A5048988244- Chemical Synthesis and Reactions
- Computational Drug Discovery Methods
- Ubiquitin and proteasome pathways
- Synthesis of Indole Derivatives
- Quinazolinone synthesis and applications
- Synthesis and Biological Evaluation
- Phenothiazines and Benzothiazines Synthesis and Activities
- Natural product bioactivities and synthesis
- interferon and immune responses
- Cytokine Signaling Pathways and Interactions
- Chemical Synthesis and Analysis
- Plant biochemistry and biosynthesis
- Cancer Research and Treatments
- Multicomponent Synthesis of Heterocycles
- Cell Adhesion Molecules Research
- Cancer therapeutics and mechanisms
- Genomics, phytochemicals, and oxidative stress
- Carbohydrate Chemistry and Synthesis
- Estrogen and related hormone effects
- Sulfur-Based Synthesis Techniques
- Asymmetric Synthesis and Catalysis
- Glioma Diagnosis and Treatment
- Telomeres, Telomerase, and Senescence
- Cancer Mechanisms and Therapy
- Synthesis of Organic Compounds
Nanjing Medical University
2015-2025
Huaian First People’s Hospital
2025
Soochow University
2025
China Pharmaceutical University
2013-2020
State Key Laboratory of Natural Medicine
2016-2017
Fuzhou University
2015-2016
Guilin University of Technology
2009
Temozolomide (TMZ) is a standard treatment for glioblastoma (GBM) patients. However, TMZ has moderate therapeutic effects due to chemoresistance of GBM cells through less clarified mechanisms. Here, we demonstrate that TMZ-derived 5-aminoimidazole-4-carboxamide (AICA) converted AICA ribosyl-5-phosphate (AICAR) in cells. This conversion catalyzed by hypoxanthine phosphoribosyl transferase 1 (HPRT1), which highly expressed human GBMs. As the bona fide activator AMP-activated protein kinase...
EGFRT790M mutation causes resistance to the first-generation tyrosine kinase inhibitors (TKIs) in patients with non-small cell lung cancer (NSCLC). However, therapeutic options for sensitizing first TKIs and delaying emergence of mutant are limited. In this study, we show that quercetin directly binds glucose-6-phosphate dehydrogenase (G6PD) inhibits its enzymatic activity through competitively abrogating NADP+ binding catalytic domain. This inhibition subsequently reduces intracellular...
Gastric cancer (GC) is the most prevalent gastrointestinal tumor with an unfavorable clinical prognosis. GC patients are largely threatened owing to metastasis and drug resistance. Tumor angiogenesis plays important role in development of gastric a challenge treatment cancer.Mouse xenograft models were used for screening therapeutic peptides on growth metastasis. Routine laboratory experimental methods including conditional cell culture, tube formation assay, qRT-PCR, Western blotting,...
A practical one-pot synthesis of various dehydroalanine esters was realized via a Cs 2 CO 3 -mediated simultaneous esterification/elimination process, starting from commercially available N-protected serines and haloalkanes.
Triple negative breast cancer (TNBC) is a type of with poor prognosis, and has no ideal therapeutic target medicine. Downregulation JWA closely related to the overall survival in many cancers including TNBC. In this study, we reported at first time that gene activating compound 1 (JAC1) inhibited proliferation TNBC vitro vivo experimental models. JAC1 specifically bound YY1 eliminated its transcriptional inhibition gene. The rescued induced G1 phase arrest apoptosis cells through p38 MAPK...
An efficient copper-catalyzed reaction for the synthesis of benzisothiazol-3(2H)-ones has been developed, starting from easily available 2-halobenzamides and carbon disulfide, which gave corresponding target products in 30-89% yield 25 examples. The proceeds via a consecutive process with S-C bond S-N formation.
Background: JWA gene is known to down-regulate SP1 and reduces the expression level of Integrin αvβ3. Here, we identified a functional polypeptide (JP1) based on active fragment protein suppress melanoma growth metastasis by inhibiting Methods: We conducted series mouse models evaluate anti-melanoma effect JP1 peptide. 18F-labeled (18F-NFP-JP1) was detected Micro-PET assay demonstrate drug biodistribution. Toxicity test in cynomolgus monkeys pharmacokinetic studies rats were done assess...
Abstract The overexpression of HER2 is associated with a malignant proliferation breast cancer. In this study, we developed non-cytotoxic JWA gene activating compound 1 (JAC1) to inhibit the HER2-positive cancer cells in vitro and vivo experimental models. JAC1 increased ubiquitination at K716 site through E3 ubiquitin ligase SMURF1 which was due decreased expression NEDD4, SMURF1. conclusion, suppresses triggered signaling. may serve as potential therapeutic agent for
Depression is the leading cause of global burden disease and disability. Abnormalities in kynurenine pathway tryptophan degradation have been closely linked to pathogenesis depression. An integrative bioinformatics analysis demonstrated that indoleamine 2,3-dioxygenase 1 (IDO1) (TDO) are potential targets for development antidepressants. A series 1-(hetero)aryl-β-carboline derivatives were designed, synthesized, evaluated as novel IDO1/TDO dual inhibitors. Among them, compound 28 displayed...
Antidiabetic agents simultaneously inhibiting hepatic glucose production and stimulating consumption could apply a better control over hyperglycemia. A series of oleanolic acid derivatives with bulky substituents at C-3 position were designed synthesized in order to search for this kind agents. All the compounds evaluated biologically vitro using glycogen phosphorylase HepG2 cells. The results indicated that several exhibited moderate-to-good inhibitory activities against phosphorylase....
I 2 /CF 3 CO Ag-mediated iodolactonization of allenoic acids has been developed to synthesize various 6- 9-membered ring vinylic iodolactones in 16–89% yield.
A highly efficient copper-catalyzed one-pot protocol is developed for the synthesis of 4-aminoquinazolines from easily available 2-iodo- or 2-bromobenzimidamides, aldehydes, and sodium azide. This approach proceeds via consecutive SNAr substitution, reduction, cyclization, oxidation tautomerization. The corresponding target products (26 examples) are obtained in 50–90% yield.
A practical synthesis of α‐amyrin ( 1 ), β‐amyrin 2 and lupeol 3 ) was accomplished in total yields 32, 42, 40% starting from easily available ursolic acid 4 oleanolic 5 betulin 6 respectively. Remarkably, these three natural pentacyclic triterpenes exhibited potential inhibitory activity against human oxidosqualene cyclase.
The Er(OTf) 3 -catalyzed cascade cyclization reaction of para -quinone methides with various 1,3-dicarbonyl compounds has been developed, which efficiently constructed a series versatile 4-aryl-3,4-dihydrocoumarins and 4-aryl-4 H -chromenes.
A one-pot highly specific isomerization of oleanolic acid esters (<bold>5a–g</bold>) to δ-oleanolic (<bold>6a–g</bold>) was achieved in the presence proton-exchanged montmorillonite (H-mont) under mild reaction conditions.
Background: Cisplatin (DDP) is a highly effective chemotherapeutic agent to most solid tumors including gastric cancer (GC), however, its clinical value limited due severe toxic side effects and secondary drug resistance.JP3, JWA protein based MMP2-targeted polypeptide, known inhibit the growth of GC in vivo.However, bidirectional JP3 DDP-resistant normal cells have not been demonstrated.The present study aims investigate actions on protecting from toxicity DDP while enhancing anti-tumor...
Glioblastoma is the most common brain tumor, with high recurrence and low survival rates. An integrative bioinformatics analysis demonstrated that anaplastic lymphoma kinase (ALK) a promising therapeutic target for glioblastoma. We designed synthesized series of 3-(arylmethylene)indole derivatives, which were further evaluated antiproliferative activity using glioma cell lines. Among them, compound 4a significantly inhibited viability glioblastoma cells. With favorable pharmacokinetic...