A5013456838- Cholinesterase and Neurodegenerative Diseases
- Pharmacological Receptor Mechanisms and Effects
- Receptor Mechanisms and Signaling
- Neuropeptides and Animal Physiology
- Computational Drug Discovery Methods
- Psoriasis: Treatment and Pathogenesis
- Synthesis and biological activity
- Pharmacological Effects of Natural Compounds
- Alzheimer's disease research and treatments
- Adenosine and Purinergic Signaling
- Catalytic C–H Functionalization Methods
- Block Copolymer Self-Assembly
- IL-33, ST2, and ILC Pathways
- Phenothiazines and Benzothiazines Synthesis and Activities
- Advanced Polymer Synthesis and Characterization
- Protein Degradation and Inhibitors
- Polymer Surface Interaction Studies
- Asthma and respiratory diseases
- Cytokine Signaling Pathways and Interactions
- Immune Cell Function and Interaction
- Quinazolinone synthesis and applications
- Catalytic Cross-Coupling Reactions
- Digital Media and Visual Art
- Synthesis and Biological Evaluation
- Molecular Biology Techniques and Applications
Fudan University
2016-2025
Zhejiang Chinese Medical University
2022-2025
Zhoushan Hospital
2022-2025
China Astronaut Research and Training Center
2017-2024
Secretaria de Salud
2024
Second Affiliated Hospital of Nanchang University
2023
Nanchang University
2023
Hunan Normal University
2022
Dongguan People’s Hospital
2020
Yangtze University
2017
Mitochondrial dysfunction in neurons has recently become a promising therapeutic target for Alzheimer’s disease (AD). Regulation of dysfunctional mitochondria through multiple pathways rather than antioxidation monotherapy indicates synergistic effects. Therefore, we developed multifunctional hybrid peptide HNSS composed antioxidant SS31 and neuroprotective S14G-Humanin. However, suitable delivery systems with excellent loading capacity effective at-site are still absent. Herein, the...
Bis-(−)-nor-meptazinols (bis-(−)-nor-MEPs) 5 were designed and synthesized by connecting two (−)-nor-MEP monomers with alkylene linkers of different lengths via the secondary amino groups. Their acetylcholinesterase (AChE) inhibitory activities more greatly influenced length chain than butyrylcholinesterase (BChE) inhibition. The most potent nonamethylene-tethered dimer 5h exhibited low-nanomolar IC50 values for both ChEs, having a 10 000-fold 1500-fold increase in inhibition AChE BChE...
Although the double-gyroid (DG) structure has been commonly formed from self-assembly of block copolymers, single-gyroid (SG) is rarely reported. Moreover, SG even shows better performance than DG in some optical applications. How to prepare become an attractive but challenging topic. We speculate that can be stabilized by synergistic effect released packing frustration and stretched bridging AB-type copolymers. Accordingly, we propose minimum conditions for design architecture enables two...
The overall response rate to checkpoint blockade remains unsatisfactory, partially due the immune-suppressive tumor microenvironment. A retinoic acid-related orphan receptor γt (RORγt) agonist (LYC-55716) is currently used in clinical trials combined with anti-PD-1, but how Th17 cell transcription factor RORγt enhances antitumor immunity of PD-1 microenvironment elusive.The expression mRNA was analyzed using qPCR assays. Flow cytometry sort and profile cells. Cell migration Transwell Biacore...
Abstract Osteosarcoma (OS) is the most frequent primary malignant bone tumor in adolescents and young adults. Despite advances therapy, OS remains an ominous problem because of its high metastatic potential, resistance to standard great physical, psychological, financial burden on patients. Available treatment options like surgery high-dose chemotherapy are limited by chemotoxicity, multimed resistance, adverse effects quality life Extrapolated from wide array vitro vivo studies, application...
A rapid microwave-assisted approach for the synthesis of phenanthridine derivatives from radical insertion/cyclization reaction biphenyl isocyanides with a C(sp(3))-H bond adjacent to heteroatom has been developed. The protocol achieves wide substrate scope and good excellent yields. kinetic isotope effect (KIE) studies, inhibition Hammett plot analysis clearly disclose that current supports mechanism.
Recent studies and clinical evidence have strongly supported the development of adenosine A2A receptor (A2AR) antagonists as novel approaches for cancer immunotherapy. By screening our in-house compound library, a pyridinone hit (1) with weak A2AR antagonistic activity was identified. Further structure–activity relationship revealed series derivatives strong potency. Compound 38 stood out potent (IC50 = 29.0 nM), good mouse liver microsomal metabolic stability (t1/2 86.1 min), excellent oral...
The self-assembly of amphiphilic macromolecules into various mesocrystals has attracted abiding interest. Although many interesting have been achieved, a low coordination number (CN) such as simple cubic are rarely reported. Here we purposely design an AB-type multiblock copolymer to target exotic spherical phases CNs. Self-consistent field theory reveals that two sophisticated mechanisms realized in the copolymer, is, stretched bridging block and released packing frustration,...
We propose to regulate the stability of gyroids ABC-type multiblock copolymers by controlling packing frustration majority-component B-blocks. Accordingly, we investigate self-assembly behaviors BABCB linear terpolymer with a variable length ratio τ middle B-block relative total B-blocks using self-consistent field theory. It is observed that gyroid region exhibits maximal width respect τ, which attributed nonmonotonical change three in morphology discrete domains, for example, cylinders....
In recent years, the adenosine A2A receptor (A2AR) has shown exciting progress in development of immunotherapies for treatment cancer. Herein, a 2-amino-7,9-dihydro-8H-purin-8-one compound (1) was identified as an A2AR antagonist hit through in-house library screening. Extensive structure–activity relationship (SAR) studies led to discovery 2-aminopteridin-7(8H)-one derivatives, which showed high potencies on cAMP assay. Compound 57 stood out with IC50 value 8.3 ± 0.4 nM against at...
Drug repurposing has become an alternative therapeutic strategy for cancer treatment given the known pharmacokinetics and toxicity. The inhibitory effects of artesunate have been reported in various cancers. In this work, we investigated nasopharyngeal carcinoma (NPC). We demonstrate that significantly inhibits proliferation via arresting NPC cells at G2/M phase. It also induces apoptosis through caspase-dependent mitochondria-independent pathways multiple cell lines. combination cisplatin...
Located on chromosome 11q13.4, miR-139-5p has been confirmed by several studies as a possible attractive biomarker for cancer, including breast but its mechanism of correlation in different molecular subtypes cancer not reported. In this study, comprehensive bioinformatics analysis was used to evaluate the expression (luminal A, luminal B, HER2-enriched, and basal-like). The target genes were predicted using an online database TargetScan miRDB, three key genes, FBN2, MEX3A, TPD52, screened...
Research into kappa opioid receptor (KOR) agonists with attenuated central-nervous-system side effects is a critical focus for developing productive and safe analgesics. Herein, series of ortho-substituted N-cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaines were designed, synthesized, subjected to bioassays. Compound 7a exhibited high subtype selectivity potent agonistic activity toward KOR (KOR, Ki = 3.9 nM, MOR/KOR 270, DOR/KOR 1075; [35S]GTPγS binding, EC50 3.4 nM)....