A5065124376- Peptidase Inhibition and Analysis
- Radiopharmaceutical Chemistry and Applications
- Galectins and Cancer Biology
- Medical Imaging Techniques and Applications
- Neuropeptides and Animal Physiology
- Glycosylation and Glycoproteins Research
- Cell Adhesion Molecules Research
- Prostate Cancer Treatment and Research
- Monoclonal and Polyclonal Antibodies Research
- Signaling Pathways in Disease
- Neuroendocrine Tumor Research Advances
- Advanced Biosensing Techniques and Applications
- HER2/EGFR in Cancer Research
- Cytokine Signaling Pathways and Interactions
- Inflammatory mediators and NSAID effects
- Cancer, Hypoxia, and Metabolism
- Peroxisome Proliferator-Activated Receptors
- Regulation of Appetite and Obesity
- Trace Elements in Health
- Radiomics and Machine Learning in Medical Imaging
- Alzheimer's disease research and treatments
- Acute Myeloid Leukemia Research
- Lung Cancer Research Studies
- Angiogenesis and VEGF in Cancer
- Cancer, Lipids, and Metabolism
University of Debrecen
2020-2024
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...
Background/Aim: Since the use of anaesthetics has drawback altering radiotracer distribution, preclinical positron emission tomography (PET) imaging findings anaesthetised animals must be carefully handled. This study aimed at assessing cerebral [<sup>18</sup>F]F-FDG uptake pattern in healthy Wistar rats under four different anaesthesia protocols using microPET/magnetic resonance (MRI) examinations. Materials and Methods: Post-injection 15±1.2 MBq [<sup>18</sup>F]F-FDG, either while awake or...
Since acute myeloid leukemias still represent the most aggressive type of adult leukemias, profound understanding disease pathology is paramount importance for diagnostic and therapeutic purposes. Hence, this study aimed to explore real-time fate with establishment an experimental myelomonoblastic leukemia (My1/De) rat model using preclinical positron emission tomography (PET) whole-body autoradiography.
The aminopeptidase N (APN/CD13) receptor plays an important role in the neoangiogenic process and metastatic tumor cell invasion. Clinical preclinical studies reported that bestatin actinonin are cytotoxic to APN/CD13-positive tumors metastases due their APN/CD13-specific inhibitor properties. Our previous have already shown 68Ga-labeled NGR peptides bind specifically APN/CD13 expressing cells. specificity of 68Ga-NGR radiopharmaceuticals enables following efficacy antiangiogenic therapy...
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,...
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...
Cyclodextrin derivates (CyDs) can form complexes with cyclooxygenase-2 induced tumor promoting prostaglandin E2 (PGE2). Based on our previous observations, 68Ga-labelled CyDs may represent promising radiopharmaceuticals in the positron emission tomography (PET) diagnostics of PGE2 positive tumors. We aimed at evaluating tumor-targeting potential 68Ga-NODAGA conjugated randomly methylated beta-cyclodextrin (68Ga-NODAGA-RAMEB) and 2-hydroxypropyl-β-cyclodextrin (68Ga-NODAGA-HPβCD) using vivo...
Formation and growth of metastases require a new vascular network. Angiogenesis plays an essential role in the expansion progression most malignancies. A high number molecular pathways regulate angiogenesis, including endothelial factor (VEGF), αvβ3 integrin, matrix metalloproteinases (MMPs), or aminopeptidase N. The aim this study is to involve new, easily accessible peptide sequences into neo-angiogenesis malignant processes. Labelling these ligands with 68Ga enable PET imaging neo-vascularization.
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...
Changes in the expression of neo-angiogenic molecules primary tumor and its metastases may significantly affect efficacy therapies. The aim this study was to evaluate alterations aminopeptidase N (APN/CD13) αvβ3 integrin receptor serially transplanted mesoblastic nephroma (Ne/De) using 68Gallium (68Ga)-labeled NOTA-cNGR NODAGA-RGD radiotracers preclinical positron emission tomography (PET) imaging.Primary metastatic tumors were induced by subrenal capsule assay (SRCA) Fischer-344 rats. In...
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...
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...
Since NGR-tripeptides (asparagine-glycine-arginine) selectively target neoangiogenesis-associated Aminopeptidase N (APN/CD13) on cancer cells, we aimed to evaluate the in vivo tumour targeting capability of radiolabelled, NGR-containing, ANP/CD13-selective [213Bi]Bi-DOTAGA-cKNGRE CD13pos. HT1080 fibrosarcoma-bearing severe combined immunodeficient CB17 mice. 10 ± 1 days after cell inoculation, positron emission tomography (PET) was performed applying [68Ga]Ga-DOTAGA-cKNGRE for verification....
Given that galectin-3 (Gal-3) is a β-galactoside-binding lectin promoting tumor growth and metastatis, it could be valuable target for the treatment of Gal-3-expressing neoplasms. An aromatic group introduced to C-3′ position lactosamine increased its affinity Gal-3. Herein, we aimed at developing radiopharmaceutical detection Gal-3 positive malignancies. To enhance specificity, heterodimeric radiotracer capable binding both αvβ3 integrin was also synthetized. Arginine-glycine-asparagine...
Aluminum (Al) excess and hypercholesterinaemia are established risks of Alzheimer's disease (AD). The aim this study was to establish an AD-resembling hypercholesterinaemic animal model-with the involvement 8 week 48 week-old Fischer-344 rats-by Al administration for safe rapid verification β-amyloid-targeted positron emission tomography (PET) radiopharmaceuticals. Measurement lipid parameters β-amyloid-affine [11C]C-Pittsburgh Compound B ([11C]C-PIB) PET examinations were performed....
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...
Given the rising prevalence of lipid metabolic disorders and malignant diseases, we aimed to establish an in vivo hypercholesterinaemic tumour-bearing rat model for induction assessment these conditions. A normal standard CRLT/N, 2 (baseline),- or 4 (2 + 2, pretreated)-week-long butter cholesterol rich (BCR) diet was applied mesoblastic nephroma (Ne/De) myelomonoblastic leukaemia (My1/De) healthy control Long—Evans Fischer 344 rats. The beginning chow administration started parallel with...