A5058272199- Peptidase Inhibition and Analysis
- Receptor Mechanisms and Signaling
- Radiopharmaceutical Chemistry and Applications
- Medical Imaging Techniques and Applications
- Fluorine in Organic Chemistry
- Neuropeptides and Animal Physiology
- Click Chemistry and Applications
- Glycosylation and Glycoproteins Research
- Monoclonal and Polyclonal Antibodies Research
- Cancer, Hypoxia, and Metabolism
- Neurotransmitter Receptor Influence on Behavior
- Neuroscience and Neuropharmacology Research
- Chemical Synthesis and Analysis
- Neuroendocrine Tumor Research Advances
- Thyroid Cancer Diagnosis and Treatment
- Cell Adhesion Molecules Research
- Protease and Inhibitor Mechanisms
- Carbohydrate Chemistry and Synthesis
- Lanthanide and Transition Metal Complexes
- Amino Acid Enzymes and Metabolism
- Sleep and Wakefulness Research
- Ferrocene Chemistry and Applications
- Immune cells in cancer
- Pharmacological Receptor Mechanisms and Effects
- Cancer-related Molecular Pathways
Friedrich-Alexander-Universität Erlangen-Nürnberg
2015-2024
Universitätsklinikum Erlangen
2012-2024
Ege University
2023
Klinik und Poliklinik für Nuklearmedizin
2006
Innsbruck Medical University
2006
Klinikum rechts der Isar
2006
Objectives To date, there is no valuable tool to assess fibrotic disease activity in humans vivo a non-invasive way. This study aims uncouple inflammatory from fibroinflammatory diseases such as IgG 4 -related disease. Methods In this cross-sectional clinical study, 27 patients with inflammatory, and overlapping manifestations of underwent positron emission tomography (PET) scanning tracers specific for fibroblast activation protein (FAP; 68 Ga-FAP inhibitor (FAPI)-04), 18...
Fibroblast activation protein (FAP) has emerged as an interesting molecular target used in the imaging and therapy of various types cancers. <sup>68</sup>Ga-labeled chelator-linked FAP inhibitors (FAPIs) have been successfully applied to PET tumor types. To broaden spectrum applicable tracers for extended studies FAP-dependent diseases, we herein report radiosynthesis preclinical evaluation <sup>18</sup>F-labeled glycosylated FAPI ([<sup>18</sup>F]FGlc-FAPI). <b>Methods:</b> An...
Click for PET: An efficient strategy based on click chemistry has been developed 18F-labeling alkyne-bearing peptides with concomitant glycosylation. The mild conditions and general applicability of this reliable reaction gives access to a new class 18F-glycopeptide radiopharmaceuticals improved biological properties in vivo imaging studies by positron emission tomography (PET). Detailed facts importance specialist readers are published as "Supporting Information". Such documents...
Abstract Integrin α ν β 3 is overexpressed on endothelial cells of growing vessels as well several tumor types, and so integrin‐binding radiolabeled cyclic RGD pentapeptides have attracted increasing interest for in vivo imaging integrin expression by positron emission tomography (PET). Of the cRGD derivatives available applications, systems comprising multiple moieties recently been shown to exhibit highly favorable properties relation monomers. To assess synthetic limits...
Glycosylation frequently improves the biokinetics and clearance properties of macromolecules in vivo could therefore be used for design radiopharmaceuticals positron emission tomography (PET). Recently, we have developed a click chemistry method (18)F-fluoroglycosylation alkyne-bearing RGD-peptides targeting integrin receptor. To investigate whether this strategy yield an (18)F-labeled RGD glycopeptide with favorable biokinetics, generated series new glycopeptides, varying 6-fluoroglycosyl...
Abstract Antipsychotic drugs are effective interventions in schizophrenia. However, the efficacy of these agents often decreases over time, which leads to treatment failure and symptom recurrence. We report that antipsychotic rat models declines concert with extracellular striatal dopamine levels rather than insufficient D2 receptor occupancy. was associated a suppression transporter activity, reversed during failure. coincided reduced neuron firing, not observed efficacy. Synaptic field...
Advanced colorectal carcinoma (CRC) is characterized by a high frequency of primary immune evasion and refractoriness to immunotherapy. Given the importance interferon (IFN)-γ in CRC immunosurveillance, we investigated whether how acquired IFN-γ resistance tumor cells would promote growth, sensitivity could be restored.Spontaneous colitis-associated development was induced mice with specific pathway inhibition intestinal epithelial cells. The influence gene status expression on survival...
3,4,5-Tri-O-acetyl-2-[18F]fluoro-2-deoxy-d-glucopyranosyl 1-phenylthiosulfonate (Ac3-[18F]FGlc-PTS) was developed as a thiol-reactive labeling reagent for the site-specific 18F-glycosylation of peptides. Taking advantage highly accessible 1,3,4,6-tetra-O-acetyl-2-deoxy-2-[18F]fluoroglucopyranose, three-step radiochemical pathway investigated and optimized, providing Ac3-[18F]FGlc-PTS in yield about 33% 90 min (decay-corrected based on starting [18F]fluoride). reacted with model pentapeptide...
Aiming to image NTS1 overexpressing tumors, the diarylpyrazole glycoconjugate 8, derived from potent antagonist SR142948A, was synthesized taking advantage of palladium-catalyzed aminocarbonylation reaction. The 8 displayed excellent affinity and selectivity toward NTS1. Radiosynthesis proceeded straightforwardly, obtaining [(18)F]8 with stability highly beneficial biodistribution in vivo as demonstrated by PET imaging HT29 tumor-bearing nude mice. Thus, tracer represents a promising...
Imaging of Y1R expression in breast cancer is still a challenging task. Herein, we report suitable (18)F-labeled high-molecular-weight glycopeptide for imaging peripheral neuropeptide Y (NPY) Y1 receptor (Y1R)-positive tumors by preclinical small-animal positron emission tomography (PET). The Y1R-preferring NPY [F(7),P(34)]NPY analogue was functionalized with an alkyne-bearing propargylglycine (Pra) position 4. corresponding fluoroglycosylated (FGlc) peptide [Pra(4)(FGlc),F(7),P(34)]NPY and...
The neurotensin (NT) receptor-1 (NTS1) is overexpressed in a variety of carcinomas and therefore an interesting target for imaging with positron emission tomography (PET). aim this study was the development new NT derivatives based on metabolically stable peptide sequence NLys-Lys-Pro-Tyr-Tle-Leu suitable PET imaging. peptides were synthesized by solid-phase supported synthesis elongated respective chelators (NODA-GA, DOTA) (68)Ga-labeling or propargylglycine (18)F-labeling via...
N-Alkylaminoferrocene (NAAF)-based prodrugs are activated in the presence of elevated amounts reactive oxygen species (ROS), which corresponds to cancer specific conditions, with formation NAAF and p-quinone methide. Both products act synergistically by increasing oxidative stress cells that causes their death. Though it has already been demonstrated best this type retain antitumor activity vivo, effects were found be substantially weaker than those observed cell cultures. Moreover,...
Abstract Introduction of [ 18 F]fluoride ion into the aromatic core phenylazocarboxylic esters was achieved in only 30 seconds, with radiochemical yields up to 95 % (85(±10) %). For labeling purposes, resulting F‐substituted azoester can be further converted radical‐arylation reactions give biaryls, or substitutions at its carbonyl unit produce azocarboxamides.
The prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein that highly expressed in the malignant human prostate epithelium. Therefore, PSMA has emerged as very attractive target for developing radiopharmaceuticals diagnosis, e.g., by positron emission tomography (PET) imaging, and radiotherapy of cancer. aim this study was to develop 18F-labeled ligands bearing different 18F-glycosyl moieties effect on vivo clearance behavior radiotracers addition their tumor...
Molecular imaging using positron emission tomography (PET) can serve as a promising tool for visualizing biological targets in the brain. Insights into expression pattern and vivo of G protein-coupled orexin receptors OX1R OX2R will further our understanding system its role various physiological pathophysiological processes. Guided by crystal structures lead compound JH112 approved hypnotic drug suvorexant bound to OX2R, respectively, we herein describe design synthesis two novel...
Molecular imaging using positron emission tomography (PET) can serve as a promising tool for visualizing biological targets in the brain. Insights into expression pattern and vivo of G protein-coupled orexin receptors OX1R OX2R will further our understanding system its role various physiological pathophysiological processes. Guided by crystal structures lead compound JH112 approved hypnotic drug suvorexant bound to OX2R, respectively, we herein describe design synthesis two novel...