Search results for "bifunctional"
showing 10 items of 123 documents
89 Zr-Immuno-Positron Emission Tomography in Oncology: State-of-the-Art 89 Zr Radiochemistry
2017
Contains fulltext : 181624.pdf (Publisher’s version ) (Open Access) Immuno-positron emission tomography (immunoPET) with (89)Zr-labeled antibodies has shown great potential in cancer imaging. It can provide important information about the pharmacokinetics and tumor-targeting properties of monoclonal antibodies and may help in anticipating on toxicity. Furthermore, it allows accurate dose planning for individualized radioimmunotherapy and may aid in patient selection and early-response monitoring for targeted therapies. The most commonly used chelator for (89)Zr is desferrioxamine (DFO). Preclinical studies have shown that DFO is not an ideal chelator because the (89)Zr-DFO complex is partly…
The analysis of modified peroxisome proliferator responsive elements of the peroxisomal bifunctional enzyme in transfected HepG2 cells reveals two re…
1995
AbstractPeroxisome proliferators (PPs) are non-genotoxic carcinogens in rodents. They can induce the expression of numerous genes via the heterodimerization of two members of the steroid hormone receptor superfamily, called the peroxisome proliferator-activated receptor (PPAR) and the 9-cis retinoic acid receptor (RXR). Many of the PP responsive genes possess a peroxisome proliferator response element (PPRE) formed by two TGACCT-related motifs. The bifunctional enzyme (HD) PPRE contains 3 such motifs, creating DR1 and DR2 sequences. PPAR and RXR regulate transcription via the DR1 element while DR2 modulates the expression of the gene via auxiliary factors in HepG2 cells.
Isomerization and Application of Aroylnorbornenecarboxylic Acids for Stereoselective Preparation of Heterocycles
2002
When boiled in acidic or basic solution, diendo-3-aroylbicyclo[2.2.1]heptane-2-carboxylic acids (1 and la) isomerize to exo-3-aroylbicyclo[2.2.1]heptane-endo-2-carboxylic acids (2 and 2a). Similar endo→exo and even exo → endo isomerization of the aroyl group occurred when the Diels-Alder product containing a mixture of 3-exo-p-toluoylbicyclo[2.2.1 ]hept-5-ene-2-endo-carboxylic acid (4) and 3-endo-p-toluoylbicyclo[2.2.1]hept-5-ene-2-exo-carboxylic acid (5) was reacted with bifunctional reagents: o-aminothiophenol, 3-amino-1-propanol, 1,4-diaminobutane or diexo-3-hydroxymethylbicyclo[2.2.1]heptane-2-amine. All the reactions yielded mixtures of norbornene diendo- and diexo-fused heterocycles (…
New potential bimodal imaging contrast agents based on DOTA-like and porphyrin macrocycles
2011
A bifunctional chelator featuring (DO3A-AM)-Porphyrin units has been prepared. The high-field relaxivity of the Gd complex is similar to those of currently available contrast agents clearly showing that the first coordination sphere remains identical to the parent molecule [Gd(DO3A-AM)(H2O)], with one coordinated water molecule.
NODAPA-OH and NODAPA-(NCS)n: Synthesis, 68Ga-radiolabelling and in vitro characterisation of novel versatile bifunctional chelators for molecular ima…
2008
This report concerns synthesis, (68)Ga-radiolabelling and stability data of 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-isothio-cyanatophenyl-acetic acid (NODAPA-NCS), 1,4,7-triazacyclononane-1-acetic acid-4,7-di-p-isothiocyanatophenyl-acetic acid (NODAPA-(NCS)(2)) and 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-hydroxyphenyl-acetic acid (NODAPA-OH), versatile bifunctional chelators with potential for molecular imaging. Protein binding and exemplified conjugation are also reported.
Polymerizable ring-shaped molecules containing aspartic acid: synthesis and free radical polymerization of a macrocycle derived from (N'-methacryloyl…
1999
A novel polymerizable macrocycle, 6, was prepared using high dilution techniques. Starting from N-(N'-methacryloyl-11-aminoundecanoyl)-L-aspartic acid dimethyl ester (2), N-(N'methacryloyl-11-aminoundecanoyl)-α,β-bis( 4,9-dioxadodecane-1,12-diamine)-L-aspartic acid amide (4) was obtained via amino-lysis with the bifunctional amine 4,9-dioxadodecane-1,12-diamine (3) in high excess. Addition of the free amino groups to toluene-2,4-diisocyanate (5) under high dilution provided macrocycle 6. The existence and purity of 6 were confirmed by mass spectrometry, NMR and IR spectroscopy, and HPLC. The methacrylic function was used to build up oligomers by free radical polymerization, using AIBN as an…
Elastomeric Organosilicon Micronetworks
1997
Trifunctional methyltrimethoxysilane and bifunctional dimethyldimethoxysilane monomers were cocondensed in water in the presence of surfactant. Strictly spherical micronetworks of narrow size distribution were obtained for particle sizes 10 nm < R < 30 nm. By special “endcapping” reactions all reactive SiOH groups were removed quantitatively, and the resulting micronetworks become soluble in common organic solvents like toluene, THF, or chloroform. For contents of trifunctional monomer larger than 50 mol % the particles do not swell irrespective of the choice of the solvent, whereas for lower mole fractions of trimethoxysilane an increasing swelling ratio is observed. Below 2.5 mol % trifun…
A hybrid catalyst for decontamination of organic pollutants based on a bifunctional dicopper(II) complex anchored over niobium oxyhydroxide
2017
Abstract This article describes the preparation and characterization of a hybrid oxidation catalyst for decontamination of organic pollutants which involves a bifunctional dicopper(II) complex and the niobium(V) oxyhydroxide as the active species, the later one being also a solid support. The pH range for the existence of the active species was determined by potentiometric and UV–vis spectroscopy at 25 °C and 0.15 M NaCl in a H 2 O/EtOH (70:30 v/v) solvent mixture containing copper(II) and the ligand N , N -2,2′-ethylenediphenylenebis(oxamic acid) (H 4 L). As far as the hybrid material is concerned, FTIR, FT-Raman, TEM and SEM images, surface area and TG/DTA analyses showed the occurrence o…
Peroxisomal and mitochondrial status of two murine oligodendrocytic cell lines (158N, 158JP): potential models for the study of peroxisomal disorders…
2009
International audience; In some neurodegenerative disorders (leukodystrophies) characterized by myelin alterations, the defect of peroxisomal functions on myelin-producing cells (oligodendrocytes) are poorly understood. The development of in vitro models is fundamental to understanding the physiopathogenesis of these diseases. We characterized two immortalized murine oligodendrocyte cell lines: a normal (158N) and a jimpy (158JP) cell line mutated for the proteolipid protein PLP/DM20. Fluorescence microscopy, flow cytometry, and western blotting analysis allow to identify major myelin proteins (PLP colocalizing with mitochondria; myelin basic protein), oligodendrocyte (CNPase and myelin oli…
Equilibrium, Kinetic and Structural Properties of Gallium(III) and Some Divalent Metal Complexes Formed with the New DATAm and DATA5m Ligands
2017
The development of 68Ge/68Ga generators has made the positron-emitting 68Ga isotope widely accessible and raised interest in new chelate complexes of Ga3+. The hexadentate 1,4-di(acetate)-6-methyl[amino(methyl)acetate]perhydro-1,4-diazepane (DATAm) ligand and its bifunctional analogue, 1,4-di(acetate)-6-pentanoic acid[amino(methyl)acetate]perhydro-1,4-diazepane (DATA5m), rapidly form complexes with 68Ga in high radiochemical yield. The stability constants of DATAm and DATA5m complexes formed with Ga3+, Zn2+, Cu2+, Mn2+ and Ca2+ have been determined by using pH potentiometry, spectrophotometry (Cu2+) and 1H and 71Ga NMR spectroscopy (Ga3+). The stability constants of Ga(DATAm) and Ga(DATA5m)…