A5080188809- Radiopharmaceutical Chemistry and Applications
- Carbohydrate Chemistry and Synthesis
- Glycosylation and Glycoproteins Research
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Peptidase Inhibition and Analysis
- Medical Imaging Techniques and Applications
- Proteoglycans and glycosaminoglycans research
- Galectins and Cancer Biology
- Radioactive element chemistry and processing
- Polyamine Metabolism and Applications
- Cancer, Hypoxia, and Metabolism
- Monoclonal and Polyclonal Antibodies Research
- Neuropeptides and Animal Physiology
- Pharmacological Receptor Mechanisms and Effects
- Lanthanide and Transition Metal Complexes
- Metal complexes synthesis and properties
- Medical Imaging and Pathology Studies
- Lung Cancer Treatments and Mutations
- Radiomics and Machine Learning in Medical Imaging
- Biopolymer Synthesis and Applications
- Chemical Synthesis and Characterization
- Lung Cancer Diagnosis and Treatment
- Neuroendocrine Tumor Research Advances
- Advanced Biosensing Techniques and Applications
University of Debrecen
2009-2023
Hungarian Academy of Sciences
2006-2013
National Institutes of Health
2006
Eunice Kennedy Shriver National Institute of Child Health and Human Development
2006
Abstract Unprecedented fast and efficient complexation of Sc III was demonstrated with the chelating agent AAZTA (AAZTA=1,4‐bis(carboxymethyl)‐6‐[bis(carboxymethyl)]amino‐6‐methylperhydro‐1,4‐diazepine) under mild experimental conditions. The robustness 44 Sc(AAZTA) − chelate conjugated biomolecules thereof is further shown by in vivo PET imaging healthy tumor mice models. new results pave way towards development Sc‐based radiopharmaceuticals using chelator.
A new pyclen-3,9-diacetate derivative ligand (H23,9-OPC2A) was synthesized possessing an etheric O-atom opposite to the pyridine ring, improve dissociation kinetics of its Mn(II) complex (pyclen = 3,6,9,15-tetraazabicyclo(9.3.1)pentadeca-1(15),11,13-triene). The is less basic than N-containing analogue (H23,9-PC2A) due non-protonable O-atom. In spite lower basicity, conditional stability [Mn(3,9-OPC2A)] (pMn -log(Mn(II)), cL cMn(II) 0.01 mM. pH 7.4) remains unaffected 8.69), compared...
Given the rising pervasiveness of melanocortin-1 receptor (MC1-R) positive melanoma malignum (MM) and pertinent metastases, radiolabelled receptor-affine alpha-melanocyte stimulating hormone-analogue (α-MSH analogue) imaging probes would be crucial importance in timely tumor diagnostic assessment. Herein we aimed at investigating biodistribution MM targeting potential newly synthesized 213Bi-conjugated MC1-R specific peptide-based radioligands with establishment overexpressing preclinical...
We have discovered five bismuth(III)-containing polyoxopalladates (POPs) which were fully characterized by solution and solid-state physicochemical techniques: the cube-shaped [BiPd12O32(AsPh)8]5– (BiPd12AsL), [BiPd12O32(AsC6H4N3)8]5– (BiPd12AsLN), [BiPd12O32(AsC6H4COO)8]13– (BiPd12AsLC) as well star-shaped [BiPd15O40(PO)10H6]11– (BiPd15P) [BiPd15O40(PPh)10]7– (BiPd15PL), respectively. The organically modified capping groups phenylarsonate, p-azidophenylarsonate, p-carboxyphenylarsonate...
Abstract Unprecedented fast and efficient complexation of Sc III was demonstrated with the chelating agent AAZTA (AAZTA=1,4‐bis(carboxymethyl)‐6‐[bis(carboxymethyl)]amino‐6‐methylperhydro‐1,4‐diazepine) under mild experimental conditions. The robustness 44 Sc(AAZTA) − chelate conjugated biomolecules thereof is further shown by in vivo PET imaging healthy tumor mice models. new results pave way towards development Sc‐based radiopharmaceuticals using chelator.
Non-macrocyclic H 4 OCTAPA derivatives form highly stable complexes with Bi( iii ), but require an appropriate rigid spacer to enhance the inertness of complex, as demonstrated by radiolabeling studies 205/206 Bi-nuclides.
Although radiolabeled alpha-melanocyte stimulating hormone-analogue NAPamide derivatives are valuable melanoma-specific diagnostic probes, their rapid elimination kinetics and high renal uptake may preclude them from being used in clinical settings. We aimed at improving the pharmacokinetics of DOTA-NAPamide compounds by incorporating a 4-(p-iodo-phenyl)-butanoic acid (IPB) into molecules. Followed 68Ga-, 205/206Bi-, 177Lu-labelling, radiopharmaceuticals ([68Ga]Ga-DOTA-IPB-NAPamide,...
The analysis and polyclonal antibody response for newly synthesized maltose-BSA conjugate neoglycoproteins is described. In this first proof of concept study, a simple carbohydrate antigen, maltose, was linked to BSA by reductive amination. An aglycone spacer utilized conserve the intact annular maltose structure promote accessibility immunogen hapten during immunization. were investigated CGE number conjugated residues determined MALDI-TOF MS. then evaluated immunization BALB/c mice tested...
Radiolabeled peptides possessing an Arg-Gly-Asp (RGD) motif are widely used radiopharmaceuticals for PET imaging of tumor angiogenesis due to their high affinity and selectivity αvβ3 integrin. This receptor is overexpressed in endothelial cells the case numerous cancer cell lines, therefore, it excellent biomarker diagnosis. The galectin-3 protein also highly expressed N-acetyllactosamine a well-established ligand this receptor. We have developed synthetic method prepare...
Introduction . Hypoxia-induced α ν β 3 integrin and aminopeptidase N (APN/CD13) receptor expression play an important role in tumor neoangiogenesis. APN/CD13-specific 68 Ga-NOTA-c(NGR), integrin-specific Ga-NODAGA-[c(RGD)] 2 , hypoxia-specific Ga-DOTA-nitroimidazole enable the vivo detection of neoangiogenic process hypoxic regions mass using positron emission tomography (PET) imaging. The aim this study was to evaluate whether Ga-NOTA-c(NGR) allow noninvasive temporal changes APN/CD13...
Tumor hypoxia induces angiogenesis, which is required for tumor cell survival. The aminopeptidase N receptor (APN/CD13) an excellent marker of angiogenesis since it overexpressed in angiogenic blood vessels and cells. Asparagine-glycine-arginine (NGR) peptide analogs bind selectively to the APN/CD13 recepto, therefore, they are important vector molecules development a PET radiotracer capable detecting APN-rich tumors. To investigate effect glycosylation pegylation on in-vivo efficacy...
Hypoxia promotes angiogenesis, which is crucial for tumor growth, and induces malignant progression increases the therapeutic resistance. Positron emission tomography (PET) enables detection of hypoxic regions in tumors using 2-nitroimidazole-based radiopharmaceuticals. We describe here a physicochemical study Sc(DO3AM-NI) complex, indicates: (a) relatively slow formation chelate acidic solution; (b) lower thermodynamic stability than reference Sc(DOTA); (c) however, it substantially more...
We have established a method for nucleophilic one-pot, two-step radiosynthesis of the popular opioid receptor radioligand 6-O-(2-[18F]fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) from novel precursor 6-O-(2-tosyloxyethyl)-6-O-desmethyl- 3-O-trityl-diprenorphine (TE-TDDPN), which we designate as Henriksen precursor. undertook an optimization synthesis conditions, aiming to enhance accessibility [18F]FE-DPN positron emission tomography (PET) studies μ-opioid receptors. Herein, report...
Melanocortin-1 receptor (MC1-R) targeting alpha-melanocyte stimulating hormone-analogue (α-MSH) biomolecules labelled with α-emitting radiometal seem to be valuable in the targeted radionuclide therapy of MC1-R positive melanoma malignum (MM). Herein is reported anti-tumor vivo therapeutic evaluation MC1-R-affine [213Bi]Bi-DOTA-NAPamide and HOLDamide treatment B16-F10 tumor-bearing C57BL/6J mice. On 6th, 8th 10th days post tumor cell inoculation; treated groups mice were intravenously...
Cyclotron-produced radiometals must be separated from the irradiated target and purified other metal impurities, which could interfere with radiolabeling process. We compared different chromatographic colorimetric methods to determine amount of transition metals in radioactive samples. Besides commercially available tests, 4-(2-pyridylazo)resorcinol xylenol orange were used as a non-selective reagents, forming water-soluble chelates most immediately. applicability pre- post-column...
Gastrin-releasing peptide receptors (GRPR) are overexpressed in prostate cancer (PCa). Since bombesin analogue aminobenzoic-acid (AMBA) binds to GRPR with high affinity, scandium-44 conjugated AMBA is a promising radiotracer the PET diagnostics of positive tumors. Herein, specificity newly synthetized [44Sc]Sc-NODAGA-AMBA was investigated vitro and vivo applying PCa PC-3 xenograft. After in-vitro assessment receptor binding, tumor-bearing mice were injected [44Sc]Sc/[68Ga]Ga-NODAGA-AMBA (in...