E. Monteagudo

发表

4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.

M. Rowley, V. Summa, A. Petrocchi, 2006, Journal of medicinal chemistry.

Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.

D. Hazuda, S. Harper, M. Rowley, 2007, Journal of medicinal chemistry.

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.

D. Hazuda, M. Rowley, V. Summa, 2008, Journal of medicinal chemistry.

Enhanced mass resolution method development, validation and assay application to support preclinical studies of a new drug candidate.

Vincenzo Pucci, R. Laufer, F. Bonelli, 2006, Rapid communications in mass spectrometry : RCM.

Application of an in Vitro Blood-Brain Barrier Model in the Selection of Experimental Drug Candidates for the Treatment of Huntington's Disease.

C. Dominguez, Laura Orsatti, V. Summa, 2019, Molecular pharmaceutics.

DPP‐IV‐resistant, long‐acting oxyntomodulin derivatives

A. Pocai, F. Bonelli, A. Pessi, 2011, Journal of peptide science : an official publication of the European Peptide Society.

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.

C. Toniatti, S. Altamura, M. Rowley, 2009, Journal of medicinal chemistry.

Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.

M. Rowley, Philip Jones, C. Steinkühler, 2009, Journal of medicinal chemistry.

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.

R. De Francesco, S. Altamura, M. Rowley, 2008, Journal of medicinal chemistry.

MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants

Adam T. Gates, D. Hazuda, M. Rudd, 2012, Antimicrobial Agents and Chemotherapy.

Quantitative Prediction of Human Clearance Guiding the Development of Raltegravir (MK-0518, Isentress) and Related HIV Integrase Inhibitors

M. Rowley, V. Summa, R. Laufer, 2009, Drug Metabolism and Disposition.

Preclinical pharmacokinetics and metabolism of a potent non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase

S. Harper, F. Narjes, M. Rowley, 2005, Xenobiotica; the fate of foreign compounds in biological systems.

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

E. Perlas, A. Guidi, E. Monteagudo, 2016, PLoS neglected tropical diseases.

ApoA-I mimetic peptides promote pre-β HDL formation in vivo causing remodeling of HDL and triglyceride accumulation at higher dose.

F. Bonelli, B. Hubbard, A. Pessi, 2010, Bioorganic & medicinal chemistry.

The metabolism and disposition of a potent inhibitor of hepatitis C virus NS3/4A protease

X. Chu, R. Evers, S. Harper, 2010, Xenobiotica; the fate of foreign compounds in biological systems.

Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.

M. Rudd, P. Coleman, S. Harper, 2012, ACS medicinal chemistry letters.

5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.

E. Réal, S. Harper, M. Botta, 2020, ACS medicinal chemistry letters.

A single-run liquid chromatography mass spectrometry method to quantify neuroactive kynurenine pathway metabolites in rat plasma.

C. Dominguez, Laura Orsatti, F. Bonelli, 2015, Journal of pharmaceutical and biomedical analysis.

Synthesis and Biological Evaluation of RGD–Cryptophycin Conjugates for Targeted Drug Delivery

V. Summa, Giulio Auciello, P. Gallinari, 2019, Pharmaceutics.

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.

M. Rowley, C. Giuliano, Philip Jones, 2011, Bioorganic & medicinal chemistry letters.

[11C]CHDI-626, a PET Tracer Candidate for Imaging Mutant Huntingtin Aggregates with Reduced Binding to AD Pathological Proteins.

J. Wityak, C. Halldin, K. Varnäs, 2021, Journal of medicinal chemistry.

Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.

S. Harper, S. Altamura, N. Gennari, 2016, ACS medicinal chemistry letters.

Identification and in vitro Characterization of a New Series of Potent and Highly Selective G9a Inhibitors as Novel Anti-Fibroadipogenic Agents.

V. Summa, G. Peruzzi, E. Monteagudo, 2022, Bioorganic & medicinal chemistry letters.

Doxorubicin disaccharide analogue: apoptosis-related improvement of efficacy in vivo.

F. Zunino, G. Capranico, R. Supino, 1997, Journal of the National Cancer Institute.

New conformationally homogeneous β‐turn antagonists of the human B2 kinin receptor

R. Terracciano, C. I. Fincham, E. Monteagudo, 2001, Journal of peptide science : an official publication of the European Peptide Society.

HILIC LC-MS for the determination of 2'-C-methyl-cytidine-triphosphate in rat liver.

C. Giuliano, F. Bonelli, K. Koeplinger, 2009, Journal of separation science.

Oligomerization, albumin binding and catabolism of therapeutic peptides in the subcutaneous compartment: An investigation on lipidated GLP-1 analogs.

Laura Orsatti, F. Bonelli, E. Monteagudo, 2022, Journal of pharmaceutical and biomedical analysis.

Synthesis and antiviral properties of novel 7-heterocyclic substituted 7-deaza-adenine nucleoside inhibitors of Hepatitis C NS5B polymerase.

M. Rowley, V. Summa, S. Avolio, 2012, Bioorganic & medicinal chemistry.

Determination of acetyl coenzyme A in human whole blood by ultra-performance liquid chromatography-mass spectrometry.

D. Elbaum, Laura Orsatti, F. Bonelli, 2018, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.

Structure-activity relationships and spectroscopic insights into a series of retro-inverso Tachykinin NK-1 receptor antagonists

R. Terracciano, A. Sisto, M. Venanzi, 2002 .

Discovery and Antiviral Profile of New Sulfamoylbenzamide Derivatives as HBV Capsid Assembly Modulators.

A. Prandi, R. De Francesco, V. Summa, 2022, Bioorganic & Medicinal Chemistry Letters.

Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement.

U. Koch, M. Rowley, V. Summa, 2009, Journal of medicinal chemistry.

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.

Michael Rowley, Cristina Gardelli, Marco Ferrara, 2007, Journal of medicinal chemistry.

Novel anthracycline oligosaccharides: influence of chemical modifications of the carbohydrate moiety on biological activity.

M. Binaschi, C. Maggi, C. Goso, 2002, Bioorganic & medicinal chemistry.

Synthesis, Biological Evaluation, and Molecular Modeling Studies of Rebeccamycin Analogues Modified in the Carbohydrate Moiety

M. Binaschi, M. Berettoni, A. Cipollone, 2008, ChemMedChem.

NMR-Spectroscopic, computational and mass-spectrometric investigations on the cis/trans analogues of 2,3,4-trihydronaphthalene-1-one

C. Maggi, M. Berettoni, A. Cipollone, 2003 .

A novel strategy for reducing phospholipids-based matrix effect in LC-ESI-MS bioanalysis by means of HybridSPE.

Vincenzo Pucci, Serena Di Palma, F. Bonelli, 2009, Journal of pharmaceutical and biomedical analysis.

A novel method using nuclear magnetic resonance for plasma protein binding assessment in drug discovery programs

V. Summa, M. Orsale, E. Monteagudo, 2019, Journal of pharmaceutical and biomedical analysis.

Turbulent flow chromatography TFC-tandem mass spectrometry supporting in vitro/vivo studies of NCEs in high throughput fashion.

F. Bonelli, A. Di Marco, E. Monteagudo, 2010, Journal of pharmaceutical and biomedical analysis.

Configurational requirements of the sugar moiety for the pharmacological activity of anthracycline disaccharides.

F. Zunino, G. Capranico, R. Supino, 1999, Biochemical pharmacology.

2′-C-Methyluridine phosphoramidite: a new building block for the preparation of RNA analogues carrying the 2′-hydroxyl group

E. Monteagudo, A. Iribarren, D. Cicero, 2001 .

Stereospecific synthesis of 1-alkylimidazole derivatives via mitsunobu reactions

M. Botta, V. Summa, F. Corelli, 1994 .

Establishment of an in Vitro Human Blood-Brain Barrier Model Derived from Induced Pluripotent Stem Cells and Comparison to a Porcine Cell-Based System

C. Dominguez, Giulio Auciello, A. Di Marco, 2020, Cells.

High sensitivity determination of valproic acid in mouse plasma using semi-automated sample preparation and liquid chromatography with tandem mass spectrometric detection.

F. Bonelli, E. Monteagudo, V. Pucci, 2005, Rapid communications in mass spectrometry : RCM.

Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.

S. Harper, V. Summa, P. Pace, 2018, ACS medicinal chemistry letters.

Kynurenine pathway activation and deviation to anthranilic and kynurenic acid in fibrosing chronic graft-versus-host disease

T. Luft, P. Dreger, C. Müller-Tidow, 2021, Cell reports. Medicine.

Fatty acid acylated peptide therapeutics: discovery of omega-n oxidation of the lipid chain as a novel metabolic pathway in preclinical species.

N. Gennari, Laura Orsatti, E. Bianchi, 2023, Journal of pharmaceutical and biomedical analysis.

Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.

Laura Orsatti, Alessia Santoprete, E. Bianchi, 2021, Journal of medicinal chemistry.

PEGylation of Neuromedin U yields a promising candidate for the treatment of obesity and diabetes.

A. Peier, A. Pocai, R. Laufer, 2012, Bioorganic & medicinal chemistry.

Personalized Metabolic Profile by Synergic Use of NMR and HRMS

F. Montorsi, A. Salonia, Laura Orsatti, 2021, Molecules.

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

A. Peier, A. Pocai, R. Laufer, 2014, Journal of peptide science : an official publication of the European Peptide Society.

High-Throughput Microsomal Stability Assay for Screening New Chemical Entities in Drug Discovery

M. Orsale, E. Monteagudo, M. Fonsi, 2008, Journal of biomolecular screening.

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.

J. I. Hernando, S. Altamura, M. Rowley, 2011, Bioorganic & medicinal chemistry letters.

Use of 'dilute-and-shoot' liquid chromatography-high resolution mass spectrometry in preclinical research: application to a DMPK study of perhexiline in mouse plasma.

Laura Orsatti, F. Bonelli, E. Monteagudo, 2016, Journal of pharmaceutical and biomedical analysis.

An efficient liquid chromatography-high resolution mass spectrometry approach for the optimization of the metabolic stability of therapeutic peptides

Laura Orsatti, F. Bonelli, E. Bianchi, 2017, Analytical and Bioanalytical Chemistry.

Conformational dynamics and DNA recognition by human MutSβ

S. Steinbacher, T. Vogt, C. Dominguez, 2023, bioRxiv.

Synthesis and biological evaluation of novel NK‐1 tachykinin receptor antagonists: The use of cycloalkyl amino acids as a template

A. Sisto, C. Maggi, C. Goso, 1995, Biopolymers.

Fosmetpantotenate (RE-024), a phosphopantothenate replacement therapy for pantothenate kinase-associated neurodegeneration: Mechanism of action and efficacy in nonclinical models

S. Harper, D. Elbaum, M. Beconi, 2018, PloS one.

Cyclic Phosphopantothenic Acid Prodrugs for Treatment of Pantothenate Kinase-Associated Neurodegeneration.

S. Harper, D. Elbaum, Giulio Auciello, 2020, Journal of medicinal chemistry.

Turnover rate of coenzyme A in mouse brain and liver

D. Elbaum, Laura Orsatti, F. Bonelli, 2021, PloS one.

MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants

Qian Huang, Adam T. Gates, D. Hazuda, 2014, Antimicrobial Agents and Chemotherapy.

Imaging Mutant Huntingtin Aggregates: Development of a Potential PET ligand.

J. Wityak, C. Halldin, L. Mrzljak, 2020, Journal of medicinal chemistry.

A liquid chromatography high‐resolution mass spectrometry in vitro assay to assess metabolism at the injection site of subcutaneously administered therapeutic peptides

Laura Orsatti, E. Bianchi, E. Monteagudo, 2018, Journal of pharmaceutical and biomedical analysis.

M. Rowley, R. Laufer, E. Monteagudo, 2009, Xenobiotica; the fate of foreign compounds in biological systems.

Synthesis and Biological

A. Sisto, C. Maggi, C. Goso, 2003 .

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Fabrizio Fiore, Michael Rowley, Cristina Gardelli, 2008, Journal of medicinal chemistry.

The conformations of discodermolide in DMSO.

J. Snyder, B. Cornett, E. Monteagudo, 2001, Journal of the American Chemical Society.

N-formimidoyl analogues of distamycin

M. Dentini, G. Giannini, E. Monteagudo, 1996 .

Characterization of a new potent and long-lasting single chain peptide agonist of RXFP1 in cells and in vivo translational models

E. Bianchi, E. Monteagudo, J. Le Bail, 2022, Scientific Reports.

Enhancement of intestinal absorption of 2-methyl cytidine prodrugs

F. Narjes, M. Rowley, R. Laufer, 2010, Drug delivery.

Design and Evaluation of [18F]CHDI-650 as a Positron Emission Tomography Ligand to Image Mutant Huntingtin Aggregates.

C. Halldin, C. Dominguez, Laura Orsatti, 2022, Journal of medicinal chemistry.

Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.

S. Harper, S. Altamura, N. Gennari, 2016, ACS medicinal chemistry letters.

High-Throughput Microsomal Stability Assay for Screening New Chemical Entities in Drug Discovery

M. Orsale, E. Monteagudo, M. Fonsi, 2008, Journal of biomolecular screening.