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Author Details

Antonio Macchiarulo
Department of Pharmaceutical Sciences, University of Perugia
1986
168
34
PMIDPaper TitleJournal TitlePublished Year
36733497The signaling function of IDO1 incites the malignant progression of mouse B16 melanoma.Oncoimmunology2023
37638806The hope and hype of ellagic acid and urolithins as ligands of SARS-CoV-2 Nsp5 and inhibitors of viral replication.J Enzyme Inhib Med Chem2023
37387273A back-door insight into the modulation of Src kinase activity by the polyamine spermidine.Elife2023
37047038Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir.Int J Mol Sci2023
36982608Turning a Tumor Microenvironment Pitfall into Opportunity: Discovery of Benzamidoxime as PD-L1 Ligand with pH-Dependent Potency.Int J Mol Sci2023
37276329Combining Solid-State NMR with Structural and Biophysical Techniques to Design Challenging Protein-Drug Conjugates.Angew Chem Int Ed Engl2023
37438993Estimating the hydrophobicity extent of molecular fragments using reversed-phase liquid chromatography.J Sep Sci2023
37296100A multicentric consortium study demonstrates that dimethylarginine dimethylaminohydrolase 2 is not a dimethylarginine dimethylaminohydrolase.Nat Commun2023
34145969Indoleamine 2,3-dioxygenase 1 (IDO1): an up-to-date overview of an eclectic immunoregulatory enzyme.FEBS J2022
35409342Critical Assessment of a Structure-Based Screening Campaign for IDO1 Inhibitors: Tips and Pitfalls.Int J Mol Sci2022
35456549Biological Evaluation of New Thienopyridinium and Thienopyrimidinium Derivatives as Human Choline Kinase Inhibitors.Pharmaceutics2022
36431824Environmentally Sustainable Achiral and Chiral Chromatographic Analysis of Amino Acids in Food Supplements.Molecules2022
36043064PROTACs bearing piperazine-containing linkers: what effect on their protonation state?RSC Adv2022
35889194The Combination of Molnupiravir with Nirmatrelvir or GC376 Has a Synergic Role in the Inhibition of SARS-CoV-2 Replication In Vitro.Microorganisms2022
36049273Development of 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.Eur J Med Chem2022
33085193The Stone Guest: How Does pH Affect Binding Properties of PD-1/PD-L1 Inhibitors?ChemMedChem2021
33741339Taxifolin and gastro-adhesive microparticles containing taxifolin promotes gastric healing in vivo, inhibits Helicobacter pylori in vitro and proton pump reversibly in silico.Chem Biol Interact2021
33667636Calmodulin binds to the STAS domain of SLC26A5 prestin with a calcium-dependent, one-lobe, binding mode.J Struct Biol2021
342902433-hydroxy-L-kynurenamine is an immunomodulatory biogenic amine.Nat Commun2021
34137184One Key and Multiple Locks: Substrate Binding in Structures of Tryptophan Dioxygenases and Hydroxylases.ChemMedChem2021
32190988New Insights from Crystallographic Data: Diversity of Structural Motifs and Molecular Recognition Properties between Groups of IDO1 Structures.ChemMedChem2020
31727470Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs).Eur J Med Chem2020
32024760Positive allosteric modulation of indoleamine 2,3-dioxygenase 1 restrains neuroinflammation.Proc Natl Acad Sci U S A2020
32024219Enantioselective HPLC Analysis to Assist the Chemical Exploration of Chiral Imidazolines.Molecules2020
32045233Discovery of Novel 5-Lipoxygenase-Activating Protein (FLAP) Inhibitors by Exploiting a Multistep Virtual Screening Protocol.J Chem Inf Model2020
31891875Optimized one-pot derivatization and enantioseparation of cysteine: Application to the study of a dietary supplement.J Pharm Biomed Anal2020
33159421Class IA PI3Ks regulate subcellular and functional dynamics of IDO1.EMBO Rep2020
33007550Fragment based drug design and diversity-oriented synthesis of carboxylic acid isosteres.Bioorg Med Chem2020
32977218Synthesis, biological evaluation, in silico modeling and crystallization of novel small monocationic molecules with potent antiproliferative activity by dual mechanism.Eur J Med Chem2020
32605792A novel mutation of indoleamine 2,3-dioxygenase 1 causes a rapid proteasomal degradation and compromises protein function.J Autoimmun2020
30677523D-leucine microparticles as an excipient to improve the aerosolization performances of dry powders for inhalation.Eur J Pharm Sci2019
31724832Tracking Hidden Binding Pockets Along the Molecular Recognition Path of l-Trp to Indoleamine 2,3-Dioxygenase 1.ChemMedChem2019
31389262Preclinical discovery and development of fingolimod for the treatment of multiple sclerosis.Expert Opin Drug Discov2019
27758684Elucidation of the Chromatographic Enantiomer Elution Order Through Computational Studies.Mini Rev Med Chem2018
30043647Lead optimization-hit expansion of new asymmetrical pyridinium/quinolinium compounds as choline kinase α1 inhibitors.Future Med Chem2018
30996817Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists.ACS Med Chem Lett2018
30391205Identification of a 2-propanol analogue modulating the non-enzymatic function of indoleamine 2,3-dioxygenase 1.Biochem Pharmacol2018
29486616Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4.Expert Opin Drug Discov2018
29275233Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.Eur J Med Chem2018
29266750Binding Mode and Structure-Activity Relationships of ITE as an Aryl Hydrocarbon Receptor (AhR) Agonist.ChemMedChem2018
29160617Exploring the enantiorecognition mechanism of Cinchona alkaloid-based zwitterionic chiral stationary phases and the basic trans-paroxetine enantiomers.J Sep Sci2018
27994058Signal Transducer and Activator of Transcription 1 Plays a Pivotal Role in RET/PTC3 Oncogene-induced Expression of Indoleamine 2,3-Dioxygenase 1.J Biol Chem2017
30108849Advances in indoleamine 2,3-dioxygenase 1 medicinal chemistry.Medchemcomm2017
28214225A Relay Pathway between Arginine and Tryptophan Metabolism Confers Immunosuppressive Properties on Dendritic Cells.Immunity2017
29107427Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors.Eur J Med Chem2017
29031064Fragment-based approach to identify IDO1 inhibitor building blocks.Eur J Med Chem2017
28771037Immunotherapy⿦ a pursuit race to tomorrow's medicines.Future Med Chem2017
28771024Binding properties of different categories of IDO1 inhibitors: a microscale thermophoresis study.Future Med Chem2017
27696702Distinct roles of immunoreceptor tyrosine-based motifs in immunosuppressive indoleamine 2,3-dioxygenase 1.J Cell Mol Med2017
27604095Laboratory-Scale Preparative Enantioseparations of Pharmaceutically Relevant Compounds on Commercially Available Chiral Stationary Phases for HPLC.Curr Med Chem2017
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Collaborators

Department of Pharmaceutical Sciences, University of Perugia
Co-authored papers 27
University of Perugia
Co-authored papers 17
University of Perugia
Co-authored papers 15
University of Perugia
Co-authored papers 11
University of Perugia
Co-authored papers 10
Department of Pharmaceutical Sciences, University of Perugia
Co-authored papers 8
Department of Pharmaceutical and Organic Chemistry, University of Granada
Co-authored papers 7
Weill Cornell School of Medicine
Co-authored papers 4
Istituto Zooprofilattico Sperimentale dell'Umbria e delle Marche "Togo Rosati"
Co-authored papers 2
Co-authored papers 2
University of Perugia
Co-authored papers 2
Englander Institute for Precision Medicine
Co-authored papers 1
Institute of Pharmaceutical Sciences, ETH Zurich
Co-authored papers 1
Weill Cornell Medical College
Co-authored papers 1
Istituto Zooprofilattico Sperimentale dell'Umbria e delle Marche "Togo Rosati"
Co-authored papers 1
Wihuri Research Institute
Co-authored papers 1
University of Colorado Anschutz Medical Campus
Co-authored papers 1
National Institute of Arthritis
Co-authored papers 1
Albert Einstein College of Medicine
Co-authored papers 1
Herbert Irving Comprehensive Cancer Center, Columbia University
Co-authored papers 1
Icahn School of Medicine at Mount Sinai
Co-authored papers 1
Institute of Pharmaceutical Sciences, ETH Zurich
Co-authored papers 1
Weill Cornell Medical College
Co-authored papers 1
Institute of Pharmaceutical Sciences, ETH Zurich
Co-authored papers 1
Expert Systems Inc.
Co-authored papers 1
Weill Cornell Medical College
Co-authored papers 1
Co-authored papers 1
Co-authored papers 1
Novartis Pharma AG
Co-authored papers 1
New York Medical College
Co-authored papers 1