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Aurlie Maisonial-Besset Tiffany Witkowski Mercedes Quintana Sophie Besse Vincent Gaumet Axel Cordonnier Cyrille Alliot Aurlien Vidal Caroline Denevault-Sabourin Sbastien Tarrit Sophie Levesque Elisabeth Miot-Noirault Jean-Michel Chezal 《Molecules (Basel, Switzerland)》2023,28(1)
The development of 64Cu-based immuno-PET radiotracers requires the use of copper-specific bifunctional chelators (BFCs) that contain functional groups allowing both convenient bioconjugation and stable copper complexes to limit in vivo bioreduction, transmetallation and/or transchelation. The excellent in vivo kinetic inertness of the pentaazamacrocyclic [64Cu]Cu-15-5 complex prompted us to investigate its potential for the 64Cu-labelling of monoclonal antibodies (mAbs), compared with the well-known NODAGA and DOTA chelators. To this end, three NODAGA, DOTA and 15-5-derived BFCs, containing a pendant azadibenzocyclooctyne moiety, were synthesised and a robust methodology was determined to form covalent bonds between them and azide-functionalised trastuzumab, an anti-HER2 mAb, using strain-promoted azide-alkyne cycloaddition. Unlike the DOTA derivative, the NODAGA- and 15-5-mAb conjugates were radiolabelled with 64Cu, obtaining excellent radiochemical yields, under mild conditions. Although all the radioimmunoconjugates showed excellent stability in PBS or mouse serum, [64Cu]Cu-15-5- and [64Cu]Cu-NODAGA-trastuzumab presented higher resistance to transchelation when challenged by EDTA. Finally, the immunoreactive fraction of the radioimmunoconjugates (88–94%) was determined in HER-2 positive BT474 human breast cancer cells, confirming that the bioconjugation and radiolabelling processes implemented had no significant impact on antigen recognition. 相似文献
54.
Aneta M. Tomkiel Krzysztof Brzezinski Zenon Łotowski Leszek Siergiejczyk Piotr Wałejko Stanisław Witkowski Jan Kowalski Jolanta Płoszyńska Andrzej Sobkowiak Jacek W. Morzycki 《Tetrahedron》2013
A new protocol for the electrochemical synthesis of glycoconjugates is presented. Thioether derivatives of cholesterol and other sterols were subjected to anodic oxidation in the presence of a sugar alcohol affording glycoconjugates with the sugar linked to a steroid moiety by an ether bond. The isomeric 6β-3α,5α-cyclo-steroidal thioethers proved to be better sterol donors than the normal 3β-Δ5-steroidal thioethers. 相似文献
55.
Magdalena Jabłońska Lucjan Chmielarz Agnieszka Węgrzyn Katarzyna Guzik Zofia Piwowarska Stefan Witkowski Richard I. Walton Peter W. Dunne František Kovanda 《Journal of Thermal Analysis and Calorimetry》2013,114(2):731-747
Layered double hydroxides (LDHs) containing Mg2+, Cu2+ or Zn2+ cations in the MeII positions and Al3+ and Fe3+ in the MeIII positions were synthesized by co-precipitation method. Detailed studies of thermal transformation of obtained LDHs into metal oxide systems were performed using high temperature X-ray diffraction in oxidising and reducing atmosphere, thermogravimetry coupled with mass spectrometry and temperature-programmed reduction. The LDH samples calcined at 600 and 900 °C were tested in the role of catalysts for selective oxidation of ammonia into nitrogen and water vapour. It was shown that all copper congaing samples presented high catalytic activity and additionally, for the Cu–Mg–Al and Cu–Mg–Fe hydrotalcite samples calcined at 600 °C relatively high stability and selectivity to dinitrogen was obtained. An increase in calcination temperature to 900 °C resulted in a decrease of their catalytic activity, possibly due to formation of well-crystallised metal oxide phases which are less catalytically active in the process of selective oxidation of ammonia. 相似文献
56.
Expression, characterization, and mutagenesis of a series of N-terminal fragments of an animal fatty acid synthase, containing the beta-ketoacyl synthase, acyl transferase, and dehydratase domains, demonstrate that the dehydratase domain consists of two pseudosubunits, derived from contiguous regions of the same polypeptide, in which a single active site is formed by the cooperation of the catalytic histidine 878 residue of the first pseudosubunit with aspartate 1032 of the second pseudosubunit. Mutagenesis and modeling studies revealed an essential role for glutamine 1036 in anchoring the position of the catalytic aspartate. These findings establish that sequence elements previously assigned to a central structural core region of the type I fatty acid synthases and some modular polyketide synthase counterparts play an essential catalytic role as part of the dehydratase domain. 相似文献
57.
Mono- and diglycerides play an important role in the metabolism of plants and animals. They are usually constitutive elements of complex mixtures and are not always as main components, which considerably hinder the identification of these analytes. This work communicates about a synthesis of a wide range of esters of glycerol and aliphatic C(6)-C(20) acids and presents gas chromatographic characteristics of 32 compounds in the form of the most reproducible parameters-linear-programmed retention indices on high-performance capillary columns with non-polar stationary phases. The article also presents mass spectra for a series of those glycerides which were not characterized earlier by these parameters. 相似文献
58.
Agnieszka Hryniewicka Iwona Misztalewska Dorota Czajkowska-Szczykowska Zofia Urbańczyk-Lipkowska Jacek W. Morzycki Stanisław Witkowski 《Tetrahedron》2014
Synthesis of new type of the Hoveyda–Grubbs catalysts containing modified N-heterocyclic carbene ligands is described herein. New catalysts bear different in size polyether clamp embracing N,N′-2,4-dimethylphenyl substituents in N-heterocyclic carbene. New complexes were tested in model RCM, enyne and CM reactions. They showed comparable activity to that of commercially available Grubbs second generation and Hoveyda–Grubbs second generation complexes. Complex with larger polyether clamp proved Z-stereoselective in a macrocycle formation and yielded more Z isomers than commercial complexes in CM reactions. The catalysts are stable and easy to purify. 相似文献
59.
The acceleration of thin plastic foils irradiated with frequency-triplet (λ = 0.44 μm) and fundamental (λ = 1.3 μm) iodine laser light was investigated. Rear-side velocities and two-dimensional behaviour of the foils were recorded with a novel 6-frame photographic diagnostic. Core velocities were inferred from calorimetry and X-ray backlighting. Unlike at 1.3 μm, the rear-side and core velocities were found to be quite different at λ = 0.44 μm. An explanation is offered in terms of lack of lateral smoothing at 0.44 μm. The ablation pressure scales as Pabl≈I0.6absλ-0.4. 相似文献
60.