A5100454201- Analytical Chemistry and Chromatography
- Microfluidic and Capillary Electrophoresis Applications
- Natural product bioactivities and synthesis
- Chemical synthesis and alkaloids
- Cholinesterase and Neurodegenerative Diseases
- Inflammatory Bowel Disease
- Synthesis and biological activity
- Electrochemical Analysis and Applications
- Computational Drug Discovery Methods
- Innovative Microfluidic and Catalytic Techniques Innovation
- Biological Activity of Diterpenoids and Biflavonoids
- Phytochemical compounds biological activities
- Quinazolinone synthesis and applications
- Nitric Oxide and Endothelin Effects
- Peptidase Inhibition and Analysis
- Cancer therapeutics and mechanisms
- Bioactive Compounds and Antitumor Agents
- Renin-Angiotensin System Studies
- Protein Degradation and Inhibitors
- Asymmetric Synthesis and Catalysis
- Liver Disease Diagnosis and Treatment
- Phosphodiesterase function and regulation
- Receptor Mechanisms and Signaling
- Inflammasome and immune disorders
- Ubiquitin and proteasome pathways
China Pharmaceutical University
2015-2025
Development Research Center
2020
Guangxi Normal University
2018
Anhui Medical University
2015
Shanghai Jiao Tong University
2013-2014
Abstract Hydrophobic tagging (HyT) is a potential therapeutic strategy for targeted protein degradation (TPD). Norbornene was discovered as an unprecedented hydrophobic tag in this study and used to degrade the anaplastic lymphoma kinase (ALK) fusion by linking it ALK inhibitors. The most promising degrader, Hyt‐9 , potently reduced levels through Hsp70 ubiquitin−proteasome system (UPS) vitro without compensatory upregulation of . Furthermore, exhibited significant tumor‐inhibiting effect...
Based on a multitarget strategy, series of novel tacrine–pyrimidone hybrids were identified for the potential treatment Alzheimer's disease (AD). Biological evaluation results demonstrated that these exhibited significant inhibitory activities toward acetylcholinesterase (AChE) and glycogen synthase kinase 3 (GSK-3). The optimal compound 27g possessed excellent dual AChE/GSK-3 inhibition both in terms potency equilibrium (AChE: IC50 = 51.1 nM; GSK-3β: 89.3 nM) displayed amelioration...
Viruses are a leading cause of infectious diseases. Well-developed animal models valuable for understanding the immune responses to viral infections and pathogenesis Zebrafish is commonly used small vertebrate model organism with strong reproductive ability, short life cycle, rapid embryonic development. Moreover, zebrafish human genomes highly similar; they have approximately 70 % homology in protein-coding genes, 84 genes associated diseases counterparts. Recent years, different groups...
Non-alcoholic fatty liver disease is a public health problem worldwide associated with high morbidity and hepatic steatosis, but no effective therapeutic interventions. Magnesium isoglycyrrhizinate (MGIG), derivative of an active component Glycyrrhiza glabra, widely used for the treatment inflammatory diseases due to its potent anti-inflammatory hepatoprotective activities. Hence, this study aimed effects MGIG on steatosis in mice fed high-fat diet (HFD). Oil Red O staining transmission...
A collection of isoxazole and oxadiazole substituted 23-hydroxybetulinic acid (HBA) derivatives were designed, synthesized evaluated for their antitumor activity. Most the newly compounds exhibited more potent antiproliferative activity than patent compound acid, especially 13e 14a about four- to sevenfold against all tested cancer cell lines acid. Furthermore, in vivo was validated H22 liver B16 melanoma xenograft mouse models. The structure-activity relationships these also discussed based...
Abstract Background Pharmaceutical care is attached with increasing importance around the world due to its clinical and economical effects. Tertiary hospitals are equipped richest healthcare resources pioneer in implementation of pharmaceutical care. Understanding current status provision tertiary not only helps improve practice but also guide development secondary primary health institutions. Method Data a cross-sectional survey were used. The was conducted from July 2015 June 2016,...
A series of novel 4‐isochromanone compounds bearing N ‐benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase ( AC hE) inhibitors. The biological evaluation showed that most the target exhibited potent inhibitory activities against hE. Among them, compound 1q possessed strongest anti‐ hE activity with an IC 50 value 0.15 n m high hE/BuChE selectivity SI > 5,000). Moreover, had low toxicity in normal nerve cells was relatively stable rat plasma. Together, current...