A5070433780- Receptor Mechanisms and Signaling
- Chronic Lymphocytic Leukemia Research
- Chronic Myeloid Leukemia Treatments
- Neuropeptides and Animal Physiology
- Acute Myeloid Leukemia Research
- Chemical Synthesis and Analysis
- Platelet Disorders and Treatments
- Nicotinic Acetylcholine Receptors Study
- Gastrointestinal Tumor Research and Treatment
- Lung Cancer Treatments and Mutations
- Epigenetics and DNA Methylation
- Cancer-related Molecular Pathways
- Lymphoma Diagnosis and Treatment
- PI3K/AKT/mTOR signaling in cancer
- Heat shock proteins research
- Listeria monocytogenes in Food Safety
- CRISPR and Genetic Engineering
- DNA Repair Mechanisms
- Virus-based gene therapy research
- HER2/EGFR in Cancer Research
- Advanced Breast Cancer Therapies
- Enzyme function and inhibition
- Oxidative Organic Chemistry Reactions
- ATP Synthase and ATPases Research
- Martial Arts: Techniques, Psychology, and Education
Zhengzhou University of Light Industry
2025
University of Science and Technology of China
2015-2024
Chinese Academy of Sciences
2015-2024
Xi'an Institute of Optics and Precision Mechanics
2024
University of Chinese Academy of Sciences
2024
China Academy of Space Technology
2024
Northeast Normal University
2024
East China Normal University
2022-2023
Sun Yat-sen University
2023
Second Affiliated Hospital of Shantou University Medical College
2023
Methicillin-resistant Staphylococcus aureus (MRSA) is currently regarded as one of the most important drug-resistant pathogens causing nosocomial and community-acquired infections. Although berberine (BER) has shown anti-MRSA activity, underlying mechanism still unclear. In this study, damage caused by BER on cell surface MRSA was systematically investigated performing susceptibility test, determining K+ alkaline phosphatase (ALP) release, detecting morphological alterations using scanning...
Through comprehensive comparison study, we found that ibrutinib, a clinically approved covalent BTK kinase inhibitor, was highly active against EGFR (L858R, del19) mutant driven NSCLC cells, but moderately to the T790M 'gatekeeper' cells and not wild-type cells. Ibrutinib strongly affected mediated signaling pathways induced apoptosis cell cycle arrest (G0/G1) in wt However, ibrutinib only slowed down tumor progression PC-9 H1975 xenograft models. MEK GSK1120212, could potentiate ibrutinib's...
FLT3-ITD mutant has been observed in about 30% of AML patients and extensively studied as a drug discovery target. On the basis our previous study that ibrutinib (9) exhibited selective moderate inhibitory activity against positive cells, through structure-guided design approach, we have discovered new type II FLT3 kinase inhibitor, compound 14 (CHMFL-FLT3-213), which highly potent effects associated oncogenic mutations (including FLT3-D835Y/H/V, FLT3-ITD-D835Y/I/N/A/G/Del, FLT3-ITD-F691L)....
Tumor suppressor protein p53, our most critical defense against tumorigenesis, can be made powerless by mechanisms such as mutations and inhibitors. Fortilin, a 172-amino acid polypeptide with potent anti-apoptotic activity, is up-regulated in many human malignancies. However, the exact mechanism which fortilin exerts its activity remains unknown. Here we present significant insight. Fortilin binds specifically to sequence-specific DNA binding domain of p53. The interaction p53 blocks...
On the basis of Ibrutinib's core pharmacophore, which was moderately active to EGFR T790M mutant, we discovered novel epidermal growth factor receptor (EGFR) inhibitor compound 19 (CHMFL-EGFR-202), potently inhibited primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M. Compound displayed a good selectivity profile among 468 kinases/mutants tested in KINOMEscan assay (S score (1) = 0.02). In particular, it did not exhibit apparent activities against INSR IGF1R kinases. The...
Blue light (BL) exerts an antimicrobial effect on pathogenic bacteria. It has been hypothesized that its bactericidal activity depends upon the generation of reactive oxygen species (such as anion superoxides) and resultant cellular damage. However, some aspects this hypothesis needed to be tested investigated. Thus, work conducted herein examined molecular impact BL treatment Cronobacter sakazakii, emerging foodborne pathogen. The results showed exhibited efficient against C. sakazakii....
Heat stress (HS) often causes sudden death of humans and animals due to heart failure, mainly resulting from the contraction cardiac microvasculature followed by myocardial ischemia. Cardiac microvascular endothelial cells (CMVECs) play an important role in maintaining vasodilatation. Aspirin (ASA) is well known for its protective abilities febrile animals. However, there little knowledge about molecular resistance mechanisms CMVECs which ASA may this context. Therefore, we used a heat model...
Water scarcity has emerged as a critical constraint on agricultural development and food security worldwide, particularly in arid semi-arid regions such Central Asia, Western North Africa, which are part of the “Belt Road” Initiative. This study, based global multi-regional input–output model, quantitatively analyzes virtual water flows between China countries along Road”. It focuses water-scarce regions, examining impact trade resource pressures security, well transfer resources patterns....
FLT3-ITD mutant has been observed in about 30% of AML patients and extensively studied as a drug discovery target. On the basis structure PCI-32765 (ibrutinib), BTK kinase inhibitor that was recently reported to bear FLT3 activity through structure-guided design approach, we have discovered compound 18 (CHMFL-FLT3-122), which displayed an IC50 40 nM against achieved selectivity over (over 10-fold). It significantly inhibited proliferation positive cancer cell lines MV4-11 (GI50 = 22 nM),...
Adeno-associated virus (AAV) vectors have been utilized extensively in gene therapy and function studies, as strong transgene expression is a prerequisite for positive outcomes. AAV8 was reported the most efficient AAV serotype transduction of liver, brain muscle compared with other serotypes. However, AAV8-mediated human hepatocytes rather poor approximately 20-fold lower efficiency that mouse hepatocytes. Therefore, we applied woodchuck hepatitis post-transcriptional regulatory element...
Hematopoietic stem and progenitor cells (HSPCs) are a heterogeneous group of with expansion, differentiation, repopulation capacities. How HSPCs orchestrate the stemness state diverse lineage differentiation at steady condition or acute stress remains largely unknown. Here, we show that zebrafish mutants deficient in an epigenetic regulator Atf7ip Setdb1 methyltransferase undergo excessive myeloid impaired HSPC manifesting decline T erythroid lineage. We find regulates hematopoiesis through...
Thromboxane A2 receptor (TP receptor), a prostanoid receptor, belongs to the G protein-coupled family, composed of three intracellular loops and extracellular connecting seven transmembrane helices. The highly conserved domains receptors were found in second loop (eLP2), which was proposed be involved ligand recognition. 3D structure eLP2 would help further explain binding mechanism. Analysis human TP model generated from molecular modeling based on bacteriorhodopsin crystallographic...
// Chen Hu 1, 2, * , Aoli Wang Hong Wu 3, Ziping Qi Xixiang Li Xiao-E Yan 4, Cheng 2 Kailin Yu Fengming Zou 3 Wenchao Wei Jiaxin Juan Liu Beilei Tao Ren 5 Shanchun Zhang 6 Cai-Hong Yun 4 Jing Qingsong 1 High Magnetic Field Laboratory, Chinese Academy of Sciences, Hefei, Anhui 230031, P. R. China University Science and Technology China, 230036, CHMFL-HCMTC Target Therapy Joint Institute Systems Biomedicine, Department Biophysics, Beijing Key Laboratory Tumor Biology Center for Molecular...
Radiotherapy is widely used in the management of advanced colorectal cancer (CRC). However, clinical efficacy limited by safe irradiated dose. Sensitizing tumor cells to radiotherapy via interrupting DNA repair a promising approach conquering limitation. The BRCA1-BARD1 complex has been demonstrated play critical role homologous recombination (HR) DSB repair, and its functions may be affected HERC2 or BAP1. Accumulated evidence illustrates that ubiquitination-deubiquitination balance...
The three-dimensional structure of a synthetic peptide corresponding to the N-terminal membrane anchor domain (residues 1—25) prostaglandin I2 synthase (also known as cytochrome P450 8A1), an eicosanoid-synthesizing microsomal P450, has been determined by two-dimensional 1H NMR spectroscopy in trifluoroethanol and dodecylphosphocholine which mimic hydrophobic environment. A combination experiments, including NOESY, TOCSY double-quantum-filtered COSY, was used obtain complete assignments for...
To overcome the difficulty of characterizing structures extracellular loops (eLPs) G protein‐coupled receptors (GPCRs) other than rhodopsin, we have explored a strategy to generate three‐dimensional structural model for GPCR, thromboxane A 2 receptor. This structure was completed by assembly NMR computation‐guided constrained peptides that mimicked and connected conserved seven transmembrane domains. The structure‐based reveals features eLPs, in which second loop (eLP ) disulfide bond...
cKIT kinase inhibitors, e.g., imatinib, could induce drug-acquired mutations such as T670I that rendered drug resistance after chronic treatment. Through a type II inhibitor design approach we discovered highly potent compound 35 (CHMFL-KIT-8140), which potently inhibited both wt (IC50 = 33 nM) and gatekeeper mutant 99 nM). Compound displayed strong antiproliferative effect against GISTs cancer cell lines GIST-T1 (cKIT wt, GI50 4 GIST-5R T670I, 26 In the cellular context it strongly c-KIT...
Chlorogenic acid (CGA) is an antibacterial agent that can be isolated from Eucommia ulmoides Oliver, a Chinese medicinal and edible plant food. The inhibitory effect of CGA on bacterial growth stiffness the outer membrane (OM) had been reported, while more evidence were required to elucidate its impairment cell wall. In this study, morphological physiochemical changes Salmonella cells under treatment investigated. Firstly, minimum concentration (MIC) against was assayed. Later, permeability...