Search Results - "Battisti, Umberto"
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Synergistic Experimental and Computational Investigation of the Bioorthogonal Reactivity of Substituted Aryltetrazines
Published in Bioconjugate chemistry (20-04-2022)“…Tetrazines (Tz) have been applied as bioorthogonal agents for various biomedical applications, including pretargeted imaging approaches. In radioimmunoimaging,…”
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Comparison of Different Organometallics Towards Electrophilic Aromatic 211At-Astatinations of Highly Reactive Tetrazines
Published in Chemistry : a European journal (16-10-2024)“…Organometallics can be used as precursors for electrophilic 211At-statinations. In this report, we compared the potential of aryl trimethylsilanes, -germanes,…”
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Recent Advances in the Development of Tetrazine Ligation Tools for Pretargeted Nuclear Imaging
Published in Pharmaceuticals (Basel, Switzerland) (30-05-2022)“…Tetrazine ligation has gained interest as a bio-orthogonal chemistry tool within the last decade. In nuclear medicine, tetrazine ligation is currently being…”
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Development of the First Aliphatic 18 F-Labeled Tetrazine Suitable for Pretargeted PET Imaging-Expanding the Bioorthogonal Tool Box
Published in Journal of medicinal chemistry (28-10-2021)“…Pretargeted imaging of nanomedicines have attracted considerable interest because it has the potential to increase imaging contrast while reducing radiation…”
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Evaluation of F-537-Tetrazine in a model for brain pretargeting imaging. Comparison to N-(3-[18F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine
Published in Nuclear medicine and biology (01-01-2024)“…Brain pretargeted nuclear imaging for the diagnosis of various neurodegenerative diseases is a quickly developing field. The tetrazine ligation is currently…”
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Analytical and preparative enantioseparation and main chiroptical properties of Iridium(III) bis(4,6-difluorophenylpyridinato)picolinato
Published in Journal of Chromatography A (07-10-2016)“…•A convenient method is presented for the direct separation of enantiomers of fac-trans-N–N, bis[2-(4,6-difluorophenyl)pyridinato-C2,N](picolinato)iridium(III)…”
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Functional characterization of N-octyl 4-methylamphetamine variants and related bivalent compounds at the dopamine and serotonin transporters using Ca2+ channels as sensors
Published in Toxicology and applied pharmacology (15-05-2021)“…The early characterization of ligands at the dopamine and serotonin transporters, DAT and SERT, respectively, is important for drug discovery, forensic…”
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Lipophilicity and Click Reactivity Determine the Performance of Bioorthogonal Tetrazine Tools in Pretargeted In Vivo Chemistry
Published in ACS pharmacology & translational science (09-04-2021)“…The development of highly selective and fast biocompatible reactions for ligation and cleavage has paved the way for new diagnostic and therapeutic…”
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Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT1A receptor agonists
Published in European journal of medicinal chemistry (05-01-2017)“…Recently, 1-(1,4-dioxaspiro[4,5]dec-2-ylmethyl)-4-(2-methoxyphenyl)piperazine (1) was reported as a potent 5-HT1AR agonist with a moderate 5-HT1AR selectivity…”
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10
Serendipitous Identification of a Covalent Activator of Liver Pyruvate Kinase
Published in Chembiochem : a European journal of chemical biology (03-01-2023)“…Enzymes are effective biological catalysts that accelerate almost all metabolic reactions in living organisms. Synthetic modulators of enzymes are useful tools…”
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Exploration of Novel Urolithin C Derivatives as Non-Competitive Inhibitors of Liver Pyruvate Kinase
Published in Pharmaceuticals (Basel, Switzerland) (28-04-2023)“…The inhibition of liver pyruvate kinase could be beneficial to halt or reverse non-alcoholic fatty liver disease (NAFLD), a progressive accumulation of fat in…”
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12
Ellagic Acid and Its Metabolites as Potent and Selective Allosteric Inhibitors of Liver Pyruvate Kinase
Published in Nutrients (2023)“…Liver pyruvate kinase (PKL) has recently emerged as a new target for non-alcoholic fatty liver disease (NAFLD), and inhibitors of this enzyme could represent a…”
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Direct Cu-mediated aromatic 18 F-labeling of highly reactive tetrazines for pretargeted bioorthogonal PET imaging
Published in Chemical science (Cambridge) (15-09-2021)“…Pretargeted imaging can be used to visualize and quantify slow-accumulating targeting vectors with short-lived radionuclides such as fluorine-18 - the most…”
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Direct Cu-mediated aromatic 18F-labeling of highly reactive tetrazines for pretargeted bioorthogonal PET imaging
Published in Chemical science (Cambridge) (15-09-2021)“…Pretargeted imaging can be used to visualize and quantify slow-accumulating targeting vectors with short-lived radionuclides such as fluorine-18 – the most…”
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Synthesis and evaluation of fluorine-18 labelled tetrazines as pre-targeting imaging agents for PET
Published in EJNMMI radiopharmacy and chemistry (06-03-2024)“…Background The brain is a challenging target for antibody-based positron emission tomography (immunoPET) imaging due to the restricted access of antibody-based…”
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A Fluorescent Probe as a Lead Compound for a Selective α‑Synuclein PET Tracer: Development of a Library of 2‑Styrylbenzothiazoles and Biological Evaluation of [18F]PFSB and [18F]MFSB
Published in ACS omega (29-08-2023)“…A method to detect and quantify aggregated α-synuclein (αSYN) fibrils in vivo would drastically impact the current understanding of multiple neurodegenerative…”
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Development of an in vitro liquid chromatography–mass spectrometry method to evaluate stereo and chemical stability of new drug candidates employing immobilized artificial membrane column
Published in Journal of Chromatography A (10-10-2014)“…•A method to evaluate stability of chiral compounds in gastrointestinal simulated fluids is reported.•The use of an IAM column confirm the influence of a…”
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“Heart-cut” bidimensional achiral-chiral liquid chromatography applied to the evaluation of stereoselective metabolism, in vivo biological activity and brain response to chiral drug candidates targeting the central nervous system
Published in Journal of Chromatography A (22-04-2016)“…•A method to evaluate simultaneously in vivo biological activity and brain response to chiral drug candidates targeting the central nervous system is…”
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Alpha-Synuclein PET Tracer Development—An Overview about Current Efforts
Published in Pharmaceuticals (Basel, Switzerland) (26-08-2021)“…Neurodegenerative diseases such as Parkinson’s disease (PD) are manifested by inclusion bodies of alpha-synuclein (α-syn) also called α-synucleinopathies…”
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Optimization of Direct Aromatic 18F-Labeling of Tetrazines
Published in Molecules (Basel, Switzerland) (22-06-2022)“…Radiolabeling of tetrazines has gained increasing attention due to their important role in pretargeted imaging or therapy. The most commonly used radionuclide…”
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