Bioconjug Chem
CRCINA, INSERM 1232-CNRS ERL 6001, University of Angers, University of Nantes, 8 quai Moncousu , 44007 Nantes , France.
Published: September 2019
Following the successful synthesis of a -functionalized version of the TE1PA ligand, a monopicolinate cyclam, we looked to demonstrate its in vivo properties versus DOTA and NOTA, after conjugation on the 9E7.4 rat antibody, an IgG against CD138 murine, which has relevant properties for multiple myeloma targeting. For each ligand, different conjugation approaches had been considered to select the most appropriate for the comparative study. The -SCN-Bn-TE1PA, NHS-DOTA, and -SCN-Bn-NOTA were finally chosen for conjugation and radiolabeling tests. For in vivo comparison, we used a model of subcutaneous grafted mice with 5T33 tumor cells. In vitro tests and immuno-PET study highlighted Cu-9E7.4--SCN-Bn-NOTA as the least attractive. Further competitive biodistribution and hepatic metabolic studies at 2, 24, and 48 h post-injection (100 μg radiolabeled with 10 MBq of Cu) were then performed with the Cu-9E7.4--SCN-Bn-TE1PA and Cu-9E7.4-NHS-DOTA. Results show a better in vivo resistance of Cu-9E7.4--SCN-Bn-TE1PA to transchelation compared to Cu-9E7.4-NHS-DOTA, especially at later times. This was confirmed with Cu-9E7.4--SCN-Bn-NOTA at 48 h PI. Cu-9E7.4--SCN-Bn-TE1PA also demonstrated an excellent hepatic clearance. Cu-9E7.4--SCN-Bn-TE1PA displayed an overall superiority compared to Cu-9E7.4-NHS-DOTA and Cu-9E7.4--SCN-Bn-NOTA in terms of in vivo stability, reinforcing the usefulness of the SCN-Bn-TE1PA ligand for Cu immuno-PET imaging.
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http://dx.doi.org/10.1021/acs.bioconjchem.9b00510 | DOI Listing |
J Mol Model
January 2025
Shanxi Jiangyang Chemical Limited Company, Taiyuan, 030041, Shanxi, China.
Context: DNAN/DNB cocrystals, as a newly developed type of energetic material, possess superior safety and thermal stability, making them a suitable alternative to traditional melt-cast explosives. Nonetheless, an exploration of the thermal degradation dynamics of the said cocrystal composite has heretofore remained uncharted. Consequently, we engaged the ReaxFF/lg force field modality to delve into the thermal dissociation processes of the DNAN/DNB cocrystal assembly across a spectrum of temperatures, encompassing 2500, 2750, 3000, 3250, and 3500 K.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Biochemistry, Faculty of Pharmacy, Badr University in Cairo (BUC), Badr City, 11829, Cairo, Egypt.
Antibody-drug conjugates (ADCs) have emerged as a promising strategy in targeted cancer therapy, enabling the precise delivery of cytotoxic agents to tumor sites while minimizing systemic toxicity. However, traditional ADCs face significant limitations, including restricted drug loading capacity, where an optimal drug-to-antibody ratio (DAR) is crucial; low DARs may lead to insufficient potency, while high DARs can cause rapid clearance and increased toxicity. Additionally, ADCs often suffer from instability in circulation due to the potential for premature release of cytotoxic agents, resulting in off-target effects and reduced therapeutic efficacy.
View Article and Find Full Text PDFBackground: Neuroblastoma is a heterogeneous disease with adrenergic (ADRN)- and therapy resistant mesenchymal (MES)-like cells driven by distinct transcription factor networks. Here, we investigate the expression of immunotherapeutic targets in each neuroblastoma subtype and propose pan-neuroblastoma and cell state specific targetable cell-surface proteins.
Methods: We characterized cell lines, patient-derived xenografts, and patient samples as ADRN-dominant or MES-dominant to define subtype-specific and pan-neuroblastoma gene sets.
Anal Methods
September 2020
College of Life Sciences, Fujian Normal University, Fuzhou 350117, Fujian, China.
An innovative magnetic immunoassay was developed for the voltammetric detection of carbohydrate antigen-125 (CA-125) on a home-made microfluidic device including a multisyringe pump, selection valve and magneto-controlled detection cell. Two kinds of biofunctionalized nanostructures including anti-CA-125 capture antibody-conjugated magnetic beads and anti-CA-125 detection antibody-labeled silver-polypyrrole (Ag-PPy) nanohybrids were utilized for a sandwiched immunoreaction in the presence of CA-125. With the help of an external magnet, the formed magnetic immunocomplexes were attached to the sensing interface to activate the electrical contact between Ag-PPy nanohybrids and the base electrode, thus resulting in the switching on of the sensor circuit for the generation of voltammetric signals thanks to electroactive Ag-PPy nanohybrids.
View Article and Find Full Text PDFAnal Methods
November 2017
Institute of Biomedical Chemistry, ul. Pogodinskaya, 10, Moscow, Russia.
A combined AFM/MS method was employed for protein registration in solution. This method is based on reversible specific capturing of a target protein from a large volume of analyzed solution onto a small sensor area of a chip with immobilized aptamer ligands. Fishing of the core antigen of hepatitis C virus (HCVcoreAg) from 10 M solution of this protein in buffer was carried out.
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