A5076251817- Radiopharmaceutical Chemistry and Applications
- Peptidase Inhibition and Analysis
- Neuroendocrine Tumor Research Advances
- Lung Cancer Research Studies
- Neuropeptides and Animal Physiology
- Medical Imaging Techniques and Applications
- Shoulder Injury and Treatment
- Trauma Management and Diagnosis
- Cell Adhesion Molecules Research
- Monoclonal and Polyclonal Antibodies Research
- Thyroid Cancer Diagnosis and Treatment
- Shoulder and Clavicle Injuries
- Knee injuries and reconstruction techniques
- Glycosylation and Glycoproteins Research
- Neuroblastoma Research and Treatments
- Chemical Synthesis and Analysis
- Total Knee Arthroplasty Outcomes
- Pelvic and Acetabular Injuries
- Orthopedic Surgery and Rehabilitation
- Nanoplatforms for cancer theranostics
- Cancer, Hypoxia, and Metabolism
- Elbow and Forearm Trauma Treatment
- Nanoparticle-Based Drug Delivery
- Congenital limb and hand anomalies
- Drug Transport and Resistance Mechanisms
Universität Innsbruck
1993-2025
Innsbruck Medical University
2014-2025
Multidisciplinary Digital Publishing Institute (Switzerland)
2019
University of Tübingen
2019
Peter MacCallum Cancer Centre
2019
University Hospital Bonn
2002-2013
Krankenhaus Nordwest
2007
University of Bonn
2006
University Clinic of Traumatology
1994-1997
Kaiser Permanente San Diego Medical Center
1993
Over the last years Gallium-68 (68Ga) has received tremendous attention for labeling of radiopharmaceuticals positron emission tomography (PET). 68Ga biomolecules is currently based on bifunctional chelators containing aminocarboxylates (mainly DOTA and NOTA). We have recently shown that cyclic peptide siderophores very good complexing properties resulting in high specific activities excellent metabolic stabilities, particular triacetylfusarinine-C (TAFC). postulated, that, starting from its...
Molecular imaging and targeted radiotherapy with radiolabeled cholecystokinin-2 receptor (CCK2R) targeting peptide probes holds high promise to improve the clinical management of patients metastatic medullary thyroid carcinoma other CCK2R-expressing malignancies. Low stability suboptimal currently available analogs has prompted us seek new stabilization strategies. In this study, we present a minigastrin analog site-specific C-terminal modifications showing highly optimized profile....
Radiolabeling of nanoparticles (NPs) has been performed for a variety reasons, such as studying pharmacokinetics, imaging, or therapy. Here, we describe the in vitro and vivo evaluation DTPA-derivatized lipid-based NP (DTPA-NP) radiolabeled with different radiometals, including 111In 99mTc, single-photon emission computed tomography (SPECT), 68Ga positron (PET), 177Lu therapeutic applications. PEGylated DTPA-NP varying DTPA amounts, composition, size were 111In, 177Lu, 68Ga, using various...
This study was designed to determine safety, tolerability, and radiation burden of a [68Ga]NODAGA-RGD-PET for imaging integrin αvβ3 expression in patients with hepatocellular carcinoma (HCC) liver cirrhosis. Moreover, metabolic stability biokinetic data were compiled. After injection 154–184 MBq [68Ga]NODAGA-RGD three consecutive PET/CT scans acquired starting 8.3 ± 2.1, 36.9 2.8, 75.1 3.4 min after tracer injection. For metabolite analysis, blood urine samples analyzed by HPLC. dosimetry...
Abstract Background Determination of the functional liver mass is important in a variety clinical settings including surgery and transplantation. [ 99m Tc]Tc-diethylenetriamine-pentaacetic acid galactosyl human serum albumin ( Tc-GSA) radiotracer targeting asialoglycoprotein receptor (ASGR) routinely used Japan for this purpose. Here we describe development evaluation 68 Ga]Ga-NODAGA-TriGalactan low molecular weight PET-tracer structure. Results For synthesis TRIS as branching unit NODAGA...
Several exploratory studies have demonstrated the feasibility of cholecystokinin-2 receptor (CCK2R) targeting in patients with medullary thyroid carcinoma (MTC) and other neuroendocrine tumors (NETs). We report results a prospective phase I/IIA pilot study (clinicaltrials.gov NCT06155994) conducted at our center <sup>68</sup>Ga-labeled peptide analog DOTA-DGlu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal-Phe-NH<sub>2</sub> (<sup>68</sup>Ga-DOTA-MGS5). <b>Methods:</b> Six advanced MTC 6...
A variety of radiolabelled minigastrin analogues targeting the cholecystokinin 2 (CCK2) receptor were developed and compared in a concerted preclinical testing to select most promising radiotracer for diagnosis treatment medullary thyroid carcinoma (MTC). DOTA–DGlu–DGlu–DGlu–DGlu–DGlu–DGlu–Ala–Tyr–Gly–Trp–Met–Asp–Phe–NH2 (CP04) after labelling with 111In displayed excellent characteristics, such as high stability, affinity, specific persistent tumour uptake low kidney retention animal...
Minigastrin (MG) analogs show high affinity to the cholecystokinin-2 receptor (CCK2R) and have therefore been intensively studied find a suitable analog for imaging treatment of CCK2R-expressing tumors. The clinical translation radioligands developed thus far has hampered by kidney uptake or low enzymatic stability. In this study, we aimed develop new MG with improved targeting properties stabilized against degradation through site-specific amino acid modifications. Method: Based on lead...
Aspergillus fumigatus produces the siderophore triacetylfusarinine C (TAFC) for iron acquisition which is essential its virulence. Therefore, TAFC a specific marker invasive aspergillosis. We have shown previously that positron emission tomography (PET) imaging with [68Ga]TAFC exhibited excellent targeting properties in an A. rat infection model. In this study, we aimed to prepare analogs modifying fusarinine (FSC) by acylation different carbon chain lengths as well charged substituents and...
Abstract Introduction Medullary thyroid cancer (MTC) is a rare malignant tumour of the parafollicular C-cells with an unpredictable clinical course and currently suboptimal diagnostic therapeutic options, in particular advanced disease. Overexpression cholecystokinin-2 receptors (CCK2R) represents promising avenue to imaging targeted therapy, ideally through theranostic approach. Materials methods A translational study (GRAN-T-MTC) conducted Phase I multicentre trial indium-111 labelled CP04...
Cholecystokinin-2 receptors (CCK2R) are overexpressed in a variety of malignant diseases and therefore have gained certain attention for peptide receptor radionuclide imaging. Among extensive approaches to improve pharmacokinetics metabolic stability minigastrin (MG) based radioligands, the concept multivalency enhanced tumour targeting has not been investigated extensively. We utilized fusarinine C (FSC) as chelating scaffold novel mono-, di-, trimeric bioconjugates CCK2R expression....
Non-invasive techniques allowing quantitative determination of the functional liver mass are great interest for patient management in a variety clinical settings. Recently, we presented [68Ga]DTPA-GSA to target hepatic asialoglycoprotein receptor this purpose. Here, introduce [68Ga]NOTA-GSA improve metabolic stability radiopharmaceutical and compare imaging properties with [68Ga]DTPA-GSA. Labeling compounds was carried out at room temperature using 1.9 M sodium acetate as buffer. For quality...
The high overexpression of cholecystokinin-2 receptors (CCK2R) in tumors, such as medullary thyroid carcinoma, allows for highly specific diagnostic and therapeutic targeting with radiolabeled peptide probes derived from natural ligands the receptor. Based on ideal imaging characteristics, availability low cost technetium-99m (99mTc)-labeled radiopharmaceuticals we have developed two hydrazinonicotinic acid (HYNIC) conjugated minigastrin analogs allowing labeling at activity. CCK2R...
Imaging of angiogenic processes is great interest in preclinical research as well clinical settings. The most commonly addressed target structure for imaging angiogenesis the integrin α(v)β(3). Here we describe synthesis and evaluation [(18)F]FProp-Cys(*)-Arg-Arg-Glu-Thr-Ala-Trp-Ala-Cys(*)-OH, a radiolabelled peptide designed to selectively α(5)β(1). Conjugation 4-nitrophenyl-(RS)-2-[(18)F]fluoropropionate provided [(18)F]FProp-Cys(*)-Arg-Arg-Glu-Thr-Ala-Trp-Ala-Cys(*)-OH high radiochemical...
The gastrointestinal stromal tumor (GIST) is a rare disease with limited therapeutic options when resistance to tyrosine kinase inhibitor (TKI) treatment occurs. authors investigated binding of various 68Ga-labeled peptides, targeting receptors reported be overexpressed in GIST, different cell lines. For this purpose, three GIST lines were tested: GIST-T1, GIST882 (Imatinib sensitive), and GIST430 resistant). DOTA-NT 8-13 (targeting NTR1), DOTA-TATE SSTR2), CP04 (a minigastrin derivative...