A5100747440- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Computational Drug Discovery Methods
- Marine Toxins and Detection Methods
- Liver Disease Diagnosis and Treatment
- Cancer Genomics and Diagnostics
- Wound Healing and Treatments
- X-ray Diffraction in Crystallography
- Synthesis of β-Lactam Compounds
- Crystallization and Solubility Studies
- Extracellular vesicles in disease
- Asymmetric Hydrogenation and Catalysis
- Cholangiocarcinoma and Gallbladder Cancer Studies
- Cancer-related gene regulation
- RNA modifications and cancer
- Asymmetric Synthesis and Catalysis
- Plant Stress Responses and Tolerance
- Ginseng Biological Effects and Applications
- Pancreatic and Hepatic Oncology Research
- Synthesis and Biological Activity
- Hepatitis B Virus Studies
- PARP inhibition in cancer therapy
- Single-cell and spatial transcriptomics
- Aerogels and thermal insulation
- Microwave-Assisted Synthesis and Applications
Second Affiliated Hospital of Xi'an Jiaotong University
2023-2024
Ludong University
2024
Nanjing University
2023-2024
Jiangsu Hengrui Medicine (China)
2024
Jilin Provincial Academy of Forestry Science
2024
University of Electronic Science and Technology of China
2023
First Affiliated Hospital of Anhui Medical University
2023
Anhui Medical University
2023
Shanghai Ninth People's Hospital
2022-2023
Shanghai Jiao Tong University
2022-2023
Fragment-based drug discovery (FBDD) has proven to be an effective means of producing high-quality chemical ligands as starting points for drug-discovery pursuits. The increasing number clinical candidate drugs developed using FBDD approaches is a testament the efficacy this approach. success fragment-based methods highly dependent on identity fragment library used screening. vast majority centered use sp 2 -rich aromatic compounds. An expanded set fragments that possess more 3D character...
The stereochemistry is one of the critical issues in Staudinger reaction. We have proposed origin stereoselectivity recently. effects solvents, additives, and pathways ketene generation on were investigated by using a clean reaction, which sensitive reaction system to stereoselectivity. results indicate that usually existed generated do not generally affect solvent affects polar favorable formation trans-β-lactams. addition orders reagents between acyl chlorides imines. tertiary amine into...
Continuous cropping obstacles seriously constrained the sustainable development of ginseng industry. The allelopathic autotoxicity ginsenosides is key “trigger” continuous in ginseng. During harvest, plants could be broken and remain soil. decomposition residue soil one important release ways ginsenosides. Therefore, mechanism through decomposed pathway needs an in-depth study. To investigate this regulation mechanism, integrated analysis transcriptomics metabolomics was applied. prototype...
A notable and obvious ketene substituent-dependent effect of temperature on the stereoselectivity in Staudinger reaction was observed. Most reactions show concave Eyring plots characterized by two lines with an inversion point, following principle isoinversion. Their cis-selectivities decrease increasing temperature. Reactions involving intramolecular p−π π−π interactions between substituents imine C-substituents reveal protruding, S-shaped or straight-line plots. increase a certain region...
Introducing a silyl group at one of the internal olefin positions in diolefinic substrates results E-selective formation macrocyclic ring-forming metathesis. The application this method to range (E)-alkenylsiloxanes is described. Protodesilylation alkenylsiloxane products yields novel Z-configured macrocycles.
Chemical space exploration is a major task of the hit-finding process during pursuit novel chemical entities. Compared with other screening technologies, computational de novo design has become popular approach to overcome limitation current libraries. Here, we reported platform named systemic evolutionary explorer (SECSE). The was conceptually inspired by fragment-based drug design, that miniaturized "lego-building" within pocket certain target. key virtual hits generation then turned into...
Traditional fragment-based drug discovery (FBDD) relies heavily on structural analysis of the hits bound to their targets. Herein, we present a complementary approach based diversity-oriented synthesis (DOS). A DOS-based fragment collection was able produce initial hit compounds against target GSK3β, allow systematic related analogues explore fragment-level structure–activity relationship, and finally lead more potent compound.
An intramolecular aza-Michael reaction with a Cbz carbamate and an enone is reported to result in 3,5-disubstituted nitrogen-containing heterocycles. Either cis or trans isomers were obtained selectively using chiral substrates achiral Pd (II) complex strong Brønsted acid catalysis. A range of undergoes these selective transformations. Functionalization the resulting products yielding bicyclic heterocycles also demonstrated.
The identification and utilization of potential candidate genes with significant effects on economically important traits have become increasingly in poultry breeding programs.The prolactin (PRLR) receptor is a specific for prolactin, which an anterior pituitary peptide hormone involved various physiological activities essential reproductive success.In chickens, the PRLR gene resides Z chromosome.We used pooled DNA sequencing approach identifying SNPs gene.Three hundred ninesix Erlang...
ADME genes are a set of which involved in drug absorption, distribution, metabolism, and excretion (ADME). However, prognostic value function head neck squamous cell carcinoma (HNSCC) remain largely unclear. In this study, we established an ADME-related model through the least absolute shrinkage selection operator (LASSO) analysis Cancer Genome Atla (TCGA) training cohort its robustness was validated by TCGA internal validation Gene Expression Omnibus (GEO) external cohort. The 14-gene...
Membrane based CO2 capture has been considered as promising alternatives due to its high efficiency and small footprint, among which, facilitated transport (FT) membranes have gained more attention to...
Enzyme-mediated modifications at the wobble position of tRNAs are essential for translation genetic code. We report genetic, biochemical and structural characterization CmoB, enzyme that recognizes unique metabolite carboxy-S-adenosine-L-methionine (Cx-SAM) catalyzes a carboxymethyl transfer reaction resulting in formation 5-oxyacetyluridine tRNAs. CmoB is distinctive it only known member SAM-dependent methyltransferase (SDMT) superfamily utilizes naturally occurring SAM analog as alkyl...
A diastereoselective intramolecular aza-Michael reaction between N-Cbz carbamates and enones was studied. The investigation revealed that Brønsted acids with different strengths produce diastereomers. catalysts TfOH TFA were used to generate differential outcomes in the reaction.
A direct binding screen of 100 000 sp3-rich molecules identified a single diastereomer macrolactam core that binds specifically to myeloid cell leukemia 1 (MCL1). comprehensive toolbox biophysical methods was applied validate the original hit and subsequent analogues also established mode competitive with NOXA BH3 peptide. X-ray crystallography ligand bound MCL1 reveals remarkable ligand/protein shape complementarity diverges from previously disclosed inhibitor costructures.
Background: Treatment of diabetic wounds is a major challenge in clinical practice. Extracellular vesicles (EVs) from adipose-derived stem cells have shown effectiveness wound models. However, obtaining ADSC-EVs requires culturing vast numbers cells, which hampered by the need for expensive equipment and reagents, extended time cost, complicated procedures before commercialization. Therefore, methods to extract EVs discarded tissue be developed, immediate application during surgery. For this...
Abstract Aspirin, as a widely used anti-inflammatory drug, has been shown to exert anti-cancer effects in variety of cancers. PD-L1 is expressed tumor cells and inhibits anti-tumor immunity. This study aims clarify whether aspirin exerts its anti-hepatocellular carcinoma (HCC) effect by inhibiting expression. The rat model HCC was established drinking 0.01% diethylnitrosamine (DEN), given gavage. gross blood biochemical indexes rats were analyzed. CD4 CD8 expression liver tissues...
Macrocyclic (E)-alkenylsiloxanes, obtained from E-selective ring-closing metathesis reactions, can be converted to the corresponding (Z)-alkenyl bromides and (E)-alkenyl iodides allowing access both E- Z-trisubstituted macrocyclic alkenes. The reaction conditions substrate scope of these stereoselective transformations are explored.
PURPOSE: Accumulation of PIK3CA, ESR1, and GATA3 mutations results in resistance to endocrine therapy breast cancer patients; however, the response these genes chemotherapy is unclear. Therefore, we sought evaluate genetic circulating tumor DNA (ctDNA) metastatic patients. METHODS: The mutation frequency 1021 was examined prior ctDNA 44 estrogen receptor–positive These were evaluated again a subset patients (n=24) following chemotherapy. Mutation defined as percentage found compared total...