A5100738287- Induction Heating and Inverter Technology
- Cell death mechanisms and regulation
- ATP Synthase and ATPases Research
- Welding Techniques and Residual Stresses
- Aluminum Alloy Microstructure Properties
- Ubiquitin and proteasome pathways
- RNA Interference and Gene Delivery
- Metallurgical Processes and Thermodynamics
- Microstructure and Mechanical Properties of Steels
- Laser and Thermal Forming Techniques
- Chemical Synthesis and Analysis
- interferon and immune responses
- Catalytic Processes in Materials Science
- Metallurgy and Material Forming
- Magnetic Properties and Applications
- Advanced Welding Techniques Analysis
- Aquaculture disease management and microbiota
- Coastal and Marine Dynamics
- Ferroptosis and cancer prognosis
- Peptidase Inhibition and Analysis
- Epigenetics and DNA Methylation
- Cancer Immunotherapy and Biomarkers
- RNA modifications and cancer
- Sulfur Compounds in Biology
- Power Systems and Technologies
Sun Yat-sen University
2013-2025
Sun Yat-sen University Cancer Center
2018-2025
North China Electric Power University
2009-2024
China Electric Power Research Institute
2009-2024
State Key Laboratory of Oncology in South China
2019-2024
Xiamen University
2024
Changzhou University
2024
Shanghai Tenth People's Hospital
2024
Tongji University
2024
Shenyang Aerospace University
2024
We report the discovery and characterization of SM-406 (compound 2), a potent orally bioavailable Smac mimetic an antagonist inhibitor apoptosis proteins (IAPs). This compound binds to XIAP, cIAP1, cIAP2 with Ki 66.4, 1.9, 5.1 nM, respectively. Compound 2 effectively antagonizes XIAP BIR3 protein in cell-free functional assay, induces rapid degradation cellular cIAP1 protein, inhibits cancer cell growth various human lines. It has good oral bioavailability mice, rats, non-human primates,...
The interaction between β-catenin and B-cell CLL/lymphoma 9 (BCL9), critical for the transcriptional activity of β-catenin, is mediated by a helical segment from BCL9 large binding groove in β-catenin. Design potent, metabolically stable peptides represents an attractive approach to inhibit In this study, we report use Huisgen 1,3-dipolar cycloaddition reaction generate triazole-stapled α-helical peptides. high efficiency mild conditions "click" combined with ease synthesis necessary...
Signal transducer and activator of transcription 3 (STAT3) is a factor an attractive therapeutic target for cancer other human diseases. Despite 20 years persistent research efforts, targeting STAT3 has been very challenging. We report herein the structure-based discovery potent small-molecule degraders based upon proteolysis chimera (PROTAC) concept. first designed SI-109 as potent, inhibitor SH2 domain. Employing ligands cereblon/cullin 4A E3 ligase SI-109, we obtained series PROTAC...
Combining anti-angiogenic therapy with immune checkpoint blockade anti-programmed cell death-1 (PD-1) antibodies is a promising treatment for hepatocellular carcinoma (HCC). Tyrosine kinase inhibitors are well-known agents and offer potential combination anti-PD-1 antibodies. This study investigated the possible underlying immunomodulatory mechanisms of combined therapy.HCC tissue samples RNA-sequencing (RNA-seq) were obtained from patients differential prognoses following treatment....
Small-molecule Smac mimetics are being developed as a novel class of anticancer drugs. Recent studies have shown that target cellular inhibitor apoptosis protein (cIAP)-1/2 for degradation and induce tumor necrosis factor-alpha (TNFalpha)-dependent in cells. In this study, we investigated the mechanism action therapeutic potential two different types mimetics, monovalent SM-122 bivalent SM-164. Our data showed removal cIAP-1/2 by or small interfering RNA is not sufficient robust...
Edwardsiella tarda, the causative agent of Edwardsiellosis, imposes medical challenges in both clinic and aquaculture. The emergence multidrug resistant strains makes antibiotic treatment impractical. identification molecules that facilitate or promote efficacy is high demand. In present study, we aimed to identify small whose abundance correlated with kanamycin resistance E. tarda by gas chromatography–mass spectrometry. We found fructose was greatly suppressed kanamycin-resistant strains....
In this study, ZIF-8 with a rhombic dodecahedron structure was prepared by hydrothermal method. Then La(OH)3, successfully loaded onto the an immersion deposition method, to form lanthanide-based metal-organic framework (La@ZIF-8) composites. The and properties of La@ZIF-8 were verified X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), transmission (TEM), thermogravimetric analysis (TGA), zeta potential measurements. optimum process...
Abstract Colorectal cancer (CRC) patients with liver metastases usually obtain less benefit from immunotherapy, and the underlying mechanisms remain understudied. Here, we identify that fibrinogen-like protein 1 (FGL1), secreted cells hepatocytes, facilitates progression of CRC in an intraportal injection model by reducing infiltration T cells. Mechanistically, tumor-associated macrophages (TAMs) activate NF-ĸB secreting TNFα/IL-1β microenvironment transcriptionally upregulate OTU...
We report herein the structure-based design of a class conformationally constrained, potent, cell-permeable small-molecule inhibitors to target SH2 domain in STAT3. Compound 11 (CJ-1383) binds STAT3 with K(i) value 0.95 µM, dose-dependently inhibits cellular signaling and cancer cell growth, induces apoptosis MDA-MB-468 line constitutively activated
Smac mimetics are being developed as a new class of anticancer therapies. Because the single-agent activity is very limited, rational combinations represent viable strategy for their clinical development. The combination with TNF-related apoptosis inducing ligand (TRAIL) may be particularly attractive because low toxicity TRAIL to normal cells and synergistic antitumor observed combination. In this study, we have investigated synergy between potent mimetic, SM-164, in vitro vivo underlying...
Recent study suggests that auranofin (AF), a US Food and Drug Administration (FDA)-approved drug for treatment of rheumatoid arthritis, has selective anticancer activity in various experimental models. Its clinical applications cancer treatment, however, have been hampered due part to its relatively moderate as single agent. In this study, we performed high-throughput screening the FDA-approved library compounds potentiate auranofin, unexpectedly identified an anti-inflammatory celecoxib...
The Hippo signaling pathway plays an essential role in organ size control and tumorigenesis. Loss of signal hyper-activation the downstream oncogenic YAP are commonly observed various types cancers. We previously identified STRN3-containing PP2A phosphatase as a negative regulator MST1/2 kinases (i.e., Hippo) gastric cancer (GC), opening possibility selectively targeting PP2Aa-STRN3-MST1/2 axis to recover against cancer. Here, we further discovered 1) disulfiram (DSF), FDA-approved drug,...
Peptide-based molecules hold great potential as targeted inhibitors of intracellular protein–protein interactions (PPIs).
Alterations in ROS metabolism and redox signaling are often observed cancer cells play a significant role tumor development drug resistance. However, the mechanisms by which alterations impact cellular sensitivity to anticancer drugs remain elusive. Here we have identified mitochondrial isoform of thioredoxin reductase 3 (mtTXNRD3), through RT-PCR microarray screen, as key molecule that confers resistance sorafenib other clinical agents. High expression mtTXNRD3 is detected drug-resistant...
In this paper, a hydrangea-like Bi2WO6 material was first synthesized by hydrothermal method. Then, as carrier, NiO-Bi2WO6 composite photocatalyst successfully the method and high-temperature calcination applied to studying removal of benzothiophene (BT) from fluid catalytic cracking (FCC) gasoline. The morphology, crystal structure elemental composition catalyst were characterized scanning electron microscopy (SEM), transmission (TEM), energy-dispersive X-ray spectroscopy (EDS), diffraction...