A5100346105- Extracellular vesicles in disease
- Synthesis and biological activity
- Cancer, Hypoxia, and Metabolism
- Click Chemistry and Applications
- MicroRNA in disease regulation
- Melanoma and MAPK Pathways
- Computational Drug Discovery Methods
- Ubiquitin and proteasome pathways
- Vitamin D Research Studies
- Cancer-related Molecular Pathways
- HER2/EGFR in Cancer Research
- Estrogen and related hormone effects
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Biological Evaluation
- RNA Interference and Gene Delivery
- Cancer therapeutics and mechanisms
- Ferroptosis and cancer prognosis
- Synthesis of heterocyclic compounds
- Advanced Synthetic Organic Chemistry
- Peptidase Inhibition and Analysis
- Monoclonal and Polyclonal Antibodies Research
- Sulfur-Based Synthesis Techniques
- ATP Synthase and ATPases Research
- T-cell and B-cell Immunology
- Chemical Synthesis and Analysis
Shanghai University of Medicine and Health Sciences
2020-2025
Ningbo University
2023-2025
Peking University
2019-2024
China Medical University
2024
AbbVie (United States)
2020-2024
First Affiliated Hospital of Jinan University
2024
Shenyang Medical College
2024
Sun Yat-sen University Cancer Center
2010-2024
Sun Yat-sen University
2010-2024
Tang Du Hospital
2024
Structures of human monoamine oxidase B (MAO B) in complex with safinamide and two coumarin derivatives, all sharing a common benzyloxy substituent, were determined by X-ray crystallography. These compounds competitively inhibit MAO Ki values the 0.1-0.5 microM range that are 30-700-fold lower than those observed A. The inhibitors bind noncovalently to B, occupying both entrance substrate cavities showing similarly oriented substituent.
RORα and RORγ are expressed in human skin cells that produce the noncalcemic 20-hydroxyvitamin D3 [20(OH)D3] 20,23-dihydroxyvitamin [20,23(OH)2D3]. Chinese hamster ovary (CHO) stably expressing a Tet-on or expression vector ROR-responsive element (RORE)-LUC reporter, mammalian 2-hybrid model examining interaction between ligand binding domain (LBD) of with an LBD-interacting LXXLL-peptide, were used to study ROR-antagonist activities. These assays revealed 20(OH)D3 20,23(OH)2D3 function as...
Ferroptosis is a phospholipid peroxidation-mediated and iron-dependent cell death form, involved in sepsis-induced organ injury other lung diseases. Yes-associated protein 1 (YAP1), key regulator of the Hippo signaling pathway, could target multiple ferroptosis regulators. Herein, this study aimed to explore involvement etiopathogenesis acute (ALI) demonstrate that YAP1 disrupt ferritinophagy moderate ALI. Cecal ligation puncture (CLP) models were constructed wild-type (WT) pulmonary...
Novel ABI-III compounds were designed and synthesized based on our previously reported ABI-I ABI-II analogues. are highly potent against a panel of melanoma prostate cancer cell lines, with the best compound having an average IC50 value 3.8 nM. They not substrate Pgp thus may effectively overcome Pgp-mediated multidrug resistance. analogues maintain their mechanisms action by inhibition tubulin polymerization.
Cell-derived exosomes are leading candidates for in vivo drug delivery carriers. In particular, derived from 293T cells used most frequently, although exosome dosing has varied greatly among studies. Considering their biological origin, it is crucial to characterize the molecular composition of if large doses be administered clinical settings. this study, we present first comprehensive analysis protein, messenger RNA and microRNA profiles cell-derived exosomes; then, characterized these data...
MCL-1 is a prosurvival B-cell lymphoma 2 family protein that plays critical role in tumor maintenance and survival can act as resistance factor to multiple anticancer therapies. Herein, we describe the generation characterization of highly potent selective inhibitor ABBV-467 present findings from first-in-human trial included patients with relapsed/refractory myeloma (NCT04178902).Binding human was assessed cell lines. The ability induce growth inhibition investigated xenograft models acute...
Growing evidence indicates that tumour cells exhibit characteristics similar to their lineage progenitor cells. We found S100 calcium binding protein A10 (S100A10) exhibited an expression pattern of liver genes. However, the role S100A10 in hepatocellular carcinoma (HCC) progression is unclear. Furthermore, extracellular vesicles (EVs) are critical mediators tumourigenesis and metastasis, but functions S100A10, particularly those related EVs (EV-S100A10), unknown.The mechanisms EV-S100A10...
The premetastatic niche (PMN) contributes to lung-specific metastatic tropism in osteosarcoma. However, the crosstalk between primary tumor cells and lung stromal is not clearly defined. Here, we dissect composition of immune PMN identify granulocytic myeloid-derived suppressor cell (gMDSC) infiltration as positively associated with immunosuppressive formation colonization. Osteosarcoma-cell-derived extracellular vesicles (EVs) activate interstitial macrophages initiate influx gMDSCs via...
Abstract Background Chemoresistance is one of the main obstacles to successful cancer therapy and frequently associated with Multidrug resistance (MDR). Many different mechanisms have been suggested explain development an MDR phenotype in cells. One most studied overexpression P-glycoprotein (P-gp), which a product MDR1 gene. Tumor cells often acquire drug-resistance due upregulation Overexpression gene has reported primary gastric adenocarcinoma. Methods This study investigated role...
To block the metabolically labile sites of novel tubulin inhibitors targeting colchicine binding site based on SMART, ABI, and PAT templates, we have designed, synthesized, biologically tested three focused sets new derivatives with modifications at carbonyl linker, para-position in C ring SMART template, modification A template. Structure-activity relationships these compounds led to identification benzimidazole imidazo[4,5-c]pyridine-fused represented by 4 7, respectively, which showed...
A new series of indole analogues based on our earlier lead compound, 2-(1H-indol-5-yl)-4-(3,4,5-trimethoxyphenyl)-1H-imidazo[4,5-c]pyridine (42), was prepared as tubulin inhibitors in an effort to find a molecule with improved cytotoxic potency and metabolic stability. indolyl-imidazopyridines (IIP) were synthesized exhibited potent polymerization inhibitory activity IC50 values ranging from 3 175 nM against panel human melanoma prostate cancer cell lines. Among these compounds, the...
There is no effective treatment for systemic sclerosis and related fibrosing diseases. Recently the action of CYP11A1 on vitamin D(3) was shown to produce biologically active 20S-hydroxyvitamin D [20(OH)D(3)] 20,23(OH)(2)D(3), 20,22(OH)(2)D(3), 17,20,23(OH)(3)D(3).Because 20(OH)D(3) noncalcemic (nontoxic) in vivo at very high doses, we evaluated its antifibrogenic activities both vitro vivo. Because it further metabolized by CYP11A1, also tested preclinical utilities hydroxyderivatives,...
Novel small molecule compounds based on various scaffolds including chalcone, flavonoid, and resorcinol dibenzyl ether were designed tested for their inhibitory activity against the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) pathway. Among them, compound NP19 inhibited human PD-1/PD-L1 interaction with IC50 values of 12.5 nM in homogeneous time-resolved fluorescence (HTRF) binding assays. In addition, dose-dependently elevated IFN-γ production a coculture model...
Exosomes are essential mediators of intercellular communication as they transport proteins and RNAs between cells. Owing to their tumor-targeting capacity, immune compatibility, low toxicity, long half-life, mesenchymal stem cell-derived exosomes have great potential for the development novel antitumor strategies. In this context, role produced by adipose-derived cells (ADSCs) treatment bladder cancer (BC) remains unclear. Here, we investigated use ADSCs a source therapeutic exosomes, well...