A5066557086- Radiopharmaceutical Chemistry and Applications
- Medical Imaging and Pathology Studies
- Medical Imaging Techniques and Applications
- Monoclonal and Polyclonal Antibodies Research
- Peptidase Inhibition and Analysis
- Neuroendocrine Tumor Research Advances
- Chemical Reactions and Isotopes
- X-ray Diffraction in Crystallography
- Lung Cancer Research Studies
- Crystallization and Solubility Studies
- Amino Acid Enzymes and Metabolism
- Cancer, Hypoxia, and Metabolism
- Cell Adhesion Molecules Research
- HER2/EGFR in Cancer Research
- Drug Transport and Resistance Mechanisms
- Chemical Synthesis and Analysis
- Lung Cancer Treatments and Mutations
- Cancer Research and Treatments
- Orthopaedic implants and arthroplasty
- Epigenetics and DNA Methylation
- Cancer Immunotherapy and Biomarkers
- Bone health and treatments
- Computational Drug Discovery Methods
- Metal complexes synthesis and properties
- Cholinesterase and Neurodegenerative Diseases
Chiba University
2016-2025
Gunma University
2005-2020
Kumamoto University
1996-2019
Kyoto University
1996-2010
Health Sciences University of Hokkaido
2009-2010
Suzuka University of Medical Science
2010
Osaka Ohtani University
2009
Nihon Medi-Physics (Japan)
2008
Burapha University
2008
Hamamatsu University School of Medicine
2004-2007
At is a promising radiohalogen for targeted α therapy. However, some astatinated compounds undergo deastatination in vivo, leading to unintended astatine accumulation nontarget tissues. Recently, group reported that the vivo stability of an astato on alkyl could be improved by placing specific substituents around group. We hypothesized such approach applied improve aromatic groups. designed and synthesized astatobenzene derivatives with neighboring different physical properties. In vitro...
Previous studies on indium-111 (111In) labeling of polypeptides and peptides using cyclic diethylenetriaminepentaacetic dianhydride (cDTPA) as a bifunctional chelating agent (BCA) have indicated that DTPA might be useful BCA for 111In at high specific activities when can incorporated without inducing intra- or intermolecular cross-linking. To investigate this hypothesis, monoreactive derivative with maleimide group the peptide binding site (MDTPA) was designed synthesized. A monoclonal...
Lectins (proteins that bind specific sugar molecules on glycoproteins and glycolipids) are expressed at various levels the surface of tumor cells. Conjugation cytotoxic agents to recognized by lectins could be useful in treatment tumors. Avidin (a highly glycosylated, positively charged protein found egg white) contains terminal N-acetylglucosamine mannose residues some lectins. In this study, we tested ability avidin, labeled through conjugation radioactive biotin B vitamin), target...
In vivo imaging of β-amyloid (Aβ) peptide aggregates in the brain may lead to early detection Alzheimer's disease (AD) and monitoring progression effectiveness AD treatment. The purpose this study was develop novel amyloid agents based on flavone as a core structure. Radioiodinated derivatives were designed synthesized. binding affinities for Aβ varied from 13 77 nM. When vitro plaque labeling carried out using post-mortem sections, all flavones intensely stained not only plaques but also...
Purpose: This study was undertaken to evaluate the renal radioactivity levels of a newly designed 67Ga-labeled antibody fragment with linkage cleaved by enzymes present on brush border membrane (BBM) lining lumen tubule.Experimental Design:67Ga-labeled S-2-(4-isothiocyanatobenzyl)-1,4,7-triazacyclononane-1,4,7-triacetic acid (SCN-Bn-NOTA) conjugated an Fab through Met-Val-Lys (67Ga-NOTA-MVK-Fab) considering that Met-Val sequence is substrate BBM and 67Ga-NOTA-Met excreted from kidney into...
Metallic radionuclides provide target-specific radiolabeled probes for molecular imaging in radiochemical yields sufficient administration to subjects without purification. However, unlabeled ligands the injectate can compete targeted molecules with probes, which eventually necessitates postlabeling Herein we describe a "1 3" design circumvent issue by taking advantage of inherent coordination properties technetium-99m (99mTc). A monovalent RGD ligand possessing an isonitrile as coordinating...
The high in vivo stability of 2,2-dihydroxymethyl-3-[18F]fluoropropyl-2-nitroimidazole ([18F]DiFA) prompted us to evaluate neopentyl as a scaffold prepare radiotheranostic system with radioiodine and astatine. Three DiFA analogues one, two, or without hydroxyl group were synthesized. While all 125I-labeled compounds remained stable against nucleophilic substitution, only glycol was cytochrome P450 (CYP)-mediated metabolism showed deiodination. 211At-labeled also both substitution...
The interposition of a cleavable linkage by enzymes on the renal brush border membrane constitutes promising approach for reducing radioactivity levels radiolabeled low-molecular-weight antibody fragments and constructs (LMW Abs). Herein, we applied molecular design to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-based reagents radiotheranostic applications with trivalent radiometals. DOTA or derivative thereof was conjugated Fab through an FGK...
Rhenium-186-1-hydroxyethylidene-1,1-diphosphonate (186Re-HEDP) has been used for the palliation of metastatic bone pain. Delayed blood clearance and high gastric uptake radioactivity have observed upon injection, due to instability 186Re-HEDP in vivo. In this study, on basis concept bifunctional radiopharmaceuticals, we designed a stable 186Re-mercaptoacetylglycylglycylglycine (MAG3) complex-conjugated bisphosphonate,...
The aim of the present study is to synthesize new mannosylated dextran derivative that can be labeled with Tc-99m for potential use in sentinel lymph node detection (SLND). compound was designed have a molecular weight 10 kDa as backbone, mannose binding receptors and S-derivatized cysteine suitable chelator labeling [(99m)Tc(H(2)O)(3)(CO)(3)](+) precursor. Reaction allyl bromide (MW 11800) yielded intermediate allyl-dextran (1) about 40% coupling. Addition resulted cysteine, DC15 (2). final...
Recently, antiprogrammed cell death protein 1 (aPD-1) and death-ligand (aPD-L1) monoclonal antibodies (mAbs) have been approved. Even though aPD-1 aPD-L1 mAbs target the same PD-1/PD-L1 axis, it is still unclear whether both exert equivalent pharmacological activity in patients who are sensitive to blockade therapy, as there no direct comparison of their pharmacokinetics (PK) antitumor effects. Therefore, we evaluated differences between PK therapeutic effects blockade-sensitive mouse...
Although the identification of inflammatory infiltrates in endomyocardial biopsy specimens is necessary for definite diagnosis myocarditis, test invasive and not sensitive. Therefore, a new diagnostic technique early noninvasive evaluation myocarditis has been awaited. Expression tenascin-C (TNC), one oligometric extracellular glycoproteins, induced various pathological states, including inflammation, suggesting that TNC can be molecular marker myocarditis.An 111In anti-TNC monoclonal...
The obstructive renal radioactivity after injection of antibody fragments/constructs labeled with metallic radionuclides would be improved by liberating a radiometal chelate urinary excretion from the molecules enzymes on brush border membrane (BBM). A tripeptide GFK sequence was newly evaluated as an enzyme-cleavable linkage and conjugated to 99mTc isonicotinic acid derivative 2-picolylglycine (99mTc-IPG). 99mTc-IPG-glycine liberated 99mTc-IPG-GFK enzymes, while 99mTc-IPG-GK (where...
The persistent localization of radioactivity in the kidney after administration 111In-DTPA-d-Phe1-octreotide impairs diagnostic accuracy this radiopharmaceutical. To better understand mechanisms responsible for renal levels 111In-DTPA-d-Phe1-octreotide, metabolism compound was compared with 111In-DTPA-l-Phe1-octreotide, where N-terminal d-phenylalanine replaced l-phenylalanine to facilitate metabolism. DTPA-d-Phe1-octreotide and DTPA-l-Phe1-octreotide were synthesized by solid-phase methods....