A5103280387- Catalytic Processes in Materials Science
- Catalysis and Oxidation Reactions
- Nanoparticle-Based Drug Delivery
- Ubiquitin and proteasome pathways
- Industrial Gas Emission Control
- Advanced Photocatalysis Techniques
- Nanoplatforms for cancer theranostics
- Pharmacogenetics and Drug Metabolism
- Peptidase Inhibition and Analysis
- Drug Transport and Resistance Mechanisms
- Anodic Oxide Films and Nanostructures
- Air Quality and Health Impacts
- Chalcogenide Semiconductor Thin Films
- Lung Cancer Treatments and Mutations
- Supramolecular Self-Assembly in Materials
- Colorectal Cancer Treatments and Studies
- Quantum Dots Synthesis And Properties
- Supramolecular Chemistry and Complexes
- Analytical chemistry methods development
- Climate Change and Health Impacts
- Natural Compounds in Disease Treatment
- Advanced Proteomics Techniques and Applications
- Heat shock proteins research
- Blood disorders and treatments
- Traditional Chinese Medicine Analysis
Jiamusi University
2024
Jupiter Medical Center
2022-2023
Scripps Research Institute
2009-2021
South China University of Technology
2021
State Key Laboratory of Luminescent Materials and Devices
2021
Nanjing University of Science and Technology
2011-2020
Ningbo Center for Disease Control and Prevention
2017-2018
Wuhan University
2016
Renmin Hospital of Wuhan University
2016
Pfizer (United States)
2013
Dasatinib was approved in 2006 for the treatment of imatinib-resistant chronic myelogenous leukemia and functions primarily through inhibition BCR-ABL Src kinase. is extensively metabolized humans by CYP3A4. In this study, we report that bioactivation dasatinib CYP3A4 proceeds a reactive intermediate leads to inactivation with <i>K</i><sub>I</sub> = 6.3 μM <i>k</i><sub>inact</sub> 0.034 min<sup>–1</sup>. The major mechanism hydroxylation at <i>para</i>-position 2-chloro-6-methylphenyl ring...
Our recent studies have provided a proteomic blueprint of the 26S proteasome complexes in heart, among which 20S proteasomes were found to contain cylinder-shaped structures consisting both alpha and beta subunits. These exhibit number features unique myocardium, including striking differences post-translational modifications (PTMs) individual subunits novel PTMs that not been previously reported. To date, mechanisms contributing regulation this myocardial proteolytic core system remain...
Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase and has been approved for treatment nonsmall cell lung cancer refractory to established treatments. Several cases adverse hepatic pulmonary events have reported, which led discontinuation therapy. While mechanism toxicity remains unknown, we present evidence that gefitinib accumulates in liver lung, it can be bioactivated hepatic, intestinal, microsomes form a reactive metabolite. The metabolite was...
The leaves of Mitragyna speciosa (kratom), a plant native to Southeast Asia, are increasingly used as pain reliever and for attenuation opioid withdrawal symptoms. Using the tools natural products chemistry, chemical synthesis, pharmacology, we provide detailed in vitro vivo pharmacological characterization alkaloids kratom. We report that metabolism kratom's major alkaloid, mitragynine, mice leads formation (a) potent mu receptor agonist antinociceptive agent, 7-hydroxymitragynine, through...
The epidermal growth factor receptor tyrosine kinase inhibitor erlotinib (ERL) is approved for treatment of non–small-cell lung cancer. Numerous reports ERL-associated toxicities are consistent with immune-mediated toxicity, including drug-induced hepatitis, interstitial disease, Stevens-Johnson syndrome, and toxic necrolysis. Although the mechanism toxicity has not been established, we present evidence that reactive intermediates formed during metabolism ERL, which can covalently conjugate...
The 20 S proteasomes play a critical role in intracellular homeostasis and stress response. Their function is tuned by covalent modifications, such as phosphorylation. In this study, we performed comprehensive characterization of the phosphoproteome for proteasome complexes both murine heart liver. A platform combining parallel approaches differential sample fractionation (SDS-PAGE, IEF, two-dimensional electrophoresis), enzymatic digestion (trypsin chymotrypsin), phosphopeptide enrichment...
In this study, we described a novel S-doped V2O5–WO3/TiO2 (VWTiS) catalyst that showed superior low-temperature NH3-selective catalytic reduction (SCR) activity in comparison with the VWTi catalyst. These catalysts were extensively studied by series of characterizations and density functional theory (DFT) calculations. Results revealed impregnated WO3 V2O5 species preferentially interacting doped S site, which improved electron transfer from to promoted formation reduced vanadium species....
Almost half of prescription medications are metabolized by cytochrome P450 3A4 and 3A5. CYP3A4 3A5 have significant substrate overlap, there is currently no way to selectively monitor the activity these two enzymes, which has led erroneous habit attributing cumulative CYP3A4. While expression ubiquitous, CYP3A5 polymorphic, with large individual differences in level. The genotype been shown alter pharmacokinetics drugs clinical trials. We report first tool compound capable determining...
Clozapine was the first of atypical antipsychotics to be developed, but its use has been restricted because toxicity issues, particularly risk potentially life-threatening drug-induced neutropenia and agranulocytosis, which occurs in about 1% patients. Bioactivation clozapine by peroxidases forms a reactive nitrenium ion, covalently adducts protein leads neutrophil toxicity. The current generation clozapine-inspired reduced through improved potency/decreased dose or structural modification...
Current molecular tools lack the ability to differentiate activity of CYP3A4 and CYP3A5 in biological samples such as human liver microsomes. Kinetic experiments crystal structure indicate that active sites both enzymes are large flexible, have more than one binding subsite within site. 1-(4-Imidazopyridinyl-7phenyl)-3-(4′-cyanobiphenyl) urea (SR-9186) was optimized through several rounds structural refinement from an initial screening hit obtain greater 1000-fold selectivity for inhibition...
A novel magnetic metal-organic framework composite was prepared by a self-assembly approach. The material properties were characterized Fourier-transform infrared spectroscopy, vibrating sample magnetometry, thermogravimetry and differential thermogravimetric analysis, X-photoelectron spectroscopy. Then, the as-prepared used as an adsorbent indicated great enrichment ability toward glyphosate, glufosinate, bialaphos, their main metabolites aminomethylphosphonic acid...
HSPA1A (HSP70-1) is a highly inducible heat shock gene up-regulated in response to environmental stresses and pollutants. The aim of our study was evaluate the sensitivity stable metabolically competent HepG2 cells containing human promoter-driven luciferase reporter (HepG2-luciferase cells) for assessing toxicity organic pollutants present air. HepG2-luciferase were validated by treatment testing three compounds (pyrene, benzo[a]pyrene, formaldehyde) that are ubiquitous maximal level...
Docetaxel (DTX) has been widely used for the treatment of many types cancer. However, DTX is poorly water-soluble and commercial formulated in non-ionic surfactant polysorbate 80 ethanol, thereby leading to hypersensitivity serious side effects. Herein, a polymer dual drug conjugate was synthesized by coupling docosahexaenoic acid (DHA) with bifunctionalized dextran. The polysaccharide dextran-DHA-DTX possessed high water solubility self-assembled into nanoparticles diameter 98.0 ± 6.4 nm....