A5101457038- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Cell Adhesion Molecules Research
- Bioactive Compounds and Antitumor Agents
- Antimicrobial Peptides and Activities
- Natural product bioactivities and synthesis
- Cancer therapeutics and mechanisms
- Peptidase Inhibition and Analysis
- Chemical Synthesis and Analysis
- Pharmacological Effects of Natural Compounds
- Chronic Kidney Disease and Diabetes
- Cardiac Valve Diseases and Treatments
- Crystallography and molecular interactions
- Acute Kidney Injury Research
- Synthesis and biological activity
- Contact Dermatitis and Allergies
- Neural Networks and Applications
- Asymmetric Synthesis and Catalysis
- Pulmonary Hypertension Research and Treatments
- Graphene and Nanomaterials Applications
- HER2/EGFR in Cancer Research
- Bioactive natural compounds
- Metal complexes synthesis and properties
- Catalytic C–H Functionalization Methods
- Cholinesterase and Neurodegenerative Diseases
The Seventh Affiliated Hospital of Sun Yat-sen University
2025
Sun Yat-sen University
2025
Experimental Center of Forestry in North China
2025
Tianjin Medical University General Hospital
2025
Technologies pour la Santé
2025
Université de Bordeaux
2024-2025
National Institutes for Food and Drug Control
2010-2024
Chinese Academy of Medical Sciences & Peking Union Medical College
2015-2024
Institut Européen de Chimie et Biologie
2021-2024
Peking Union Medical College Hospital
2015-2024
Drug-induced liver injury (DILI) is one of the major concerns during drug development. Wide acceptance 3 R principles and innovation in-vitro techniques have introduced various novel model options, among which three-dimensional (3D) cell spheroid cultures shown a promising prospect in DILI prediction. The present study developed 3D quadruple co-culture for prediction via self-assembly. Induction by phorbol 12-myristate 13-acetate at concentration 15.42 ng/mL 48 hours with following 24-hour...
Novel films on Ti-based orthopedic implants for localized antimicrobial delivery, which comprises dual-diameter TiO2 nanotubes with the inner layers of compact and fluorine-free oxide tightly bonding to Ti, were formed by voltage-increased anodization F- sedimentation procedure. The closely aligned structured upper 35 70 nm diametric tubes as nanocaps, respectively, underlying 140 nanoreservoirs. Followed loading ponericin G1 (a kind peptide (AMP)) into vacuum-assisted physisorption,...
A series of naphthyridinol analogs α-tocopherol (α-TOH, right) with varying sidechain substitution was synthesized to determine how systematic changes in the lipophilicity these potent antioxidants impact their radical-trapping activities lipid bilayers, regenerability by water-soluble reductants, and binding human tocopherol transport protein (TTP). The naphthyridinols were assayed phosphatidylcholine unilamellar liposomes using a recently developed high-throughput assay that employs boron...
Cardiac fibrosis, as a pathological process, plays an important role in various cardiac diseases. microRNA-155 (miR-155) is one of the most miRNAs, and previous studies have shown that it regulatory factor fibrotic However, mechanism by which miR-155 affects myocardial fibrosis remains unclear. In this study, we aim to establish biological function induced diabetes mice. We used normal C57BL/6 wild type (WT) knockout (KO) mice diabetic model intraperitoneal injection streptozotocin, utilized...
Abstract Structural analysis of a co‐crystal helically‐folded peptide‐foldamer hybrid in complex with hDM2 E3 ubiquitin ligase, revealed unique orientation for the C ‐terminal proline pyrrolidine ring pointing backwards sequence, and suggested new opportunities macrocyclization. In particular, we found that prolyl residue could be replaced by its (2 S ,4 )‐4‐mercaptoprolyl analogue optimal bisthioether crosslinking cysteine installed at position 4 sequence. The resulting i , +7 stapled is...
Objective: To investigate whether the histone deacetylase (HDAC) activator ITSA‐1 can ameliorate systemic inflammation after cardiac arrest (CA), thereby enhancing function and neurological outcomes in rats. Materials Methods: Sixty‐nine healthy adult male Wistar rats were subjected to 12 min of CA induced by Vecuronium bromide. The randomly assigned five groups: normal control, sham operation, suberoylanilide hydroxamic acid (SAHA), ITSA‐1. study evaluated effects on function, survival,...
Fluid shear stress (FSS) is an important biomechanical factor regulating the osteogenic differentiation of human mesenchymal stem cells (hMSCs) and therefore widely used in bone tissue engineering. However, mechanotransduction FSS hMSCs remains largely unknown. As β1 integrins are considered to be mechanoreceptors other cells, we suspect that should also for sense stimulation FSS. We a perfusion culture system produce loading on seeded PLGA three-dimensional (3D) scaffolds investigated roles...
Human malignant glioblastoma (GBM) is a highly invasive and lethal brain tumor. Targeting of integrin downstream signaling mediators in GBM such as focal adhesion kinase (FAK) seems reasonable recently demonstrated promising results early clinical studies. Herein, we report the structure-guided development series covalent inhibitors FAK. These new compounds displayed potent inhibitory potency against FAK enzymatic activity with IC50 values nanomolar range. Several retarded tumor cell growth...
Copper is an essential mineral and plays important roles in skin growth activity. delivery through can provide beneficial effects but its potential to induce irritation reactions often overlooked. Data on dermal toxicity caused by copper compounds scant. Some recognized vitro methods are unsuitable for all metal compounds. Here, we employ a keratinocyte-based model evaluated the of at cellular, genomic proteomic levels. We determined cell viability cytotoxicity using tetrazolium reduction...
Focal Adhesion Kinase signaling pathway and its functions have been involved in the development aggressiveness of tumor malignancy, it then presents a promising cancer therapeutic target. Several reversible FAK inhibitors developed are being conducted clinical trials. On other hand, irreversible covalent would bring many desirable pharmacological features including high potency increased duration action. Herein we report structure-guided first highly potent inhibitor kinase. This showed very...
Currently available data indicate the potential application of rapamycin and its analogues in clinic as anticancer therapeutic agents through inhibiting tumor cell growth angiogenesis. However, whether can directly suppress metastasis remains unclear. In present study, we demonstrated that treatment results reduced formation metastatic nodules lung by B16 cells. This is due to two mechanisms. First, expression alphav integrin down-regulated treatment, subsequently, phosphorylation focal...
Salinomycin diastereoisomers and their benzoylated derivatives were synthesized evaluated for both antiproliferative activity neurotoxicity in vitro. The results indicated that the stereoscopic configurations of spiro C17 C21 atoms as well benzoyl groups O-20 on rigid B/C/D spiro-ketal structures are crucial biological neural toxicity. In general, there some positive correlations between these salinomycin derivatives, indicating possibly similar mechanisms action.
Surgical intervention is the main treatment for a ruptured congenital sinus of Valsalva aneurysm (SVA). However, reports on surgical experience are scarce. We retrospectively analysed cases our centre to summarize 10-year experience.A total 286 patients who were diagnosed with SVA and underwent repair between 2007 2016 identified analysis. Follow-up data (mean ± standard deviation: 49.6 34.9 months) obtained from outpatient department records telephone calls.The SVAs originated right...
Construction of non-aromatic 1,2,3,6-tetrahydro-1,2,3,4-tetrazines through [4 + 2] cycloaddition α-halogeno hydrazones with azodicarboxylic acid derivatives.
The HK-2 cell model based on clusterin, osteopontin, CysC and KIM-1 would allow the prediction of nephrotoxicity at early stages.
In forensic toxicology, hair has become a hot biological material for drug testing due to its wider detection window and noninvasive sampling process compared traditional liquid materials (e.g., blood urine). However, as matrix differs from body fluids, it is not easily aliquoted analysis. Nevertheless, pretreatment methods have gradually improved the first chemical methods, such alkali digestion acid hydrolysis, now include physical method of pulverization further improvements beyond...