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Sergio Altamura

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Savina Malancona; Michael Rowley; Rita Scarpelli; Christian Steinkühler; Sergio Altamura; Gessica Filocamo; Jose Ignacio Martin Hernando; Olaf Kinzel; Philip Jones
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.
Olaf Kinzel; Savina Malancona; Edith Monteagudo; Maria Orsale; Maria Cecilia Palumbi; Vincenzo Pucci; Michael Rowley; Romina Sasso; Rita Scarpelli; Christian Steinkühler; Anna Alfieri; Sergio Altamura; Mirko Brunetti; Simone Bufali; Fabrizio Colaceci; Federica Ferrigno; Gessica Filocamo; Massimiliano Fonsi; paola gallinari; Jose Ignacio Martin Hernando; Philip Jones
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.
Frank Narjes; Maria-Cecilia Palumbi; Ian Stansfield; Simone Zaramella; Sergio Altamura; Paola Baiocco; Stefania Colarusso; Immacolata Conte; Benedetta Crescenzi; Raffaele De Francesco; Stefania Di Marco; Caterina Ercolani; Marco Ferrara; Maria del Rosario Rico Ferreira; Fabrizio Fiore; Claudio Giuliano; Jörg Habermann; Uwe Koch; Ralph Laufer; Geert Leroux-Roels; Angela Claire Mackay; Philip Meuleman; Giovanni Migliaccio; Michael Rowley
Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.

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All Publications

2011: Savina Malancona; Michael Rowley; Rita Scarpelli; Christian Steinkühler; Sergio Altamura; Gessica Filocamo; Jose Ignacio Martin Hernando; Olaf Kinzel; Philip Jones
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.
Bioorganic & medicinal chemistry letters 2011;21(15):4422-8.
2011: Olaf Kinzel; Savina Malancona; Edith Monteagudo; Maria Orsale; Maria Cecilia Palumbi; Vincenzo Pucci; Michael Rowley; Romina Sasso; Rita Scarpelli; Christian Steinkühler; Anna Alfieri; Sergio Altamura; Mirko Brunetti; Simone Bufali; Fabrizio Colaceci; Federica Ferrigno; Gessica Filocamo; Massimiliano Fonsi; paola gallinari; Jose Ignacio Martin Hernando; Philip Jones
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.
Bioorganic & medicinal chemistry letters 2011;21(15):4429-35.
2011: Frank Narjes; Maria-Cecilia Palumbi; Ian Stansfield; Simone Zaramella; Sergio Altamura; Paola Baiocco; Stefania Colarusso; Immacolata Conte; Benedetta Crescenzi; Raffaele De Francesco; Stefania Di Marco; Caterina Ercolani; Marco Ferrara; Maria del Rosario Rico Ferreira; Fabrizio Fiore; Claudio Giuliano; Jörg Habermann; Uwe Koch; Ralph Laufer; Geert Leroux-Roels; Angela Claire Mackay; Philip Meuleman; Giovanni Migliaccio; Michael Rowley
Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.
Journal of medicinal chemistry 2011;54(1):289-301.
2009: Philip Jones; Sergio Altamura; Julia Boueres; Federica Ferrigno; Massimiliano Fonsi; Claudia Giomini; Stefania Lamartina; Edith Monteagudo; Jesus M Ontoria; Maria Vittoria Orsale; Maria Cecilia Palumbi; Silvia Pesci; Giuseppe Roscilli; Rita Scarpelli; Carsten Schultz-Fademrecht; Carlo Toniatti; Michael Rowley
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.
Journal of medicinal chemistry 2009;52(22):7170-85.
2009: Jesus M Ontoria; Sergio Altamura; Annalise Di Marco; Federica Ferrigno; Ralph Laufer; Ester Muraglia; Maria Cecilia Palumbi; Michael Rowley; Rita Scarpelli; Carsten Schultz-Fademrecht; Sergio Serafini; Christian Steinkühler; Philip Jones
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.
Journal of medicinal chemistry 2009;52(21):6782-9.
2009: Jesus M Ontoria; Edwin H Rydberg; Stefania Di Marco; Licia tomei; Barbara Attenni; Savina Malancona; José I Martin Hernando; Nadia Gennari; Uwe Koch; Frank Narjes; Michael Rowley; Vincenzo Summa; Steve S Carroll; David B Olsen; Raffaele De Francesco; Sergio Altamura; Giovanni Migliaccio; Andrea Carfì
Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.
Journal of medicinal chemistry 2009;52(16):5217-27.
2008: Marco Mattu; Paolo Di Giovine; Christian Steinkuhler; Raffaele De Francesco; Sergio Altamura; Ottavia Cecchetti; Andrea Carfì; Gaetano Barbato
Development and optimization of a binding assay for histone deacetylase 4 using surface plasmon resonance.
Analytical biochemistry 2008;377(2):267-9.
2008: Philip Jones; Sergio Altamura; Raffaele De Francesco; Odalys Gonzalez Paz; Olaf Kinzel; Giuseppe Mesiti; Edith Monteagudo; Giovanna Pescatore; Michael Rowley; Maria Verdirame; Christian Steinkühler
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
Journal of medicinal chemistry 2008;51(8):2350-3.
2008: Philip Jones; Sergio Altamura; Raffaele De Francesco; paola gallinari; Armin Lahm; Petra Neddermann; Michael Rowley; Sergio Serafini; Christian Steinkühler
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
Bioorganic & medicinal chemistry letters 2008;18(6):1814-9.
2006: Philip Jones; Sergio Altamura; Prasun K Chakravarty; Ottavia Cecchetti; Raffaele De Francesco; paola gallinari; Raffaele Ingenito; Peter T Meinke; Alessia Petrocchi; Michael Rowley; Rita Scarpelli; Sergio Serafini; Christian Steinkühler
A series of novel, potent, and selective histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(23):5948-52.
2006: Uwe Koch; Barbara Attenni; Savina Malancona; Stefania Colarusso; Immacolata Conte; Marcello Di Filippo; Steven Harper; Barbara Pacini; Claudia Giomini; Steven Thomas; Ilario Incitti; Licia tomei; Raffaele De Francesco; Sergio Altamura; Victor G Matassa; Frank Narjes
2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: discovery, SAR, modeling, and mutagenesis.
Journal of medicinal chemistry 2006;49(5):1693-705.
2005: Stefania Di Marco; Cinzia Volpari; Licia tomei; Sergio Altamura; Steven Harper; Frank Narjes; Uwe Koch; Michael Rowley; Raffaele De Francesco; Giovanni Migliaccio; Andrea Carfí
Interdomain communication in hepatitis C virus polymerase abolished by small molecule inhibitors bound to a novel allosteric site.
The Journal of biological chemistry 2005;280(33):29765-70.
2005: Steven Harper; Salvatore Avolio; Barbara Pacini; Marcello Di Filippo; Sergio Altamura; Licia tomei; Giacomo Paonessa; Stefania Di Marco; Andrea Carfi; Claudio Giuliano; Julio Padron; Fabio Bonelli; Giovanni Migliaccio; Raffaele De Francesco; Ralph Laufer; Michael Rowley; Frank Narjes
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase.
Journal of medicinal chemistry 2005;48(14):4547-57.
2005: Licia tomei; Sergio Altamura; Giacomo Paonessa; Raffaele De Francesco; Giovanni Migliaccio
HCV antiviral resistance: the impact of in vitro studies on the development of antiviral agents targeting the viral NS5B polymerase.
Antiviral chemistry & chemotherapy 2005;16(4):225-45.
2004: Petra Neddermann; Manuela Quintavalle; Chiara Di Pietro; Angelica Clementi; Mauro Cerretani; Sergio Altamura; Linda Bartholomew; Raffaele De Francesco
Reduction of hepatitis C virus NS5A hyperphosphorylation by selective inhibition of cellular kinases activates viral RNA replication in cell culture.
Journal of virology 2004;78(23):13306-14.
2004: Vincenzo Summa; Alessia Petrocchi; Victor G Matassa; Marina Taliani; Ralph Laufer; Raffaele De Francesco; Sergio Altamura; Paola Pace
HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.
Journal of medicinal chemistry 2004;47(22):5336-9.
2004: Paola Pace; Emanuela Nizi; Barbara Pacini; Silvia Pesci; Victor G Matassa; Raffaele De Francesco; Sergio Altamura; Vincenzo Summa
The monoethyl ester of meconic acid is an active site inhibitor of HCV NS5B RNA-dependent RNA polymerase.
Bioorganic & medicinal chemistry letters 2004;14(12):3257-61.
2004: Vincenzo Summa; Alessia Petrocchi; Paola Pace; Victor G Matassa; Raffaele De Francesco; Sergio Altamura; Licia tomei; Uwe Koch; Philippe Neuner
Discovery of alpha,gamma-diketo acids as potent selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase.
Journal of medicinal chemistry 2004;47(1):14-7.
2004: Licia tomei; Sergio Altamura; Linda Bartholomew; Monica Bisbocci; Carolyn Bailey; Michele Bosserman; Antonella Cellucci; Eleonora Forte; Ilario Incitti; Laura Orsatti; Uwe Koch; Raffaele De Francesco; David B Olsen; Steven S Carroll; Giovanni Migliaccio
Characterization of the inhibition of hepatitis C virus RNA replication by nonnucleosides.
Journal of virology 2004;78(2):938-46.
2003: Giovanni Migliaccio; Joanne E Tomassini; Steven S Carroll; Licia tomei; Sergio Altamura; Balkrishen Bhat; Linda Bartholomew; Michele Bosserman; Alessandra Ceccacci; Lawrence F Colwell; Riccardo Cortese; Raffaele De Francesco; Anne B Eldrup; Krista Getty; Xiaoli S Hou; Robert L LaFemina; Steven W Ludmerer; Malcolm MacCoss; Daniel R McMasters; Mark Stahlhut; David B Olsen; Daria J Hazuda; Osvaldo A Flores
Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro.
The Journal of biological chemistry 2003;278(49):49164-70.
2003: Licia tomei; Sergio Altamura; Linda Bartholomew; Antonino Biroccio; Alessandra Ceccacci; Laura Pacini; Frank Narjes; Nadia Gennari; Monica Bisbocci; Ilario Incitti; Laura Orsatti; Steven Harper; Ian Stansfield; Michael Rowley; Raffaele De Francesco; Giovanni Migliaccio
Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
Journal of virology 2003;77(24):13225-31.
2003: Raffaele De Francesco; Licia tomei; Sergio Altamura; Vincenzo Summa; Giovanni Migliaccio
Approaching a new era for hepatitis C virus therapy: inhibitors of the NS3-4A serine protease and the NS5B RNA-dependent RNA polymerase.
Antiviral research 2003;58(1):1-16.
2003: Caterina Trozzi; Linda Bartholomew; Alessandra Ceccacci; Gabriella Biasiol; Laura Pacini; Sergio Altamura; Frank Narjes; Ester Muraglia; Giacomo Paonessa; Uwe Koch; Raffaele De Francesco; Christian Steinkuhler; Giovanni Migliaccio
In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor.
Journal of virology 2003;77(6):3669-79.
2003: Stefania Colarusso; Uwe Koch; Benjamin Gerlach; Christian Steinkühler; Raffaele De Francesco; Sergio Altamura; Victor G Matassa; Frank Narjes
Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.
Journal of medicinal chemistry 2003;46(3):345-8.
2002: Christian Steinkühler; Gabriella Biasiol; Mauro Cerretani; Laura Di Renzo; Mirko Brunetti; Paolo Ingallinella; Raffaele De Francesco; Sergio Altamura
A scintillation proximity active site binding assay for the hepatitis C virus serine protease.
Analytical biochemistry 2002;307(1):99-104.
2002: Amedeo De Tomassi; Maura Pizzuti; Rita Graziani; ANDREA SBARDELLATI; Sergio Altamura; Giacomo Paonessa; Cinzia Traboni
Cell clones selected from the Huh7 human hepatoma cell line support efficient replication of a subgenomic GB virus B replicon.
Journal of virology 2002;76(15):7736-46.
2002: Paolo Ingallinella; Daniela Fattori; Sergio Altamura; Christian Steinkühler; Uwe Koch; Daniel O Cicero; Renzo Bazzo; Riccardo Cortese; Elisabetta Bianchi; Antonello Pessi
Prime site binding inhibitors of a serine protease: NS3/4A of hepatitis C virus.
Biochemistry 2002;41(17):5483-92.
2002: Frank Narjes; Koehler F Konrad; Uwe Koch; Benjamin Gerlach; Stefania Colarusso; Christian Steinkühler; Mirko Brunetti; Sergio Altamura; Raffaele De Francesco; Victor G Matassa
A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCV NS3 protease.
Bioorganic & medicinal chemistry letters 2002;12(4):701-4.
2000: Paolo Ingallinella; Elisabetta Bianchi; Raffaele Ingenito; Uwe Koch; Christian Steinkühler; Sergio Altamura; Antonello Pessi
Optimization of the P'-region of peptide inhibitors of hepatitis C virus NS3/4A protease.
Biochemistry 2000;39(42):12898-906.
2000: Licia tomei; R L Vitale; Ilario Incitti; Sergio Serafini; Sergio Altamura; alessandra vitelli; Raffaele De Francesco
Biochemical characterization of a hepatitis C virus RNA-dependent RNA polymerase mutant lacking the C-terminal hydrophobic sequence.
The Journal of general virology 2000;81(Pt 3):759-67.
1999: Mauro Cerretani; L Di Renzo; Sergio Serafini; alessandra vitelli; Nadia Gennari; Elisabetta Bianchi; Antonello Pessi; A Urbani; Stefano Colloca; Raffaele De Francesco; Christian Steinkühler; Sergio Altamura
A high-throughput radiometric assay for hepatitis C virus NS3 protease.
Analytical biochemistry 1999;266(2):192-7.
1998: Giovanna Liuzzo; Antonino Buffon; Luigi M Biasucci; JR Gallimore; giuseppina caligiuri; alessandra vitelli; Sergio Altamura; Gennaro Ciliberto; Antonio G Rebuzzi; Filippo Crea; M B Pepys; Attilio Maseri
Enhanced inflammatory response to coronary angioplasty in patients with severe unstable angina.
Circulation 1998;98(22):2370-6.
1998: Paolo Ingallinella; Sergio Altamura; Elisabetta Bianchi; Marina Taliani; Raffaele Ingenito; Riccardo Cortese; Raffaele De Francesco; Christian Steinkühler; Antonello Pessi
Potent peptide inhibitors of human hepatitis C virus NS3 protease are obtained by optimizing the cleavage products.
Biochemistry 1998;37(25):8906-14.
1997: Nazzareno Dimasi; F Martin; Cinzia Volpari; Mirko Brunetti; Gabriella Biasiol; Sergio Altamura; Riccardo Cortese; Raffaele De Francesco; Christian Steinkühler; maurizio sollazzo
Characterization of engineered hepatitis C virus NS3 protease inhibitors affinity selected from human pancreatic secretory trypsin inhibitor and minibody repertoires.
Journal of virology 1997;71(10):7461-9.
1997: F Martin; Cinzia Volpari; C Steinkuhler; Nazzareno Dimasi; Mirko Brunetti; Gabriella Biasiol; Sergio Altamura; Riccardo Cortese; Raffaele De Francesco; maurizio sollazzo
Affinity selection of a camelized V(H) domain antibody inhibitor of hepatitis C virus NS3 protease.
Protein engineering 1997;10(5):607-14.
1996: Luigi M Biasucci; alessandra vitelli; Giovanna Liuzzo; Sergio Altamura; giuseppina caligiuri; C Monaco; Antonio G Rebuzzi; Gennaro Ciliberto; Attilio Maseri
Elevated levels of interleukin-6 in unstable angina.
Circulation 1996;94(5):874-7.
1996: Giuseppe Campiani; Vito Nacci; Isabella Fiorini; M P De Filippis; Antonio Garofalo; Giovanni Greco; Ettore Novellino; Sergio Altamura; L Di Renzo
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.
Journal of medicinal chemistry 1996;39(14):2672-80.
1996: Raffaele De Francesco; Sven-Erik Behrens; Licia tomei; Sergio Altamura; J Jiricny
RNA-dependent RNA polymerase of hepatitis C virus.
Methods in enzymology 1996;275():58-67.
1995: A Cabibbo; E Sporeno; Carlo Toniatti; Sergio Altamura; Rocco Savino; Giacomo Paonessa; Gennaro Ciliberto
Monovalent phage display of human interleukin (hIL)-6: selection of superbinder variants from a complex molecular repertoire in the hIL-6 D-helix.
Gene 1995;167(1-2):41-7.
1995: Armin Lahm; Rocco Savino; A L Salvati; A Cabibbo; Laura Ciapponi; A Demartis; Carlo Toniatti; Giacomo Paonessa; Sergio Altamura; Gennaro Ciliberto
The molecular design of human IL-6 receptor antagonists.
Annals of the New York Academy of Sciences 1995;762():136-50; discussion 150-1.
1994: Rocco Savino; Laura Ciapponi; Armin Lahm; A Demartis; A Cabibbo; Carlo Toniatti; P Delmastro; Sergio Altamura; Gennaro Ciliberto
Rational design of a receptor super-antagonist of human interleukin-6.
The EMBO journal 1994;13(24):5863-70.
1994: Rocco Savino; Armin Lahm; A L Salvati; Laura Ciapponi; E Sporeno; Sergio Altamura; Giacomo Paonessa; Carlo Toniatti; Gennaro Ciliberto
Generation of interleukin-6 receptor antagonists by molecular-modeling guided mutagenesis of residues important for gp130 activation.
The EMBO journal 1994;13(6):1357-67.
1994: A Wallace; Sergio Altamura; Carlo Toniatti; alessandra vitelli; Elisabetta Bianchi; P Delmastro; Gennaro Ciliberto; Antonello Pessi
A Multimeric Synthetic Peptide Combinatorial Library.
Peptide research 1994;7(1):27-31.