A5100631758- Hepatitis B Virus Studies
- Hepatitis C virus research
- Polyoxometalates: Synthesis and Applications
- Histone Deacetylase Inhibitors Research
- Synthesis and Catalytic Reactions
- Chemical Synthesis and Reactions
- Chemical Synthesis and Analysis
- HIV/AIDS drug development and treatment
- Click Chemistry and Applications
- Respiratory viral infections research
- Immunotherapy and Immune Responses
- Electrochemical sensors and biosensors
- Epigenetics and DNA Methylation
- Synthesis and Reactions of Organic Compounds
- Advanced Nanomaterials in Catalysis
- Fluorine in Organic Chemistry
- Oxidative Organic Chemistry Reactions
- Cell death mechanisms and regulation
- Bioactive Compounds and Antitumor Agents
- Liver Disease Diagnosis and Treatment
- Sulfur-Based Synthesis Techniques
- Protein Degradation and Inhibitors
- Endoplasmic Reticulum Stress and Disease
- Ubiquitin and proteasome pathways
- Axon Guidance and Neuronal Signaling
Roche (China)
2016-2025
Northwestern University
2025
Institute of Medicinal Plant Development
2025
Xiangya Hospital Central South University
2018-2024
Central South University
2018-2024
Southern Medical University
2019-2023
Nanfang Hospital
2019-2023
Jiangsu Province Hospital
2023
Nanjing Medical University
2023
Harbin University of Science and Technology
2013-2021
Abstract The biological role of miR-500a-5p has not yet been reported in the context colorectal cancer (CRC). Here, we show that expression is decreased CRC tissues compared with adjacent normal tissues. Low associated malignant progression. Moreover, transfection cells induces G0/G1 cell cycle arrest and inhibits their growth migration. Mechanistically, directly targets HDAC2 HDAC2-mediated proliferation nude mice. Furthermore, YY1 binds to promoter negatively regulates its transcription....
Palivizumab is a US Food and Drug Administration-approved monoclonal antibody for the prevention of respiratory syncytial virus (RSV) lower disease in high-risk infants. Motavizumab, derived from palivizumab with enhanced antiviral activity, has recently been tested humans. Although escape mutants have generated laboratory, development resistant RSV patients receiving not reported previously.
New processes that can selectively prepare α-mono or α,α-dichloro ketones and β-ketoesters using 1,3-dichloro-5,5-dimethylhydantoin (DCDMH) are reported. Using silica gel as the catalyst methanol solvent heating for 1 h under reflux, α-monochlorinated products were obtained in 86–98% yield. However a deep eutectic (choline chloride: p-TsOH = 1:1) stirring 45 min at room temperature, α,α-dichlorinated 86–95%
Targeting the capsid protein of hepatitis B virus (HBV) and thus interrupting normal formation have been an attractive approach to block replication HBV viruses. We carried out multidimensional structural optimizations based on heteroaryldihydropyrimidine (HAP) analogue Bay41-4109 (1) identified a novel series inhibitors that demonstrated promising cellular selectivity indexes, metabolic stabilities, in vitro safety profiles. Herein we disclose design, synthesis, structure-activity...
Abstract RACK1 is upregulated in the various types of human cancers, and considered to play a role development progression cancer. However, mechanism RACK colon cancer are poorly understood. In this study, we detected expression 63 normal colonic mucosa, 60 inflammatory polyps, adenomas, 180 adenocarcinomas, 40 lymph node metastases by immunohistochemistry, observed that was progressively elevated carcinogenic process epithelium, expressional levels were positively correlated with malignant...
Abstract T cell senescence and exhaustion are major barriers to successful cancer immunotherapy. Here we show that miR-155 increases CD8 + antitumor function by restraining functional through epigenetic silencing of drivers terminal differentiation. enhances Polycomb repressor complex 2 (PRC2) activity indirectly promoting the expression PRC2-associated factor Phf19 downregulation Akt inhibitor, Ship1. orchestrates a transcriptional program extensively shared with restrain sustain responses....
The rise of multidrug resistant (MDR) Gram-negative (GN) pathogens and the decline available antibiotics that can effectively treat these severe infections are a major threat to modern medicine. Developing novel against MDR GN is particularly difficult as compounds have permeate double membrane, which has very different physicochemical properties, circumvent plethora resistance mechanisms such multiple efflux pumps target modifications. bacterial type II topoisomerases DNA gyrase (GyrA2B2)...
Described herein is the first-time disclosure of Linvencorvir (RG7907), a clinical compound and hepatitis B virus (HBV) core protein allosteric modulator, for treatment chronic HBV infection. Built upon structure hetero aryl dihydropyrimidine, RG7907 was rationally designed by combining all drug-like features low CYP3A4 induction, potent anti-HBV activity, high metabolic stability, hERG liability, favorable animal pharmacokinetic (PK) profiles. In particular, chemistry strategy to mitigate...
Specific mutations in respiratory syncytial virus (RSV) fusion protein can cause palivizumab resistance. We assessed the incidence of sequence polymorphisms and resistance clinical RSV isolates collected from immunoprophylaxis-naive subjects. Polymorphisms were identified at low frequency, only polymorphic antigenic site A (<1% all polymorphisms) conferred
Described herein are the discovery and structure–activity relationship (SAR) studies of third-generation 4-H heteroaryldihydropyrimidines (4-H HAPs) featuring introduction a C6 carboxyl group as novel HBV capsid inhibitors. This new series HAPs showed improved anti-HBV activity better drug-like properties compared to first- second-generation HAPs. X-ray crystallographic study analogue 12 (HAP_R01) with Cp149 Y132A mutant hexamer clearly elucidated role played for increased binding affinity,...
Abstract Overexpression of ANXA1 and EphA2 has been linked to various cancers both proteins have attracted considerable attention for the development new anticancer drugs. Here we report that competes with Cbl binding increases its stability by inhibiting Cbl-mediated ubiquitination degradation in nasopharyngeal carcinoma (NPC). Binding promoted NPC cell growth metastasis vitro vivo elevating levels increasing activity oncogenic signaling (pS897-EphA2). Expression was positively correlated...
Histone deacetylase 6 (HDAC6) removes the acetyl group from lysine residues in a number of non-histone substrates and plays important roles microtubule dynamics chaperone activities. There is growing interest identifying HDAC6-selective inhibitors as chemical biology tools ultimately new therapeutic agents. Herein we report design, synthesis, phenotypic screening novel class 3-aminopyrrolidinone-based hydroxamic acids HDAC6 inhibitors. In particular, α-methyl-substituted enantiomer 33 (3-S)...
A unique hybrid compound with dimeric monocopper-substituted Keggin polyoxoanions as ten-connected linkages, [Cu5(en)9][(PW11CuO39)2]·18H2O (1) (en = ethylenediamine), has been synthesized and characterized by elemental analysis, IR, TG powder X-ray diffraction single-crystal diffraction. In 1, each [PW11CuO39]210− cluster an unusual deca-dentate connector links ten [Cu(en)2]2+ complexes to form a three-dimensional (3D) framework (44·832·129) topology. The successful synthesis of 1 provides...
Abstract HDAC7 plays a crucial role in cancers, and is the main drug target of several HDAC inhibitors. However, mechanism nasopharyngeal carcinoma (NPC) are still unclear. In this study, we observed that was significantly upregulated NPC tissues relative to normal mucosa (NNM) tissues, expression levels were positively correlated with progression negatively patient prognosis, knockdown dramatically inhibited vitro proliferation, migration, invasion cells, growth xenografts mice, indicating...
Protein aggregation is a hallmark of neurodegenerative diseases, which connects these neuropathologies by common phenotype. Various proteins and peptides form aggregates that are poorly degraded, their ensuing pathological accumulation underlies diseases. Similarities may exist in the mechanisms responsible for buildup aggregates. Therefore, therapeutics designed to treat one disease be beneficial others. In ALS models, compound NU-9 was previously shown block neurodegeneration produced...
PKMYT1 is a crucial regulator of the cell cycle, particularly involved in G2/M transition through inhibitory phosphorylation CDK1, and promising therapeutic target for cancer therapy. Data mining Roche kinome screen database identified hit characterized by 100% activity at 10 μM concentration, which was further validated with enzymatic assay showing double-digit nanomolar potency. The featured quinolinone central core phenol headgroup. replacement problematic headgroup an indazole moiety...
Abstract EphA2 is an important oncogenic protein and emerging drug target, but the role mechanism of ligand-independent phosphorylation at tyrosine 772 (pY772-EphA2) unclear. In this study, we established nasopharyngeal carcinoma (NPC) cell lines with stable expression exogenous EphA2-Y772A (phosphorylation inactivation) using endogenous EphA2-knockdown cells, observed that pY772A was responsible for EphA2-promoting NPC proliferation anchorage-independent in vivo growth mice....
Background Chemotherapy is one of the primary treatments for ovarian cancer patients. Autophagy has been linked to chemotherapy resistance in tumor cells. Recent studies have suggested that fibroblast growth factor 19 (FGF19) may be involved onset and progression malignancies. However, relationship between FGF19 autophagy still unknown. Methods Next-generation sequencing (NGS) was conducted analyze gene mutation profiles 62 cases high grade serous (HGSOC). Fluorescence situ hybridization...