Search Results - "Brouwer, Arwin J"
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Activity-based probes for rhomboid proteases discovered in a mass spectrometry-based assay
Published in Proceedings of the National Academy of Sciences - PNAS (12-02-2013)“…Rhomboid proteases are evolutionary conserved intramembrane serine proteases. Because of their emerging role in many important biological pathways, rhomboids…”
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Broad-Spectrum Antimalarial Activity of Peptido Sulfonyl Fluorides, a New Class of Proteasome Inhibitors
Published in Antimicrobial Agents and Chemotherapy (01-08-2013)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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3
Efficient microwave-assisted synthesis of multivalent dendrimeric peptides using cycloaddition reaction (click) chemistry
Published in Chemical communications (Cambridge, England) (28-09-2005)“…Multivalent dendrimeric peptides were synthesized via a microwave-assisted Huisgen 1,3-dipolar cycloaddition between azido peptides and dendrimeric alkynes in…”
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4
Hydrolytic (In)stability of Methacrylate Esters in Covalently Cross-Linked Hydrogels Based on Chondroitin Sulfate and Hyaluronic Acid Methacrylate
Published in ACS omega (12-10-2021)“…Chondroitin sulfate (CS) and hyaluronic acid (HA) methacrylate (MA) hydrogels are under investigation for biomedical applications. Here, the hydrolytic…”
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5
Potent and Highly Selective Inhibitors of the Proteasome Trypsin-like Site by Incorporation of Basic Side Chain Containing Amino Acid Derived Sulfonyl Fluorides
Published in Journal of medicinal chemistry (28-06-2018)“…A unique category of basic side chain containing amino acid derived sulfonyl fluorides (SFs) has been synthesized for incorporation into new proteasome…”
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Targeted Covalent Inhibition of Prolyl Oligopeptidase (POP): Discovery of Sulfonylfluoride Peptidomimetics
Published in Cell chemical biology (16-08-2018)“…Prolyl oligopeptidase (POP), a serine protease highly expressed in the brain, has recently emerged as an enticing therapeutic target for the treatment of…”
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7
Structure‐Based Design and Synthesis of Lipid A Derivatives to Modulate Cytokine Responses
Published in Chemistry : a European journal (06-06-2024)“…Agonists of Toll like receptors (TLRs) have attracted interest as adjuvants and immune modulators. A crystal structure of TLR4/MD2 with E. coli LPS indicates…”
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Peptide microarray analysis of the cross‐talk between O‐GlcNAcylation and tyrosine phosphorylation
Published in FEBS letters (01-07-2017)“…O‐GlcNAcylation of proteins regulates important cellular processes. A few reports noted that O‐GlcNAcylation exhibits cross‐talk with tyrosine phosphorylation…”
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Synthesis of monophosphoryl lipid A using 2-naphtylmethyl ethers as permanent protecting groups
Published in Carbohydrate research (01-12-2020)“…Lipid A, which is a conserved component of lipopolysaccharides of gram-negative bacteria, has attracted considerable interest for the development of…”
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10
Proteasome inhibition by new dual warhead containing peptido vinyl sulfonyl fluorides
Published in Bioorganic & medicinal chemistry (15-08-2016)“…[Display omitted] The success of inhibition of the proteasome by formation of covalent bonds is a major victory over the long held-view that this would lead to…”
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Selective Inhibition of the Immunoproteasome by Ligand-Induced Crosslinking of the Active Site
Published in Angewandte Chemie International Edition (27-10-2014)“…The concept of proteasome inhibition ranks among the latest achievements in the treatment of blood cancer and represents a promising strategy for modulating…”
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12
Delayed fibril formation of amylin(20–29) by incorporation of alkene dipeptidosulfonamide isosteres obtained by solid phase olefin cross metathesis
Published in Bioorganic & medicinal chemistry (2008)“…The synthesis of a new peptidomimetic structure, the alkene dipeptidosulfonamide isostere, is described. The synthesis is based on a cross metathesis reaction…”
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Potential peptidic proteasome inhibitors by incorporation of an electrophilic trap based on amino acid derived α-substituted sulfonyl fluorides
Published in Bioorganic & medicinal chemistry (01-10-2017)“…[Display omitted] Peptido sulfonyl fluoride derivatives were designed and synthesized containing a substituent on the alpha position (αPSFs) with respect to…”
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Peptido Sulfonyl Fluorides as New Powerful Proteasome Inhibitors
Published in Journal of medicinal chemistry (27-12-2012)“…A new class of potent proteasome inhibitors is described, of which the members contain an amino acid inspired sulfonyl fluoride as the electrophilic trap. In…”
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15
Synthesis of DOTA-conjugated multivalent cyclic-RGD peptide dendrimers via 1,3-dipolar cycloaddition and their biological evaluation: implications for tumor targeting and tumor imaging purposes
Published in Organic & biomolecular chemistry (01-01-2007)“…This report describes the design and synthesis of a series of alpha(V)beta(3) integrin-directed monomeric, dimeric and tetrameric cyclo[Arg-Gly-Asp-d-Phe-Lys]…”
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Expedient synthesis of a novel asymmetric selectively deprotectable derivative of the ATAC scaffold
Published in Tetrahedron (01-07-2014)“…An efficient multigram scale synthesis of a new asymmetric triazacyclophane scaffold, the ATAC (Asymmetric-TAC) scaffold, bearing three selectively removable…”
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Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA
Published in Organic & biomolecular chemistry (28-11-2015)“…A new divalent highly potent inhibitor of the Pseudomonas aeruginosa lectin and virulence factor LecA was prepared. It contains two thiourea linkages which…”
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Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap
Published in Bioorganic & medicinal chemistry (01-04-2011)“…We have designed and synthesized novel irreversible serine protease inhibitors containing aliphatic sulfonyl fluorides as an electrophilic trap. These…”
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Synthesis of the TACO Scaffold as a New Selectively Deprotectable Conformationally Restricted Triazacyclophane Based Scaffold
Published in Organic letters (06-06-2014)“…The synthesis of a new triazacyclophane scaffold (TACO scaffold) containing three selectively deprotectable amines is described. The TACO scaffold is…”
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Scaffold optimization in discontinuous epitope containing protein mimics of gp120 using smart libraries
Published in Organic & biomolecular chemistry (28-04-2013)“…A diversity of protein surface discontinuous epitope mimics is now rapidly and efficiently accessible. Despite the important role of protein-protein…”
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