A5081161833- Sphingolipid Metabolism and Signaling
- Wnt/β-catenin signaling in development and cancer
- Cancer, Hypoxia, and Metabolism
- Computational Drug Discovery Methods
- PI3K/AKT/mTOR signaling in cancer
- Caveolin-1 and cellular processes
- Hepatitis C virus research
- Bioactive Compounds and Antitumor Agents
- Ubiquitin and proteasome pathways
- Synthesis and Biological Evaluation
- Chemical Synthesis and Analysis
- Chemical synthesis and alkaloids
- Biochemical and Molecular Research
- Click Chemistry and Applications
- Sesquiterpenes and Asteraceae Studies
- Cancer-related gene regulation
- Protein Kinase Regulation and GTPase Signaling
- Crystallization and Solubility Studies
- Quinazolinone synthesis and applications
- Asymmetric Synthesis and Catalysis
- Lipid Membrane Structure and Behavior
- X-ray Diffraction in Crystallography
- Erythrocyte Function and Pathophysiology
- Cholesterol and Lipid Metabolism
- Traditional and Medicinal Uses of Annonaceae
Fudan University
2014-2024
Shanghai Institute of Pharmaceutical Industry
2015
Shanghai Medical College of Fudan University
1996-2014
University of North Carolina at Chapel Hill
2012
Shanghai Institute of Organic Chemistry
2011
Chinese Academy of Sciences
2011
The choline transporter (ChT) is used to transporte choline-derivate-modified nanoparticles across the blood-brain barrier. It demonstrated that ChT an ideal Trojan horse. exhibit higher permeability brain capillary endothelial cells (BCECs) monolayer in vitro and gene distribution expression vivo. Detailed facts of importance specialist readers are published as "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They made available submitted by authors....
Glycolytic enzyme phosphoglycerate mutase 1 (PGAM1) plays a critical role in cancer metabolism by coordinating glycolysis and biosynthesis. A well-validated PGAM1 inhibitor, however, has not been reported for treating pancreatic ductal adenocarcinoma (PDAC), which is one of the deadliest malignancies worldwide. By uncovering elevated expressions were statistically related to worse prognosis PDAC cohort 50 patients, we developed series allosteric inhibitors structure-guided optimization. The...
Sphingomyelin synthase (SMS) plays an important role in plasma atherogenic lipoprotein metabolism, inflammation, and the development of atherosclerosis. To understand whether impaired apoB secretion inflammation response is a direct result from lack SMS activity, this study, we prepared series compounds that inhibit activity. Further, characterized Dy105, most potent inhibitor. We found Dy105 treatment significantly reduces SM levels SM-rich microdomain on cell membranes. Moreover,...
Sphingomyelin synthase 2 (SMS2) is a promising therapeutic target for several chronic inflammation-associated diseases, including atherosclerosis, fatty liver, and insulin resistance. Herein, we report the identification of 4-benzyloxybenzo[ d]isoxazole-3-amine derivatives as potent highly selective SMS2 inhibitors through conformational restriction strategy. After systematic structural modifications, compounds with high selectivity good potency in vitro were selected further evaluation....
Analogues or isosteres of α,γ-diketoacid (DKA) 1a show potent inhibition hepatitis C virus (HCV) NS5B polymerase through chelation the two magnesium ions at active site. The anti-HCV activity flavonoid quercetin (2) could partly be attributed to it being a structural mimic DKAs. In order delineate features required for inhibitory effect and improve potency, novel types analogues, 7-O-arylmethylquercetins quercetin-3-O-benzoic acid esters, were designed, synthesized evaluated their properties...
Post-translational modifications play vital roles in fine-tuning a myriad of physiological processes, and one the most important is acetylation. Here, we report ligand-directed site-selective acetylation using KHAc, derivative phosphoglycerate mutase 1 (PGAM1) inhibitor. KHAc binds to PGAM1 transfers its acetyl group ε-NH2 Lys100 inactivate enzyme. The transfer process was visualized by time-resolved crystallography, demonstrating that driven proximity effects. capable selectively...
Recently, irreversible inhibitors have attracted great interest in antitumors due to their advantages of forming covalent bonds target proteins. Herein, some benzothiazepinone compounds (BTZs) been designed and synthesized as novel GSK-3β with high selectivity for the kinase panel. The binding mode was identified by kinetics mass spectrometry, main labeled residue confirmed be unique Cys14 that exists only GSK-3β. candidate 4-3 (IC50 = 6.6 μM) showed good proliferation inhibition...
ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTHighly Diastereoselective Epoxidation of Cycloalkenols with Monoperoxyphthalic Acid in WaterDeyong Ye, Francesco Fringuelli, Oriana Piermatti, and Ferdinando PizzoView Author Information Department Organic Chemistry, Shanghai Medical University 200032, Shanghai, China, Dipartimento di Chimica, Università Perugia, Via Elce Sotto 8, 06100 ItalyCite this: J. Org. Chem. 1997, 62, 11, 3748–3750Publication Date (Web):May 30, 1997Publication History...
Upregulation of phosphoglycerate mutase 1 (PGAM1) has been identified as one common phenomenon in a variety cancers. Inhibition PGAM1 provides new promising therapeutic strategy for cancer treatment. Herein, based on our previous work, series N-xanthone benzenesulfonamides were discovered novel inhibitors. The representative molecule 15h, with an IC50 2.1 μM, showed enhanced inhibitory activity and higher enzyme specificity compared to PGMI-004A, well slightly improved antiproliferative activity.