A5101858608- Biochemical and Molecular Research
- Myeloproliferative Neoplasms: Diagnosis and Treatment
- SARS-CoV-2 and COVID-19 Research
- Cytokine Signaling Pathways and Interactions
- Kruppel-like factors research
- Hepatitis C virus research
- Adenosine and Purinergic Signaling
- Cancer-related gene regulation
- Optical Imaging and Spectroscopy Techniques
- Synthesis and Biological Evaluation
- Customer Service Quality and Loyalty
- IL-33, ST2, and ILC Pathways
- Lung Cancer Treatments and Mutations
- Infectious Encephalopathies and Encephalitis
- Stellar, planetary, and galactic studies
- Plasma Applications and Diagnostics
- Neuroscience and Neuropharmacology Research
- Inflammatory Myopathies and Dermatomyositis
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- E-commerce and Technology Innovations
- Optical and Acousto-Optic Technologies
- Public Policy and Administration Research
- Customer churn and segmentation
- Ginger and Zingiberaceae research
- Photoacoustic and Ultrasonic Imaging
East China University of Science and Technology
2019-2025
First Affiliated Hospital of Henan University
2024-2025
Puyang Vocational and Technical College
2024
China Tobacco Guangxi Industrial (China)
2024
Zhengzhou University
2018-2022
Chinese Academy of Medical Sciences & Peking Union Medical College
2022
China-Japan Friendship Hospital
2022
Capital Medical University
2022
China Pharmaceutical University
2022
Taizhou Second People's Hospital
2021
Abstract Emerging and re-emerging RNA viruses occasionally cause epidemics pandemics worldwide, such as the on-going outbreak of novel coronavirus SARS-CoV-2. Herein, we identified two potent inhibitors human DHODH, S312 S416, with favorable drug-likeness pharmacokinetic profiles, which all showed broad-spectrum antiviral effects against various viruses, including influenza A virus, Zika Ebola particularly Notably, S416 is reported to be most inhibitor so far an EC 50 17 nmol/L SI value...
A novel series of peptidomimetic aldehydes was designed and synthesized to target 3C protease (3Cpro) enterovirus 71 (EV71). Most the compounds exhibited high antiviral activity, among them, compound 18p demonstrated potent enzyme inhibitory activity broad-spectrum on a panel enteroviruses rhinoviruses. The crystal structure EV71 3Cpro in complex with determined at resolution 1.2 Å revealed that covalently linked catalytic Cys147 an aldehyde group. In addition, these also good against 3CLpro...
The accurate prediction of binding free energy is a major challenge in structure-based drug design. Quantum mechanics (QM)-based approaches show promising potential predicting ligand–protein affinity by accurately describing the behavior and structure electrons. However, traditional QM calculations face computational limitations, hindering their practical application Nevertheless, fragment molecular orbital (FMO) method has gained widespread design due to its ability reduce costs achieve...
In this paper, we describe the discovery and optimization of a series noncovalent reversible epidermal growth factor receptor inhibitors EGFRL858R/T790M/C797S. One most promising compounds, 25g, inhibited enzymatic activity EGFRL858R/T790M/C797S with an IC50 value 2.2 nM. Cell proliferation assays showed that 25g effectively selectively EGFRL858R/T790M/C797S-dependent cells. This which occupy both ATP binding site allosteric EGFR kinase, may serve as basis for development fourth-generation...
Hepatocellular carcinoma (HCC) is one of the most fatal cancers worldwide. In this article, we show that expression abnormal spindle‐like microcephaly‐associated protein (ASPM) up‐regulated in liver cancer samples, and up‐regulation significantly associated with tumor aggressiveness reduced survival times patients. Down‐regulation ASPM inhibits proliferation, invasion, migration epithelial‐to‐mesenchymal transition HCC cells vitro formation nude mice. interacts disheveled‐2 (Dvl2)...
Knowledge of the role CYP2E1 in hepatocarcinogenesis is largely based on epidemiological and animal studies, with a primary focus metabolic activation procarcinogens. Few studies have directly assessed effects HCC malignant phenotypes.The expression tissues was determined by qRT-PCR, western blotting immunohistochemistry. Overexpression cell achieved lentivirus transfection. The function were detected CCK-8, wound healing, transwell assays, xenograft models pulmonary metastasis model....
Abstract Emerging and re-emerging RNA viruses occasionally cause epidemics pandemics worldwide, such as the on-going outbreak of coronavirus SARS-CoV-2. Existing direct-acting antiviral (DAA) drugs cannot be applied immediately to new because virus-specificity, development DAA from beginning is not timely for outbreaks. Thus, host-targeting (HTA) have many advantages fight against a broad spectrum viruses, by blocking viral replication overcoming potential mutagenesis simultaneously. Herein,...
COVID-19, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is still an emergent pandemic for humans. The virus infection achieved penetrating its spike protein to host cells via binding with ACE2. Moreover, recent studies show that SARS-CoV-2 may have multiple receptors need be further revealed. shares similar sequences of the Middle East Respiratory Syndrome Coronavirus (MERS-CoV), which can invade either DPP4 or sialic acids. Sialic acids linked terminal...
Ethnopharmacological relevance: The herb Abutilon theophrasti Medic. (AT, Qingma in Chinese), a widely distributed medicinal plant various regions worldwide, is commonly used China for treating inflammatory diseases the gastrointestinal (GI) tract such as dysentery. However, pharmacological basis of this peptic ulcer, also an condition GI tract, remains insufficiently understood. Aim study: To investigate ameliorating effects and mechanism action standardized aqueous extract AT (ATAE) on...
Abstract The SARS‐CoV‐2 spike (S) protein, a trimeric structure comprising three receptor binding domains (RBDs) and N‐terminal (NTDs), undergoes substantial conformational changes to fusion‐prone open state for angiotensin‐converting enzyme 2 (ACE2) host cell infection. Stabilizing its closed is key antiviral strategy but remains challenging. Here, we introduce S416, novel amphipathic molecule acting as “molecular bolt”. Cryo‐EM study reveals that S416 binds concurrently six sites across...
High extracellular concentrations of adenosine triphosphate (ATP) in the tumor microenvironment generate by sequential dephosphorylation CD39 and CD73, resulting potent immunosuppression to inhibit T cell natural killer (NK) function. as determining enzyme for production, has been shown correlate with poor clinical prognosis. Conventional inhibitors analogues 5′-monophosphate (AMP) may have a risk further metabolism analogues. Here, we report new series malonic acid non-nucleoside...
Poor medication adherence is one of the leading causes suboptimal glycaemic control in approximately half patients with type 2 diabetes mellitus (T2DM). Long-acting antidiabetic drugs are clinically needed for improving patients' compliance. Dipeptidyl peptidase-4 (DPP-4) inhibitors play an increasingly important role treatment T2DM because their favorable properties weight neutrality and hypoglycemia avoidance. Herein, we report successful discovery scale-up synthesis compound 5, a...
Human dihydroorotate dehydrogenase (DHODH) is a viable target for the development of therapeutics to treat cancer and immunological diseases, such as rheumatoid arthritis (RA), psoriasis multiple sclerosis (MS). Herein, series acrylamide-based novel DHODH inhibitors potential RA treatment agents were designed synthesized. 2-Acrylamidobenzoic acid analog 11 was identified lead compound structure–activity relationship (SAR) studies. The replacement phenyl group with naphthyl moieties improved...
Objective Interstitial lung diseases (ILDs) secondary to anti-synthetase syndrome (ASS) greatly influence the prognoses of patients with ASS. Here we aimed investigate peripheral immune responses understand pathogenesis this condition. Methods We performed single-cell RNA sequencing (scRNA-seq) blood mononuclear cells (PBMCs) from 5 ASS-ILD and 3 healthy donors (HDs). Flow cytometry PBMCs was replenish results scRNA-seq. Results used scRNA-seq depict a high-resolution visualization cellular...
Muscone is the main active compound of Moschus. In this paper, cardioprotective effect on acute myocardial ischemia (AMI) rats and its potential mechanisms were investigated. AMI rat models established to evaluate protective antioxidative function hearts. Moreover, Western blot analysis was conducted quantify phosphorylated PI3K AKT levels in PI3K/Akt pathway for further investigating mechanism Muscone. Results showed that could markedly lessen infarct size injury, improve cardiac function,...
Porous chitosan microspheres with diameters ranging from 180 μm to 280 were successfully prepared, using an anti-phase suspension method combined temperature controlled freeze-extraction. The mean pore diameter could be regulated 5 60 by varying the freezing through cooling rate. Results in vitro chondrocyte cultures showed that cells attach, proliferate, and spread on these porous as well inside microcarriers. materials cell co-cultures characterized both optical scanning electron...