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Inside Cover: Efficient Self‐Assembly of Di‐, Tri‐, Tetra‐, and Hexavalent Hosts with Predefined Geometries for the Investigation of Multivalency (Chem. Eur. J. 37/2015)
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Dr. Sabrina Lusvarghi Dr. Rodolfo Ghirlando Prof. Dr. Chi‐Huey Wong Dr. Carole A. Bewley 《Angewandte Chemie (International ed. in English)》2015,54(19):5603-5608
High‐mannose‐type glycans (HMTGs) decorating viral spike proteins are targets for virus neutralization. For carbohydrate‐binding proteins, multivalency is important for high avidity binding and potent inhibition. To define the chemical determinants controlling multivalent interactions we designed glycopeptide HMTG mimetics with systematically varied mannose valency and spacing. Using the potent antiviral lectin griffithsin (GRFT) as a model, we identified by NMR spectroscopy, SPR, analytical ultracentrifugation, and microcalorimetry glycopeptides that fully recapitulate the specificity and kinetics of binding to Man9GlcNAc2Asn and a synthetic nonamannoside. We find that mannose spacing and valency dictate whether glycopeptides engage GRFT in a face‐to‐face or an intermolecular binding mode. Surprisingly, although face‐to‐face interactions are of higher affinity, intermolecular interactions are longer lived. These findings yield key insights into mechanisms involved in glycan‐mediated viral inhibition. 相似文献
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Facile Self‐Assembly of Metallo‐Supramolecular Ring‐in‐Ring and Spiderweb Structures Using Multivalent Terpyridine Ligands
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Jun‐Hao Fu Yin‐Hsuan Lee Yun‐Jui He Prof. Dr. Yi‐Tsu Chan 《Angewandte Chemie (International ed. in English)》2015,54(21):6231-6235
A series of metallo‐supramolecular ring‐in‐ring structures was generated by assembling CdII ions and the multivalent terpyridine ligands ( L1‐3 ) composed of one 60°‐bent and two 120°‐bent bis(terpyridine)s with varying alkyl linker lengths. The mechanistic study for the self‐assembly process excluded an entropically templated pathway and showed that the intramolecularly complexed species is the key intermediate leading to ring‐in‐ring formation. The next‐generation superstructure, a spiderweb, was produced in quantitative yield using the elongated decakis(terpyridine) ligand ( L5 ). 相似文献
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Dr. Adina Borbély Dr. Fabien Thoreau Dr. Eduard Figueras Malika Kadri Dr. Jean-Luc Coll Dr. Didier Boturyn Prof. Dr. Norbert Sewald 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(12):2602-2605
The effective delivery of cytotoxic agents to tumor cells is a key challenge in anticancer therapy. Multivalent integrinspecific ligands are considered a promising tool to increase the binding affinity, selectivity, and internalization efficiency of small-molecule drug conjugates. Herein, we report the synthesis and biological evaluation of a multimeric conjugate containing the high-affinity integrin αvβ3 binding ligand RAFT-c(RGDfK)4, a lysosomally cleavable Val-Cit linker, and cryptophycin-55 glycinate, a potent inhibitor of tubulin polymerization. In vitro cytotoxicity assays verified that the multimeric RGD-cryptophycin conjugate displays improved potency compared to the monomeric analogue in integrin αvβ3 overexpressing tumor cell lines, while significantly reduced activity was observed in the integrin-negative cell line. 相似文献
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Olga Martínez‐Ávila Dr. Karolin Hijazi Dr. Marco Marradi Dr. Caroline Clavel Dr. Colin Campion Dr. Charles Kelly Prof. Soledad Penadés Prof. Dr. 《Chemistry (Weinheim an der Bergstrasse, Germany)》2009,15(38):9874-9888
The HIV envelope glycoprotein gp120 takes advantage of the high‐mannose clusters on its surface to target the C‐type lectin dendritic cell‐specific intracellular adhesion molecule‐3‐grabbing non‐integrin (DC‐SIGN) on dendritic cells. Mimicking the cluster presentation of oligomannosides on the virus surface is a strategy for designing carbohydrate‐based antiviral agents. Bio‐inspired by the cluster presentation of gp120, we have designed and prepared a small library of multivalent water‐soluble gold glyconanoparticles (manno‐GNPs) presenting truncated (oligo)mannosides of the high‐mannose undecasaccharide Man9GlcNAc2 and have tested them as inhibitors of DC‐SIGN binding to gp120. These glyconanoparticles are ligands for DC‐SIGN, which also interacts in the early steps of infection with a large number of pathogens through specific recognition of associated glycans. (Oligo)mannosides endowed with different spacers ending in thiol groups, which enable attachment of the glycoconjugates to the gold surface, have been prepared. manno‐GNPs with different spacers and variable density of mannose (oligo)saccharides have been obtained and characterized. Surface plasmon resonance (SPR) experiments with selected manno‐GNPs have been performed to study their inhibition potency towards DC‐SIGN binding to gp120. The tested manno‐GNPs completely inhibit the binding from the micro‐ to the nanomolar range, while the corresponding monovalent mannosides require millimolar concentrations. manno‐GNPs containing the disaccharide Manα1‐2Manα are the best inhibitors, showing more than 20 000‐fold increased activity (100 % inhibition at 115 nM ) compared to the corresponding monomeric disaccharide (100 % inhibition at 2.2 mM ). Furthermore, increasing the density of dimannoside on the gold platform from 50 to 100 % does not improve the level of inhibition. 相似文献
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Karol Nowosinski Stephan Warnke Kevin Pagel Dávid Komáromy Wei Jiang Christoph A. Schalley 《Journal of mass spectrometry : JMS》2016,51(4):269-281
The solution‐phase photooxygenation of multiply threaded crown/ammonium pseudorotaxanes containing anthracene spacers is monitored by electrospray ionization Fourier‐transform ion‐cyclotron‐resonance (ESI‐FTICR) mass spectrometry. The oxygenated pseudorotaxanes are mass‐selected and fragmented by infrared multiphoton dissociation (IRMPD) and/or collision‐induced dissociation (CID) experiments and and their behavior compared to that of the non‐oxygenated precursors. [4+2]Cycloreversion reactions lead to the loss of O2, when no other reaction channel with competitive energy demand is available. Thus, the release of molecular oxygen can serve as a reference reaction for the energy demand of other fragmentation reactions such as the dissociation of the crown/ammonium binding motifs. The photooxygenation induces curvature into the initially planar anthracene and thus significantly changes the geometry of the divalent, anthracene‐spacered wheel. This is reflected in ion‐mobility data. Coulomb repulsion in multiply charged pseudorotaxanes assists the oxygen loss as the re‐planarization of the anthracene increases the distance between the two charges. Copyright © 2016 John Wiley & Sons, Ltd. 相似文献
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Daniel Lauster Maria Glanz Markus Bardua Dr. Kai Ludwig Dr. Markus Hellmund Dr. Ute Hoffmann Prof. Dr. Alf Hamann Dr. Christoph Böttcher Prof. Dr. Rainer Haag Prof. Dr. Christian P. R. Hackenberger Prof. Dr. Andreas Herrmann 《Angewandte Chemie (International ed. in English)》2017,56(21):5931-5936
To inhibit binding of the influenza A virus to the host cell glycocalyx, we generate multivalent peptide–polymer nanoparticles binding with nanomolar affinity to the virus via its spike protein hemagglutinin. The chosen dendritic polyglycerol scaffolds are highly biocompatible and well suited for a multivalent presentation. We could demonstrate in vitro that by increasing the size of the polymer scaffold and adjusting the peptide density, viral infection is drastically reduced. Such a peptide–polymer conjugate qualified also in an in vivo infection scenario. With this study we introduce the first non-carbohydrate-based, covalently linked, multivalent virus inhibitor in the nano- to picomolar range by ensuring low peptide-ligand density on a larger dendritic scaffold. 相似文献
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