A5037320081- Glycosylation and Glycoproteins Research
- Monoclonal and Polyclonal Antibodies Research
- Carbohydrate Chemistry and Synthesis
- Advanced Biosensing Techniques and Applications
- Click Chemistry and Applications
- Antimicrobial Peptides and Activities
- Trypanosoma species research and implications
- Protein Structure and Dynamics
- RNA Research and Splicing
- RNA modifications and cancer
- Influenza Virus Research Studies
- Neuropeptides and Animal Physiology
- Chemical Synthesis and Analysis
- Lymphoma Diagnosis and Treatment
- Cancer-related gene regulation
- Aerogels and thermal insulation
- Immune Response and Inflammation
- Invertebrate Immune Response Mechanisms
- PI3K/AKT/mTOR signaling in cancer
- Protein Hydrolysis and Bioactive Peptides
- Advanced Cellulose Research Studies
- Galectins and Cancer Biology
- Advanced Glycation End Products research
- ATP Synthase and ATPases Research
- Seaweed-derived Bioactive Compounds
University of Alberta
2018-2024
Dalian Medical University
2023
Hubei University of Technology
2023
Alberta Glycomics Centre
2018
Peking University
2014-2018
Genomics (United Kingdom)
2018
Human neuraminidases (NEU) are associated with human diseases including cancer, atherosclerosis, and diabetes. To obtain small molecule inhibitors as research tools for the study of their biological functions, we designed a library 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (DANA) analogues modifications at C4 C9 positions. This allowed us to discover selective targeting NEU3 isoenzyme. Our most inhibitor has Ki 320 ± 40 nM 15-fold selectivity over other neuraminidase isoenzymes. blocks...
Background Chronic vascular disease atherosclerosis starts with an uptake of atherogenic modified low-density lipoproteins (LDLs) by resident macrophages, resulting in formation arterial fatty streaks and eventually atheromatous plaques. Increased plasma sialic acid levels, increased neuraminidase activity, reduced LDL content have been previously associated coronary artery human patients, but the mechanism underlying this association has not explored. Methods Results We tested hypothesis...
Bruton's tyrosine kinase (Btk) is an attractive drug target for treating several B-cell lineage cancers. Ibrutinib a first-in-class covalent irreversible Btk inhibitor and has demonstrated impressive effects in multiple clinical trials. Herein, we present series of novel 2,5-diaminopyrimidine inhibitors Btk. Compared with ibrutinib, these exhibited different selectivity profile the analyzed kinases as well dual-action mode inhibition both activation catalytic activity, which counteracts...
Inhibitors of human neuraminidase enzymes (NEU) are recognized as important tools for the study biological functions NEU and will be potent elucidating role these in regulating repertoire cellular glycans. Here we report discovery selective inhibitors 1 (NEU1) 2 (NEU2) with exceptional potency. A library modified 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (DANA) analogues, variability C5- or C9-position, were synthesized evaluated against four isoenyzmes (NEU1–4). Hydrophobic groups an...
The immobilization of functional proteins onto solid supports using affinity tags is an attractive approach in recent development protein microarray technologies. Among the commonly used fusion tags, glutathione S-transferase (GST) have been indispensable tools for protein–protein interaction studies and extensive applications recombinant purification reversible immobilization. Here, by utilizing pyrimidine-based small-molecule probes with a sulfonyl fluoride reactive group, we report novel...
The processes of activation, extravasation, and migration immune cells to a site are early essential steps in the induction an acute inflammatory response. These events part cascade, which involves multiple regulatory steps. Using murine air pouch model inflammation with LPS as inducer, we demonstrate that isoenzymes neuraminidase family (NEU1, 3, 4) play roles these by acting positive or negative regulators leukocyte infiltration. In genetically knocked-out (KO) mice for different NEU genes...
The human neuraminidase enzymes (NEU1, NEU2, NEU3, and NEU4) are a class of implicated in pathologies including cancer diabetes. Several reports have linked activity to the regulation cell migration cells. Using an vitro assay on fibronectin (FN) coated surfaces, we investigated role these integrin-mediated migration. We observed that inhibition caused significant retardation breast (MDA-MB-231) prostate (PC-3) lines when using inhibitors NEU3 NEU4. In contrast, NEU1 increase for same lines....
<bold>L1-Bpyne</bold> was discovered as a potent inhibitor and cell permeable probe of glyoxalase I.
Fluorophosphonate probes covalently immobilize proteins onto solid support by reacting with tyrosine 111 in the GST tag.
Cell migration to a site of inflammation is an important step the immune response. This process coordinated by cytokines, receptors, and signal processing machinery cell. Many cellular receptors are glycosylated, their activity can be modulated through changes in glycan structure. Furthermore, glycosylation critical folding trafficking receptors. In this work, we investigated role native human neuraminidase enzymes (NEU) transmigration. We used cultured T cell line (Jurkat) transwell assay...
Natural polysaccharides with high viscosity, good thermal stability, and biocompatibility can improve the mechanical properties of inorganic silica aerogels enhance their application safety. However, effects preparation methods polysaccharide-silica on microstructure have not been systematically studied. To better investigate effect aerogel materials, two different structures were prepared using Konjac glucomannan (KGM) tetraethoxysilane (TEOS) via physical blending (KTB) co-precursor (KTC),...
Abstract Mucopolysaccharidoses (MPS) are lysosomal storage diseases caused by defects in catabolism of glycosaminoglycans. MPS I, II, III and VII associated with accumulation heparan sulphate manifest neurological deterioration. Most these currently lack effective treatments. Here, we report that, compared to controls, neuraminidase 1 (NEU1) activity is drastically reduced brain tissues patients mouse models IIIA, IIIB IIIC, but not other disorders presenting storage. We further show that...
Human neuraminidases play critical roles in many physiological and pathological processes. Humans have four isoenzymes of NEU, making selective inhibitors important tools to investigate the function individual isoenzymes. A typical scaffold for NEU is 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (DANA) where C9 modifications can be potency selectivity against human NEU. To design improved DANA analogues, we generated a library compounds with either short alkyl chain or biphenyl substituent...
Abstract Small nuclear ribonucleoprotein polypeptide G (SNRPG) or Smith protein (SmG) is vitally involved in the biogenesis of major and minor spliceosome precursors that are spliceosomaluridyl-rich small particles (U snRNPs; U1, U2, U4 U5). The plausible involvement SNRPG tumor formation oncogenesis has made it center studies. In this study, for first time, tumorigenic immune-modulating functioning employing TCGA GEO dataset-derived brain tumors been scrutinized by us. Most demonstrate...
Abstract The processes of activation, extravasation, and migration immune cells to a site are early essential steps in the induction an acute inflammatory response. These events part cascade which involves multiple regulatory steps. Using murine air-pouch model inflammation with LPS as inducer we demonstrate that isoenzymes neuraminidase family (NEU1, 3, 4) play roles this process acting positive or negative regulators leukocyte infiltration. Genetically knocked-out (KO) mice for different...