A5030878746- Circular RNAs in diseases
- MicroRNA in disease regulation
- Peptidase Inhibition and Analysis
- Cancer-related molecular mechanisms research
- HER2/EGFR in Cancer Research
- Membrane-based Ion Separation Techniques
- Monoclonal and Polyclonal Antibodies Research
- Potassium and Related Disorders
- Lung Cancer Treatments and Mutations
- Advancements in Battery Materials
- Neuropeptides and Animal Physiology
- Advanced Breast Cancer Therapies
- RNA modifications and cancer
- Chemical Synthesis and Analysis
- Cancer-related gene regulation
- Diabetes Treatment and Management
- Biological and pharmacological studies of plants
- Genomic variations and chromosomal abnormalities
- Cancer Mechanisms and Therapy
- Amyloidosis: Diagnosis, Treatment, Outcomes
- Redox biology and oxidative stress
- Microtubule and mitosis dynamics
- Helicobacter pylori-related gastroenterology studies
- Genomics, phytochemicals, and oxidative stress
- Phytochemistry and biological activity of medicinal plants
Anhui Medical University
2022-2023
Second Hospital of Anhui Medical University
2022-2023
Jiangsu Hengrui Medicine (China)
2022-2023
Peking Union Medical College Hospital
2022
Chinese Academy of Medical Sciences & Peking Union Medical College
2022
Xiamen University
2021
Harbin Medical University
2018-2020
Shantou University Medical College
2019
Shantou University
2019
Hanzhong People's Hospital
2018
Abstract More and more evidence indicates that circular RNAs (circRNAs) have important roles in several diseases, especially cancers. However, their involvement remains to be investigated breast cancer. Through screening circRNA profile, we identified 235 differentially expressed circRNAs Subsequently, explored the clinical significance of two circTADA2As a large cohort triple-negative cancer (TNBC), performed functional analysis circTADA2A-E6 vitro vivo support findings. Finally, evaluated...
First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic mutations. Ultimately, these patients' disease progresses, often driven by a second-site mutation in the kinase domain (T790M). Another liability of first drugs is severe adverse events inhibition WT EGFR. As such, our goal was to develop highly potent irreversible inhibitor largest selectivity ratio between drug-resistant double mutants (L858R/T790M, Del/T790M) and...
Highly potent human glucagon receptor (hGluR) antagonists have been prepared employing both medicinal chemistry and targeted libraries based on modification of the core (proximal) dimethoxyphenyl group, benzyl ether linkage, as well (distal) benzylic aryl group lead 2, 3-cyano-4-hydroxybenzoic acid (3,5-dimethoxy-4-isopropylbenzyloxybenzylidene)hydrazide. Electron-rich proximal moieties such mono- dimethoxy benzenes, naphthalenes, indoles were found to be active. The SAR was quite...
BackgroundAndrogen receptor (AR) plays a crucial role as transcription factor in promoting the development of hepatocellular carcinoma (HCC) which is prone to aberrant chromatin modifications. However, regulatory effects AR on epigenetic mediators HCC remain ill-defined. Enhancer zeste homolog 2 (EZH2), an oncogene responsible for tri-methylation histone H3 at lysine 27 (H3K27me3), was identified be overexpressed approximate 70–90% cases, prompted us investigate whether or how regulates EZH2...
Cervical cancer is one of the most malignant types tumor and fourth leading cause cancer‑associated mortality in females worldwide. High expression brain cytoplasmic RNA 1 (BCYRN1) has been detected various tumors. The present study aimed to investigate effect BCYRN1 viability motility cervical cancer, relevant mechanism. results demonstrated that was upregulated tissues compared with normal tissues. Elevated levels were also three human cell lines (SiHa, HeLa CaSki) non-cancerous...
Rapid mutations of proteins that are targeted in cancer therapy often lead to drug resistance. Often, the mutation directly affects a drug's binding site, effectively blocking drug, but these can have other effects such as changing protein turnover half-life. Utilizing SILAC MS, we measured cellular rates an important non-small cell lung target, epidermal growth factor receptor (EGFR). Wild-type (WT) EGFR, EGFR with single activating mutant (Del 746-750 or L858R), and drug-resistant double...
Emodin is a promising anti-cancer reagent. To improve the physicochemical and property, we modified its structure get derivative called emodin succinyl ester (ESE). Here, investigated effect of ESE on suppression hepatocellular carcinoma (HCC) underlying mechanism. Our results showed that strongly inhibited HCC cell proliferation migration in vitro. Further study revealed treatment decreased transcription level protein expression androgen receptor (AR) enhancer zeste homolog 2 (EZH2), two...
BlsE, a predicted radical S-adenosyl-L-methionine (SAM) protein, was anaerobically purified and reconstituted in vitro to study its function the blasticidin S biosynthetic pathway. The putative role of BlsE elucidated based on bioinformatics analysis, genetic inactivation biochemical characterization. Biochemical results showed that is SAM-dependent enzyme utilizes cytosylglucuronic acid, accumulated intermediate metabolite blsE mutant, as substrate catalyzes decarboxylation at C5 position...
Circular RNAs (circRNAs) play important roles in carcinogenesis. Here, we investigated the mechanisms and clinical significance of circ-NOL10, a highly repressed circRNA breast cancer. Subsequently, also identified RNA-binding proteins (RBPs) that regulate circ-NOL10. Bioinformatics analysis was utilized to predict regulatory RBPs as well circ-NOL10 downstream microRNAs (miRNAs) mRNA targets. RNA immunoprecipitation, luciferase assay, fluorescence situ hybridization, cell proliferation,...
The peptidyl nucleoside arginomycin is active against Gram-positive bacteria and fungi but displays much lower toxicity to mice than its analog blasticidin S. It features a rare amino acid, β-methylarginine, which attached the deoxyhexose moiety via 4'-aminoacyl bond. We here report cloning of complete biosynthetic gene cluster for from Streptomyces arginensis NRRL 15941. Among 14 putative essential open reading frames, argM, encoding an aspartate aminotransferase (AAT), adjacent argN,...
Acute myocardial infarction (AMI) is a common coronary artery disease. This study attempted to reveal the impact of circ-SUZ12 (hsa_circ_0042961) on cardiomyocyte injury after exposure hypoxia.Circ-SUZ12 was screened out from GEO dataset GSE169594. RNA expression and protein level were detected by quantitative real-time PCR (qRT-PCR) Western blot, respectively. The characteristics identified measuring its resistance Rnase R or actinomycin D (Act D) treatment. CCK-8 EdU assays performed...
Myocardial infarction has been recognized globally as a serious problem featured with high mortality and morbidity. In addition, hypoxia represents the central feature of myocardial infarction. Recently, it reported that circular RNAs can exert critical functions in biological processes diseases. However, most remain unclear cells cultured under hypoxic conditions. this study, we focused on exploring role circ_SMAD7 (namely hsa_circ_0000848 study) cardiomyocyte conditions to provide novel...
Capsid assembly modulators (CpAMs) represent a new class of antivirals targeting hepatitis B virus (HBV) core protein to disrupt the process. In this work, novel chemotype featuring fused heterocycle amide was discovered through pharmacophore exploration. Lead optimization resulted in compound 8 with an EC50 value 511 nM, and then methyl substitution on piperazine found improve vitro potency remarkably. Further SAR studies established key SHR5133, which showed high antiviral potency,...
Abstract Activating mutations in EGFR confer constitutive activity providing the oncogenic drive EGFR-mutant NSCLC. First and 2nd generation tyrosine kinase inhibitors (TKIs) are effective drugs this setting, but constrained by dose-limiting toxicities attributed to inhibition of wild type (WT) drug resistance caused, majority cases, via a T790M secondary mutation EGFR. We report pharmacology novel irreversible 3rd TKI active against with activating mutations, sparing WT Our was studied...