Jun;3(3):253-64.

Malancona S, Donghi M, Ferrara M, Martin Hernando JI, Pompei M, Pesci S, Ontoria JM, Koch U, Rowley M, Summa V. (2010) Allosteric inhibitors of hepatitis C virus NS5B polymerase thumb domain site II: structure-based design and synthesis of new templates. Bioorg Med Chem. 2010 Apr 15;18(8):2836-48.

Cianetti S, Cooper VB, Attenni B, Pucci V, Fiore F, Giuliano C, Laufer R, Gardelli C, Monteagudo E, Narjes F, Pearce GE, Rowley M. (2010) Enhancement of intestinal absorption of 2-methyl cytidine prodrugs. Drug Deliv. 2010 May;17(4):214-22.

Pescatore G, Branca D, Fiore F, Kinzel O, Bufi LL, Muraglia E, Orvieto F, Rowley M, Toniatti C, Torrisi C, Jones P. (2010) Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2010 Feb 1;20(3):1094-9.

Ferrigno F, Branca D, Kinzel O, Lillini S, Llauger Bufi L, Monteagudo E, Muraglia E, Rowley M, Schultz-Fademrecht C, Toniatti C, Torrisi C, Jones P. (2010) Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1100-5.

Torrisi C, Bisbocci M, Ingenito R, Ontoria JM, Rowley M, Schultz-Fademrecht C, Toniatti C, Jones P. (2010) Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2010 Jan 15;20(2):448-52.

Scarpelli R, Boueres JK, Cerretani M, Ferrigno F, Ontoria JM, Rowley M, Schultz-Fademrecht C, Toniatti C, Jones P. (2010) Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors. Bioorg Med Chem Lett. 2010 Jan 15;20(2):488-92.

Peruzzi D, Mesiti G, Ciliberto G, La Monica N, Aurisicchio L. (2010) Telomerase and HER-2/neu as targets of genetic cancer vaccines in dogs. Vaccine. 2010 Feb 3;28(5):1201-8.

Pompei M, Di Francesco ME, Pesci S, Koch U, Vignetti SE, Veneziano M, Pace P, Summa V. (2010) Novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease by P3 succinamide fragment depeptidization strategy. Bioorg Med Chem Lett. 2010 Jan 1;20(1):168-74.

Ingenito R, Burton C, Langella A, Chen X, Zytko K, Pessi A, Wang J, Bianchi E. (2010) Novel potent apoA-I peptide mimetics that stimulate cholesterol efflux and pre-beta particle formation in vitro. Bioorg Med Chem Lett. 2010 Jan 1;20(1):236-9.

Verdirame M, Veneziano M, Alfieri A, Di Marco A, Monteagudo E, Bonelli F. (2010) Turbulent flow chromatography TFC-tandem mass spectrometry supporting in vitro/vivo studies of NCEs in high throughput fashion. J Pharm Biomed Anal. 2010 Mar 11;51(4):834-41.

2009

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) 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. J Med Chem. 2009 Nov 12;52(21):6782-9.

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) Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors. J Med Chem. 2009 Aug 27;52(16):5217-27.

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) 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. J Med Chem. 2009 Nov 26;52(22):7170-85.

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

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) Phosphoramidate prodrugs of 2′-C-methylcytidine for therapy of hepatitis C virus infection. J Med Chem. 2009 Sep 10;52(17):5394-407.

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

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

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

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) 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. J Med Chem. 2009 Aug 13;52(15):4820-37.

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) Coadministration of telomerase genetic vaccine and a novel TLR9 agonist in nonhuman primates. Mol Ther. 2009 Oct;17(10):1804-13.

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

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

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

Branca D, Cerretani M, Jones P, Koch U, Orvieto F, Palumbi MC, Rowley M, Toniatti C, Muraglia E. (2009) Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4042-5.
Orvieto F, Branca D, Giomini C, Jones P, Koch U, Ontoria JM, Palumbi MC, Rowley M, Toniatti C, Muraglia E. (2009) Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4196-200.

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

Petrocchi A, Jones P, Rowley M, Fiore F, Summa V. (2009) 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. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4245-9.

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

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) Cyclic phosphoramidates as prodrugs of 2′-C-methylcytidine. Eur J Med Chem. 2009 Sep;44(9):3765-70.

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) Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties. J Med Chem. 2009 Jun 11;52(11):3453-6.

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

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

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

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

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

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

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) Comparative expression pathway analysis of human and canine mammary tumors. BMC Genomics. 2009 Mar 27;10:135.

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

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

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

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

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

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

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

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

2008

Muraglia E, Altamura S, Branca D, Cecchetti O, Ferrigno F, Orsale MV, Palumbi MC, Rowley M, Scarpelli R, Steinkühler C, Jones P. (2008) 2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6083-7.

Fonsi M, Orsale MV, Monteagudo E. (2008) High-throughput microsomal stability assay for screening new chemical entities in drug discovery. J Biomol Screen. 2008 Oct;13(9):862-9.