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Zwitterionic Hydrogels: From Synthetic Design to Biomedical Applications.
Langmuir
January 2025
State Key Laboratory of Separation Membranes and Membrane Processes, Key Laboratory of Hollow Fiber Membrane Materials and Membrane Processes (MOE), & Tianjin Key Laboratory of Hollow Fiber Membrane Materials and Processes, School of Materials Science and Engineering, Tiangong University, Tianjin, 300387, China.
Zwitterionic hydrogels have emerged as a highly promising class of biomaterials, attracting considerable attention due to their unique properties and diverse biomedical applications. Zwitterionic moieties, with their balanced positive and negative charges, endow hydrogels with exceptional hydration, resistance to nonspecific protein adsorption, and low immunogenicity due to their distinctive molecular structure. These properties facilitate various biomedical applications, such as medical device coatings, tissue engineering, drug delivery, and biosensing.
View Article and Find Full Text PDFIncreasing brain half-life of antibodies by additional binding to myelin oligodendrocyte glycoprotein, a CNS specific protein.
Fluids Barriers CNS
January 2025
Laboratory for Therapeutic and Diagnostic Antibodies, KU Leuven - University of Leuven, O&N II Herestraat 49 box 820, 3000, Leuven, Belgium.
Background: Therapeutic antibodies for the treatment of neurological disease show great potential, but their applications are rather limited due to limited brain exposure. The most well-studied approach to enhance brain influx of protein therapeutics, is receptor-mediated transcytosis (RMT) by targeting nutrient receptors to shuttle protein therapeutics over the blood-brain barrier (BBB) along with their endogenous cargos. While higher brain exposure is achieved with RMT, the timeframe is short due to rather fast brain clearance.
View Article and Find Full Text PDFHeterotropic allosteric modulation of CYP3A4 in vitro by progesterone: Evidence for improvement in prediction of time-dependent inhibition for macrolides.
Drug Metab Dispos
January 2025
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana.
Predictions of drug-drug interactions resulting from time-dependent inhibition (TDI) of CYP3A4 have consistently overestimated or mispredicted (ie, false positives) the interaction that is observed in vivo. Recent findings demonstrated that the presence of the allosteric modulator progesterone (PGS) in the in vitro assay could alter the in vitro kinetics of CYP3A4 TDI with inhibitors that interact with the heme moiety, such as metabolic-intermediate complex forming inhibitors. The impact of the presence of 100 μM PGS on the TDI of molecules in the class of macrolides typically associated with metabolic-intermediate complex formation was investigated.
View Article and Find Full Text PDFStructural insights into polyisoprenyl-binding glycosyltransferases.
Structure
January 2025
Department of Physiology and Cellular Biophysics, Columbia University Irving Medical Center, New York, NY 10032, USA. Electronic address:
Glycosyltransferases (GTs) catalyze the addition of sugars to diverse substrates facilitating complex glycoconjugate biosynthesis across all domains of life. When embedded in or associated with the membrane, these enzymes often depend on polyisoprenyl-phosphate or -pyrophosphate (PP) lipid carriers, including undecaprenyl phosphate in bacteria and dolichol phosphate in eukaryotes, to transfer glycan moieties. GTs that bind PP substrates (PP-GTs) are functionally diverse but share some common structural features within their family or subfamily, particularly with respect to how they interact with their cognate PP ligands.
View Article and Find Full Text PDFSynthesis, antimicrobial evaluation, ADMET prediction, molecular docking and dynamics studies of pyridine and thiophene moiety-containing chalcones.
R Soc Open Sci
January 2025
Department of Chemistry, Jagannath University, Dhaka 1100, Bangladesh.
In this study, three pyridine- and four thiophene-containing chalcone derivatives were synthesized via Claisen-Schmidt condensation reaction, where five derivatives were new. Different spectral analyses (IR, H NMR, HRMS) clarified the structures and these proposed compounds were screened for antimicrobial activity by the agar disc diffusion technique. Compound was conspicuously active against most of the bacterial and fungal strains.
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