A5102027936- Catalytic C–H Functionalization Methods
- Synthesis and Reactivity of Heterocycles
- Axial and Atropisomeric Chirality Synthesis
- Synthesis and Biological Evaluation
- Catalytic Cross-Coupling Reactions
- Antibiotic Resistance in Bacteria
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- RNA modifications and cancer
- Cyclopropane Reaction Mechanisms
- RNA Research and Splicing
- Synthesis and biological activity
- Multicomponent Synthesis of Heterocycles
- Circular RNAs in diseases
- Molecular spectroscopy and chirality
- interferon and immune responses
- Adipose Tissue and Metabolism
- Pancreatic function and diabetes
- Pharmacological Effects of Natural Compounds
- Photoreceptor and optogenetics research
- Plant Physiology and Cultivation Studies
- Synthesis and Catalytic Reactions
- Spectroscopy and Chemometric Analyses
- Parkinson's Disease Mechanisms and Treatments
- Spectroscopy Techniques in Biomedical and Chemical Research
Chinese Academy of Sciences
2014-2025
Shanghai Institute of Materia Medica
2012-2025
Chinese Academy of Medical Sciences & Peking Union Medical College
2025
Guangzhou Institutes of Biomedicine and Health
2020-2024
State Key Laboratory of Respiratory Disease
2020-2024
University of Chinese Academy of Sciences
2020-2024
Zhejiang University
2023
Wuhan University
2020-2023
Renmin Hospital of Wuhan University
2020-2023
Second Affiliated Hospital of Zhejiang University
2023
Ubiquitin-specific protease 1 (USP1), a well-known member of the deubiquitinating enzymes, serves as key regulator in DNA damage repair (DDR) processes. Herein, we utilized ring-opening and cyclization strategies based on KSQ-4279 to design novel series USP1 inhibitors featuring morpholine scaffold. Notably, compound 38-P2 exhibited more potent enzymatic cellular inhibition activity compared KSQ-4279. Mechanistically, was characterized selective, reversible, noncompetitive inhibitor....
Trichomes originate from the epidermal cells of nearly all terrestrial plants, which are specialized unicellular or multicellular structures. Although molecular mechanism regulating trichome formation has been extensively characterized, most genes essential for remain unknown. In this study, we identified an associated locus on long arm chromosome 10 using a genome-wide association study (GWAS) type-I trichomes 180 diverse Solanum lycopersicum (tomato) accessions. Using map-based cloning...
Parkinson's disease (PD) is the second most common neurodegenerative disease. Pathologically, PD characterized by formation of Lewy bodies (LBs) in brain, which mainly comprises phosphorylated and aggregated α-synuclein (α-syn). The aberrant aggregation α-syn believed to play a key role pathogenesis PD. While expression can be reduced antisense oligonucleotides (ASOs), challenge deliver ASOs safely effectively into neurons remains unresolved. Here, we developed safe highly effective ASO...
Enantioselective 7-exo-trig cyclocarbopalladation-initiated carbonylation cascade reactions, leading to seven-membered dibenzo[b,d]azepin-6-ones containing a thermodynamically controlled stereogenic axis, have been realized for the first time. A series of 7-acetate- or 7-acetamide-substituted are obtained under atmospheric pressure CO in good yields with excellent diastereo- and enantioselectivities. The calculated energy difference between diastereoisomers generated from biaryl axis center...
Follicle-stimulating hormone (FSH) is involved in mammalian reproduction via binding to FSH receptor (FSHR). However, several studies have found that and FSHR play important roles extragonadal tissue. Here, we identified the expression of human mouse pancreatic islet β-cells. Blocking signaling by Fshr knock-out led impaired glucose tolerance owing decreased insulin secretion, while high levels caused insufficient secretion as well. In vitro, orchestrated glucose-stimulated (GSIS) a bell...
Significance The signaling mechanisms mediating glutamatergic synapse assembly are fundamental to our understanding of neural circuit function, plasticity, and disorders, but have remained elusive. We provide direct evidence that two components the conserved planar cell polarity pathway, which assembles asymmetric cell–cell junctions, opposing functions in formation. Celsr3 promotes whereas Vangl2 inhibits assembly, suggesting this mechanism is accessible for both positive negative...
The tumor microenvironment is comprised of cancer cells and various stromal their respective cellular components. Cancer-associated fibroblasts (CAFs), a major part the cells, are key determinant in progression, while glucose-regulated protein (GRP)78 overexpressed many human cancers involved invasion metastasis. This study developed microfluidic-based three dimension (3D) co-culture device to mimic an vitro order investigate cell real-time. bionic chip provided significant information...
A palladium-catalyzed imidoylative cycloamidation of N-alkyl-2-isocyanobenzamides with 2,6-disubstituted aryl iodides, affording unprecedented axially chiral 2-arylquinazolinones, has been developed good yields and atroposelectivities. In this coupling–cyclization process, the biaryl linkage heteroaromatic ring are formed sequentially in one step. When N-(2,4-dimethoxyphenyl)-2-isocyanobenzamide is applied as a substrate, 2,3-diarylquinazolinones containing two stereogenic axes produced...
Enantioenriched pyrido[6]helicenes and furan-containing pyrido[7]helicenes have been synthesized through palladium-catalyzed double imidoylative cyclization by applying axially achiral multiaryl bisisocyanides aryl iodides as coupling components. Two pyridyl rings were constructed sequentially forming four C–C bonds in one pot with low catalyst loading. A control study using precyclized biaryl monoisocyanides revealed the second pyridine-forming enantiomer-generating step, which also enabled...
Taxol is a cytotoxic antiepithelioma chemotherapy drug widely used clinically, which results in appearing broad range of taxol-resistant tumors. Oncoprotein 18 (Op18)/stathmin genetically highly conserved small-molecule cytosolic phosphoprotein and expressed Extracellular signal-regulated kinase (ERK) main member mitogen-activated protein kinases (MAPKs). The study demonstrated that combination blockage ERK signal by inhibitor PD98059 greatly promoted taxol-induced cellular apoptosis growth...
The molecular characterization of carbapenem-resistant hypervirulent Klebsiella pneumoniae (CR-hvKP) isolates is not well studied. Our goal was to investigate the epidemiology CR-hvKP strains that were isolated from a Chinese hospital.All clinical K. (CR-KP) collected and identified patient samples between 2014 2017 hospital. subjected screening for by string test detection aerobactin gene. further confirmed through neutrophil phagocytosis mice lethality assay. investigated their capsular...
Abstract Sulfiredoxin 1 (SRXN1) is a pivotal regulator of the antioxidant response in eukaryotic cells. However, role SRXN1 hepatocellular carcinoma (HCC) far from clear. The present study aims to elucidate whether participates tumorigenesis and metastasis HCC determine molecular mechanisms. We found that expression was up‐regulated tissue samples correlated with poor prognosis patients. also observed knockdown by transient siRNA transfection inhibited cell proliferation, migration invasion....
Enantioenriched 2-azabicyclo[3.1.0]hexanes are accessed from readily available allyl substituted α-isocyanoesters by intramolecular (1 + 2) cycloaddition with the olefinic moiety and isocyano carbon as respective C2 C1 units. Cyclopropanation is initiated 1,1-hydrocupration of isocyanide followed formimidoylcopper to copper α-aminocarbenoid equilibration subsequent cycloaddition. The unprecedented copper/chiral phosphoric acid (CPA) catalytic system can be operated in presence water under...
A 1,2-difunctionalization of an unactivated alkene, imidoyl-carbamoylation, has been developed through a palladium-catalyzed four-component cascade reaction involving aryl iodide, alkenyl isocyanide, CO, and amine. Continuous migratory insertion three different functionalities to the Pd(II) intermediate generated from previous step takes place in well-defined sequence. Four chemical bonds, including C–C bonds one C–N bond, are formed this process, leading convenient convergent access...
The relevance of microRNA-15a (miR-15a) to autoimmunity has been reported. Herein, we intended probe the potential roles miR-15a shuttled by adipose-derived mesenchymal stem cells (adMSCs)-derived extracellular vesicles (Evs) in colorectal cancer (CRC). Initially, CRC were treated with interferon gamma (IFN-γ) screen out differentially expressed genes transcriptome sequencing. Following a 24-h co-culture 20 μM adMSCs-derived Evs, cell viability, migration, invasion, and apoptosis assessed....
An unprecedented tandem carbonylation/aminocarbonylation triggered by palladium-catalyzed enantioselective Heck-type exocyclopalladation delivering chiral heterocyclic α-ketoamides has been developed.
Obesity and type 2 diabetes (T2D) are the leading causes of progressive decline in muscle regeneration fitness adults. The microenvironment is known to play a key role controlling stem cell regenerative capacity, yet underlying mechanism remains elusive. Here, we found that Baf60c expression skeletal significantly downregulated obese T2D mice humans. Myofiber-specific ablation impairs contraction, accompanied by robust upregulation Dkk3, muscle-enriched secreted protein. Dkk3 inhibits...
A catalytic-condition-controlled synthesis strategy was reported to build quinolizinone and indolizine derivatives from the easily available enamide triazole substrates with high regioselectivity good functional group tolerance. More especially, this transformation has successfully fulfilled a C–H bond activation of terminal olefin enamides followed by [3 + 3] [2 cyclization cascade under different catalytic conditions, respectively, provide two kinds potentially biologically active...
Impact statement We have developed a manually curated online reference database, DANMEL ( http://124.239.252.254/danmel/ ), that addresses the lack of accurate dissection and annotation genetic structures mobile elements (MGEs) with genes for drug resistance. contains accurately annotated genetically dissected MGEs covering 5 categories 135 subcategories/subfamilies MGEs. Further, provides detailed guide on how to precisely annotate also SEARCH/BLAST functions facilitate finding Overall,...
An efficient tandem route to the synthesis of 3H-1,2a(1),3-triazaacenaphthylene derivatives cyclazine family has been developed. Target compounds were obtained in moderate good yields by a Yb(OTf)(3)/Ag(2)CO(3)-catalyzed, three-component domino reaction. This turn will set stage for wide application this useful reaction structurally diverse polyheterocyclic skeletons containing imidazo[1,2-a]pyridine privileged structure.
Nasopharyngeal carcinoma (NPC) is a refractory tumour, and chemotherapy one of the primary treatment modalities. Oncoprotein 18 (Op18)/stathmin conserved small cytosolic phosphoprotein highly expressed in tumours, which plays vital role maintaining malignant phenotype tumours. Taxol clinically widely used chemotherapeutic agent for broad range taxol-resistant This study showed that Op18/stathmin silencing by RNA interference (RNAi) combined taxol cooperatively improved cellular apoptosis...
Licochalcone A (LCA) exhibited anticancer activity through modulating reactive oxygen species (ROS) levels in some cancer cells and has been evidenced to suppress colorectal (CRC) formation progression. However, whether LCA mediates the progression of CRC by regulating ROS production remains unclear. To address this, HCT-116 were treated with LCA, resulting G0/G1 phase arrest, apoptosis, high generation, which attenuated N-acetyl-L-cysteine, a inhibitor. In addition, suppressed expression...