Covalent binding of various clinically important nitrogen mustards to the cysteine-34 residue of human serum albumin, in vitro and in vivo, is demonstrated. A rapid method for detection of these adducts is presented, based on liquid chromatography-tandem mass spectrometry analysis of the adducted tripeptide Cys*-Pro-Phe after digestion of the protein with Pronase.
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http://dx.doi.org/10.1007/s00204-001-0318-2 | DOI Listing |
Phys Chem Chem Phys
January 2025
Department of Physics, Assam University, Silchar-788011, India.
Density functional theory has been employed to study indolo[3,2,1-]carbazole donor-based dyes, incorporating one and two units of 2,4-dimethoxybenzene auxiliary donors. Electrostatic potential analysis highlights the dye with one auxiliary donor (D2) as having the highest charge-donating capability. Structural analysis shows that auxiliary donors enhance planarity, reduce steric hindrance, and improve π-conjugation.
View Article and Find Full Text PDFMedComm (2020)
January 2025
Department of Urology, Guangdong Provincial Clinical Research Center for Geriatrics, Shenzhen Clinical Research Centre for Geriatrics Shenzhen People's Hospital, The First Affiliated Hospital, Southern University of Science and Technology Shenzhen China.
Periodontitis is a chronic periodontal inflammatory disease caused by periodontal pathogens commonly seen in adults. Eupalinolide B (EB) is a sesquiterpenoid natural product extracted from Eupatorium lindleyanum and has been reported as a potential drug for cancers and immune disorders. Here, we explored the ameliorative effects and underlying molecular mechanism of EB on periodontitis for the first time.
View Article and Find Full Text PDFACS Med Chem Lett
January 2025
Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) is a unique peptidyl-prolyl isomerase (PPIase), and inactivation of Pin1 with a covalent inhibitor is a potential strategy for developing anticancer agents. Herein, a series of sulfolane amino-substituted 2-chloro-5-nitropyrimidine derivatives were disclosed as structurally distinct covalent inhibitors toward Pin1, which were validated for their covalent binding to Cys113 of Pin1 by X-ray cocrystal structures of compounds (IC = 11.55 μM) and (IC = 3.
View Article and Find Full Text PDFAdv Sci (Weinh)
January 2025
Department of Chemistry, University of North Texas1508 W Mulberry St, Denton, TX, 76201, USA.
Efficient removal of TcO from radioactive effluents while recovering drinking water remains a challenge. Herein, an excellent ReO (a nonradioactive surrogate of TcO ) scavenger is presented through covalently bonding imidazolium poly(ionic liquids) polymers with an ionic porous aromatic framework (iPAF), namely iPAF-P67, following an adsorption-site density-addition strategy. It shows rapid sorption kinetics, high uptake capacity, and exceptional selectivity toward ReO .
View Article and Find Full Text PDFJ Control Release
January 2025
State Key Laboratory of Food Science and Resources, China-Canada Joint Lab of Food Science and Technology (Nanchang), Key Laboratory of Bioactive Polysaccharides of Jiangxi Province, Nanchang University, Nanchang 330047, China.
Selenium deficiency associated with a high risk of many diseases remains a global challenge. Owing to the narrow margin between "nutrition-toxicity" doses of selenium, it is imperative to achieve accurate selenium supplement. Nano‑selenium (SeNPs) is a novel form of selenium supplement with low toxicity, but it could be trapped and removed by intestinal mucus, thus limiting its oral delivery.
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