A5036867748- Glycosylation and Glycoproteins Research
- Carbohydrate Chemistry and Synthesis
- Galectins and Cancer Biology
- Monoclonal and Polyclonal Antibodies Research
- Chemical Synthesis and Analysis
- Biochemical and Structural Characterization
- Bacteriophages and microbial interactions
- Antimicrobial Peptides and Activities
- Click Chemistry and Applications
- Toxin Mechanisms and Immunotoxins
- Escherichia coli research studies
- Peptidase Inhibition and Analysis
- Cyclopropane Reaction Mechanisms
- Signaling Pathways in Disease
- Dendrimers and Hyperbranched Polymers
- Lysosomal Storage Disorders Research
- Advanced Proteomics Techniques and Applications
- Mass Spectrometry Techniques and Applications
- Influenza Virus Research Studies
- Infant Nutrition and Health
- Bacterial Genetics and Biotechnology
- Microbial Natural Products and Biosynthesis
- Streptococcal Infections and Treatments
- RNA and protein synthesis mechanisms
- Helicobacter pylori-related gastroenterology studies
Utrecht University
2016-2025
Jiangnan University
2022
Pharmo Institute
2004-2021
Cancer Genomics Centre
2016-2017
University of Konstanz
2013
KU Leuven
2009
University Medical Center Utrecht
2008
Heidelberg University
2008
University Hospital Heidelberg
2008
University of Turku
2004
Multivalent carbohydrates are currently produced in many forms ranging from dendrimers, polymers, micelles, vesicles, nanoparticles to functionalized nanotubes, order enhance the potency of as ligands or inhibitors. Variations valency range systems containing two carbohydrate units those more than 2000. In this perspective a number popular target proteins for multivalent binding/inhibition have been selected. The optimal displaying largest multivalency effects discussed with respect their...
Abstract Discovery of glycan‐competitive galectin‐3‐binding compounds that attenuate lung fibrosis in a murine model and block intracellular galectin‐3 accumulation at damaged vesicles, hence revealing galectin‐3–glycan interactions involved progression activities, is reported. 3,3′‐Bis‐(4‐aryltriazol‐1‐yl)thiodigalactosides were synthesized evaluated as antagonists galectin‐1, ‐2, ‐3, ‐4 N‐terminal, C‐terminal, ‐7 ‐8 ‐9 C‐terminal domains. Compounds displaying low‐nanomolar affinities for...
Galectins are mammalian carbohydrate-binding proteins that involved in cell–cell and cell–matrix adhesion, cell migration, growth regulation with relevance to inflammation tumor spread. These important functions account for the interest design suitable low molecular weight inhibitors match distinct modes of presentation carbohydrate recognition domains different galectin subfamilies. Using 3,5-di-(2-aminoethoxy)benzoic acid as branching unit, wedgelike glycodendrimers two, four, eight...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTHigh enantioselectivity in the intramolecular cyclopropanation of allyl diazoacetates using a novel rhodium(II) catalystMichael P. Doyle, Roland J. Pieters, Stephen F. Martin, Richard E. Austin, Christopher Oalmann, and Paul MuellerCite this: Am. Chem. Soc. 1991, 113, 4, 1423–1424Publication Date (Print):February 1, 1991Publication History Published online1 May 2002Published inissue 1 February...
Chemical cross-linking mass spectrometry is rapidly emerging as a prominent technique to study protein structures. Structural information obtained by covalently connecting peptides in close proximity small reagents and identifying the resulting peptide pairs spectrometry. However, substoichiometric reaction efficiencies render routine detection of cross-linked problematic. Here, we present new trifunctional reagent, termed PhoX, which decorated with stable phosphonic acid handle. This makes...
Carbohydrates participate in almost every aspect of biology from protein sorting to modulating cell differentiation and cell–cell interactions. To date, the majority data gathered on glycan expression has been obtained via analysis with either anti-glycan antibodies or lectins. A detailed understanding specificities these reagents is critical carbohydrates biological systems. Glycan microarrays are increasingly used determine binding specificity glycan-binding proteins (GBPs). In this study,...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of nitrogen-containing polycycles via rhodium(II)-induced cyclization-cycloaddition and insertion reactions N-(diazoacetoacetyl)amides. Conformational control reaction selectivityMichael P. Doyle, Roland J. Pieters, Jack Taunton, Hoan Q. Pho, Albert Padwa, Donald L. Hertzog, Laura PrecedoCite this: Org. Chem. 1991, 56, 2, 820–829Publication Date (Print):January 1, 1991Publication History Published online1 May 2002Published inissue 1...
Multivalent dendrimeric peptides were synthesized via a microwave-assisted Huisgen 1,3-dipolar cycloaddition between azido and alkynes in yields ranging from 46 to 96%.
Sticky fingers. The optimal ligand for the cholera toxin (CT), GM1-oligosaccharide (GM1os), was linked to dendritic structures that contained long spacer arms by using highly efficient "click" chemistry coupling. In inhibition studies very large multivalency effects were observed; best structure an unprecedented 380 000-fold more potent than a monovalent GM1os derivative.
The synthesis of a new rigid spacer based on carbohydrate-triazole repeating units and their incorporation into divalent systems is described. Inhibition studies showed that well-matched system with flexible ends leads to the most potent inhibition Pseudomonas aeruginosa lectin LecA.
The blood-brain barrier (BBB) formed by brain capillary endothelial cells (BCECs) constitutes a firm physical, chemical, and immunological barrier, making the accessible to only few percent of potential drugs intended for treatment inside central nervous system. With purpose overcoming restraints BBB allowing transport drugs, siRNA, or DNA into brain, novel approach is use superparamagnetic iron oxide nanoparticles (SPIONs) as drug carriers. aim this study was investigate ability fluorescent...
Ion mobility separates molecules in the gas-phase based on their physico-chemical properties, providing information about size as collisional cross-sections. The timsTOF Pro combines trapped ion with a quadrupole, collision cell and TOF mass analyzer, to probe ions at high speeds on-the-fly fragmentation. Here, we show that this platform is beneficial for cross-linking MS (XL-MS). Cross-linking reagents covalently link amino acids proximity, resulting peptide pairs after proteolytic...
The bacterial pathogens
SARS-CoV-2 viruses engage ACE2 as a functional receptor with their spike protein. The S1 domain of the protein contains C-terminal binding (RBD) and an N-terminal (NTD). NTD other coronaviruses includes glycan cleft. However, for NTD, protein–glycan was only observed weakly sialic acids highly sensitive methods. Amino acid changes in variants concern (VoC) show antigenic pressure, which can be indication NTD-mediated binding. Trimeric proteins SARS-CoV-2, alpha, beta, delta, omicron did not...
New and rigid multivalent lactose molecules were prepared. The structures contain lactose-2-aminothiazoline units at the periphery that formed from a cyclisation of thiourea sulphur onto triple bond spacer. lactosides evaluated as inhibitors against lectin binding in solid phase inhibition assay. In this assay glycoprotein asialofetuin was immobilized surface microtiter plate wells, mimicking cell presentation, while mammalian galectins-1, -3 or -5 solution. Between three galectins, folding...
Abstract A facile and high‐yielding synthesis of multivalent 1,4‐disubstituted 1,2,3‐triazole‐linked glycodendrimers is described. Azido carbohydrates are linked by a Cu I ‐catalyzed [3+2] cycloaddition reaction to dendritic acetylenes using microwave irradiation. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005)
Lipid II is a crucial component in bacterial cell wall synthesis [Breukink, E., et al. (1999) Science 286, 2361−2364]. It the target of number important antibiotics, which include vancomycin and nisin de Kruijff, B. (2006) Nat. Rev. Drug Discovery 5, 321−332]. Here we show that hybrid antibiotic consists fragments significantly more active than separate against resistant entercocci (VRE). Three different hybrids were synthesized using click chemistry compared. Optimal spacer lengths...
Dendrimers were fitted out with up to eight mannose moieties by "click" chemistry. They subsequently attached aluminum oxide chips via a spacer that was linked the dendrimer core; this resulted in microarray of glycodendrimers. Binding glycodendrimers fluorescent lectins ConA and GNA observable real time. In single experiment it possible observe multivalency enhancement or cluster effect binding event. This small for ConA, agreement its widely spaced sites, whereas large GNA, twelve much...