A5075447034- Cancer therapeutics and mechanisms
- Lung Cancer Treatments and Mutations
- Quinazolinone synthesis and applications
- Melanoma and MAPK Pathways
- Synthesis and Characterization of Heterocyclic Compounds
- Lung Cancer Research Studies
- Computational Drug Discovery Methods
- Pharmacological Effects of Natural Compounds
- Ubiquitin and proteasome pathways
- Protein Kinase Regulation and GTPase Signaling
- Cancer Mechanisms and Therapy
- Gout, Hyperuricemia, Uric Acid
- Immune Response and Inflammation
- Protein Degradation and Inhibitors
- Natural product bioactivities and synthesis
- Synthesis and biological activity
- Cytokine Signaling Pathways and Interactions
- Microbial Natural Products and Biosynthesis
- PI3K/AKT/mTOR signaling in cancer
- Chronic Myeloid Leukemia Treatments
- Phenothiazines and Benzothiazines Synthesis and Activities
- Traditional Chinese Medicine Analysis
- Glioma Diagnosis and Treatment
- Antibiotics Pharmacokinetics and Efficacy
- Click Chemistry and Applications
Southern Medical University
2014-2024
Australian Synchrotron
2009
Jinan University
2007
Based on the close relationship between programmed death protein ligand 1 (PD-L1) and epidermal growth factor receptor (EGFR) in glioblastoma (GBM), we designed synthesized a series of small molecules as potential dual inhibitors EGFR PD-L1. Among them, compound EP26 exhibited highest inhibitory activity against (IC50 = 37.5 nM) PD-1/PD-L1 interaction 1.77 μM). In addition, displayed superior vitro antiproliferative activities immunomodulatory effects by promoting U87MG cell U87MG/Jurkat...
Epidermal growth factor receptor (EGFR) inhibitors have been used in clinical for the treatment of non-small-cell lung cancer years. However, emergence drug resistance continues to be a major problem. To identify potential inhibitors, molecular docking-based virtual screening was conducted on ChemDiv and Enamine commercial databases using Glide program. After multi-step VS visual inspection, total 23 compounds with novel varied structures were selected, predicted ADMET properties within...
Developing a simple analytical method suitable for therapeutic drug monitoring in clinical setting is key to establishing guidelines on accurate dose administration and the advancement of precision medicine. We devised rapid through combination streptavidin-modified microparticles time-resolved fluorescence immunoassay monitoring. The performance this was investigated validated using samples. By determination doxorubicin concentration, proposed assay has shown satisfactory linear range...
Lung cancer is the leading cause of death, and epidermal growth factor receptor (EGFR) kinase domain mutations are a common non-small-cell lung (NSCLC), major subtype cancers. Patients harboring most these respond well to EGFR inhibitors Gefitinib Erlotinib initially, but soon develop resistance them due emergence gatekeeper mutation T790M. The new-generation such as AZD9291, HM61713, CO-1686 WZ4002 can overcome T790M through covalent binding Cys 797, ultimately lose their efficacy upon...
Clinical treatment by FDA-approved ROS1/ALK inhibitor Crizotinib significantly improved the therapeutic outcomes. However, emergence of drug resistance, especially driven acquired mutations, have become an inevitable problem and worsened clinical effects Crizotinib. To combat some novel 2-aminopyridine derivatives were designed rationally based on molecular simulation, then synthesised subjected to biological test. The preferred spiro derivative C01 exhibited remarkable activity against...
ABSTRACT Topotecan (TPT) is an important anti‐cancer drug that inhibits topoisomerase I. A sensitive and robust liquid chromatography–tandem mass spectrometry (LC‐MS/MS) method potentially determines TPT in beagle dog plasma needed for a bioequivalence study of formulations. We developed validated LC‐MS/MS to evaluate terms specificity, linearity, precision, accuracy, stability, extraction recovery matrix effect. Plasma samples were treated with Ostro TM sorbent plate (a effective tool)...
ROS1 and ALK are promising targets of anticancer drugs for non-small-cell lung cancer. Since they have 49% amide acid sequence homology in the kinases domain 77% identity at ATP binding area, some inhibitors also showed significant responses clinical trial, such as type-I inhibitor crizotinib PF-06463922. As a newly therapeutic target, selective is relatively rare. Moreover, molecular basis selectivity versus still remains unclear. In order to disclose preference toward over aid design...
Targeting the epidermal growth factor receptor (EGFR) is one of potential ways to treat glioblastoma (GBM). In this study, we investigate anti-GBM tumor effects EGFR inhibitor SMUZ106 in both vitro and vivo conditions. The on proliferation GBM cells were explored through MTT clone formation experiments. Additionally, flow cytometry experiments conducted study cell cycle apoptosis cells. inhibitory activity selectivity protein proved by Western blotting, molecular docking, kinase spectrum...
Standardized myrtol, an essential oil containing primarily cineole, limonene and α-pinene, has been used for treating nasosinusitis, bronchitis chronic obstructive pulmonary disease (COPD).To investigate the effects of standardized myrtol in a model acute lung injury (ALI) induced by lipopolysaccharides (LPS).Male BALB/c mice were treated with 1.5 h prior to exposure atomized LPS. Six hours after LPS challenge, was determined neutrophil recruitment, cytokine levels total protein...
Of patients bearing unresectable tumors at advanced stages, most undergo serious pain. For adjacent to vital organs or nerves, eliminating local cancer pain without adverse effects remains a formidable challenge. Interventional ablative therapies (IATs), such as radio frequency ablation (RFA), microwave ablation, and irreversible electroporation, have been clinically adopted treat various carcinomas. In this study, we established another palliative interventional therapy eliminate pain,...