Search Results - "van den Berg, Richard J. B. H. N."

Structural basis of selective cannabinoid CB2 receptor activation by Li, Xiaoting, Chang, Hao, Bouma, Jara, de Paus, Laura V., Mukhopadhyay, Partha, Paloczi, Janos, Mustafa, Mohammed, van der Horst, Cas, Kumar, Sanjay Sunil, Wu, Lijie, Yu, Yanan, van den Berg, Richard J. B. H. N., Janssen, Antonius P. A., Lichtman, Aron, Liu, Zhi-Jie, Pacher, Pal, van der Stelt, Mario, Heitman, Laura H., Hua, Tian

“…Cannabinoid CB 2 receptor (CB 2 R) agonists are investigated as therapeutic agents in the clinic. However, their molecular mode-of-action is not fully…”
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Glycosphingolipids-Nature, Function, and Pharmacological Modulation by Wennekes, Tom, van den Berg, Richard J. B. H. N., Boot, Rolf G., van der Marel, Gijsbert A., Overkleeft, Herman S., Aerts, Johannes M. F. G.

“…The discovery of the glycosphingolipids is generally attributed to Johan L. W. Thudichum, who in 1884 published on the chemical composition of the brain. In…”
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Development of Adamantan-1-yl-methoxy-Functionalized 1-Deoxynojirimycin Derivatives as Selective Inhibitors of Glucosylceramide Metabolism in Man by Wennekes, Tom, van den Berg, Richard J. B. H. N, Donker, Wilma, van der Marel, Gijsbert A, Strijland, Anneke, Aerts, Johannes M. F. G, Overkleeft, Herman S

“…In this article, we present a straightforward synthesis of adamantan-1-yl-methoxy-functionalized 1-deoxynojirimycin derivatives. The used synthetic routes are…”
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The Development of an Aza-C-Glycoside Library Based on a Tandem Staudinger/Aza-Wittig/Ugi Three-Component Reaction by Wennekes, Tom, Bonger, Kimberly M., Vogel, Katrin, van den Berg, Richard J. B. H. N., Strijland, Anneke, Donker-Koopman, Wilma E., Aerts, Johannes M. F. G., van der Marel, Gijsbert A., Overkleeft, Herman S.

“…We report the tandem Staudinger/aza‐Wittig/Ugi three‐component reaction mediated synthesis of a 64‐member compound library of aza‐C‐glycosides. The library is…”
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Synthesis of l-altro-1-Deoxynojirimycin, d-allo-1-Deoxynojirimycin, and d-galacto-1-Deoxynojirimycin from a Single Chiral Cyanohydrin by van den Nieuwendijk, Adrianus M. C. H, Ruben, Mark, Engelsma, Sander E, Risseeuw, Martijn D. P, van den Berg, Richard J. B. H. N, Boot, Rolf G, Aerts, Johannes M, Brussee, Johannes, van der Marel, Gijs A, Overkleeft, Herman S

“…The chemoenzymatic synthesis of three 1-deoxynojirimycin-type iminosugars is reported. Key steps in the synthetic scheme include a Dibal…”
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Discovery of a Photoaffinity Probe that Captures the Active Conformation of the Cannabinoid CB2 Receptor by De Paus, Laura V., An, Yu, Janssen, Antonius P. A., Berg, Richard J. B. H. N., Heitman, Laura H., Stelt, Mario

“…The cannabinoid receptor type 2 (CB2R) is a G protein‐coupled receptor with therapeutic potential for the treatment of inflammatory disorders. Fluorescent…”
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Discovery of isoquinoline sulfonamides as allosteric gyrase inhibitors with activity against fluoroquinolone-resistant bacteria by Bakker, Alexander T., Kotsogianni, Ioli, Avalos, Mariana, Punt, Jeroen M., Liu, Bing, Piermarini, Diana, Gagestein, Berend, Slingerland, Cornelis J., Zhang, Le, Willemse, Joost J., Ghimire, Leela B., van den Berg, Richard J. H. B. N., Janssen, Antonius P. A., Ottenhoff, Tom H. M., van Boeckel, Constant A. A., van Wezel, Gilles P., Ghilarov, Dmitry, Martin, Nathaniel I., van der Stelt, Mario

“…Bacteria have evolved resistance to nearly all known antibacterials, emphasizing the need to identify antibiotics that operate via novel mechanisms. Here we…”
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Synthesis and Evaluation of Hybrid Structures Composed of Two Glucosylceramide Synthase Inhibitors by van den Berg, Richard J. B. H. N., van Rijssel, Erwin R., Ferraz, Maria Joao, Houben, Judith, Strijland, Anneke, Donker-Koopman, Wilma E., Wennekes, Tom, Bonger, Kimberly M., Ghisaidoobe, Amar B. T., Hoogendoorn, Sascha, van der Marel, Gijsbert A., Codée, Jeroen D. C., Overkleeft, Herman S., Aerts, Johannes M. F. G.

“…Glucosylceramide metabolism and the enzymes involved have attracted significant interest in medicinal chemistry, because aberrations in the levels of…”
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An Efficient Synthesis of the Natural Tetrahydrofuran Pachastrissamine Starting from d-ribo-Phytosphingosine by van den Berg, Richard J. B. H. N, Boltje, Thomas J, Verhagen, Carlo P, Litjens, Remy E. J. N, van der Marel, Gijsbert A, Overkleeft, Herman S

“…The natural product pachastrissamine, an anhydrophytosphingosine derivative isolated from various sponges and endowed with cytotoxic activity against several…”
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Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding by Deng, Hui, Kooijman, Sander, van den Nieuwendijk, Adrianus M. C. H, Ogasawara, Daisuke, van der Wel, Tom, van Dalen, Floris, Baggelaar, Marc P, Janssen, Freek J, van den Berg, Richard J. B. H. N, den Dulk, Hans, Cravatt, Benjamin F, Overkleeft, Herman S, Rensen, Patrick C. N, van der Stelt, Mario

“…Triazole ureas constitute a versatile class of irreversible inhibitors that target serine hydrolases in both cells and animal models. We have previously…”
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Identification and Development of Biphenyl Substituted Iminosugars as Improved Dual Glucosylceramide Synthase/Neutral Glucosylceramidase Inhibitors by Ghisaidoobe, Amar T, van den Berg, Richard J. B. H. N, Butt, Saleem S, Strijland, Anneke, Donker-Koopman, Wilma E, Scheij, Saskia, van den Nieuwendijk, Adrianus M. C. H, Koomen, Gerrit-Jan, van Loevezijn, Arnold, Leemhuis, Mark, Wennekes, Tom, van der Stelt, Mario, van der Marel, Gijsbert A, van Boeckel, Constant A. A, Aerts, Johannes M. F. G, Overkleeft, Herman S

“…This work details the evaluation of a number of N-alkylated deoxynojirimycin derivatives on their merits as dual glucosylceramide synthase/neutral…”
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A chemical genetic screen reveals that iminosugar inhibitors of plant glucosylceramide synthase inhibit root growth in Arabidopsis and cereals by Rugen, Michael D., Vernet, Mathieu M. J. L., Hantouti, Laila, Soenens, Amalia, Andriotis, Vasilios M. E., Rejzek, Martin, Brett, Paul, van den Berg, Richard J. B. H. N., Aerts, Johannes M. F. G., Overkleeft, Hermen S., Field, Robert A.

“…Iminosugars are carbohydrate mimics that are useful as molecular probes to dissect metabolism in plants. To analyse the effects of iminosugar derivatives on…”
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Synthesis of 6‑Hydroxysphingosine and α‑Hydroxy Ceramide Using a Cross-Metathesis Strategy by Wisse, Patrick, de Geus, Mark A. R, Cross, Gen, van den Nieuwendijk, Adrianus M. C. H, van Rooden, Eva J, van den Berg, Richard J. B. H. N, Aerts, Johannes M. F. G, van der Marel, Gijsbert A, Codée, Jeroen D. C, Overkleeft, Herman S

“…In this paper, a new synthetic route toward 6-hydroxysphingosine and α-hydroxy ceramide is described. The synthesis employs a cross-metathesis to unite a…”
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Epi-Cyclophellitol Cyclosulfate, a Mechanism-Based Endoplasmic Reticulum α‑Glucosidase II Inhibitor, Blocks Replication of SARS-CoV‑2 and Other Coronaviruses by Thaler, Melissa, Ofman, Tim P., Kok, Ken, Heming, Jurriaan J. A., Moran, Elisha, Pickles, Isabelle, Leijs, Anouk A., van den Nieuwendijk, Adrianus M. C. H., van den Berg, Richard J. B. H. N., Ruijgrok, Gijs, Armstrong, Zachary, Salgado-Benvindo, Clarisse, Ninaber, Dennis K., Snijder, Eric J., van Boeckel, Constant A. A., Artola, Marta, Davies, Gideon J., Overkleeft, Herman S., van Hemert, Martijn J.

“…The combined inhibition of endoplasmic reticulum (ER) α-glucosidases I and II has been shown to inhibit replication of a broad range of viruses that rely on ER…”
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ortho-Carborane-Modified N-Substituted Deoxynojirimycins by Hoogendoorn, Sascha, Mock, Elliot D., Strijland, Anneke, Donker-Koopman, Wilma E., van den Elst, Hans, van den Berg, Richard J. B. H. N., Aerts, Johannes M. F. G., van der Marel, Gijsbert A., Overkleeft, Herman S.

“…N‐alkyl‐deoxynojirimycins (DNMs) are an important class of glycoprocessing enzyme inhibitors. Our work on DNMs focuses on identifying potent and selective…”
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Synthesis and Evaluation of Lipophilic Aza-C-glycosides as Inhibitors of Glucosylceramide Metabolism by Wennekes, Tom, van den Berg, Richard J. B. H. N., Boltje, Thomas J., Donker-Koopman, Wilma E., Kuijper, Bastiaan, van der Marel, Gijsbert A., Strijland, Anneke, Verhagen, Carlo P., Aerts, Johannes M. F. G., Overkleeft, Herman S.

“…The structure–activity relationship of lipophilic aza‐C‐glycosides as inhibitors of the three enzymes of glucosylceramide metabolism is investigated. A library…”
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Synthesis and evaluation of homo-bivalent GnRHR ligands by Bonger, Kimberly M., van den Berg, Richard J.B.H.N., Heitman, Laura H., IJzerman, Ad P., Oosterom, Julia, Timmers, Cornelis M., Overkleeft, Herman S., van der Marel, Gijsbert A.

“…G protein coupled receptors (GPCRs) are important drug targets in pharmaceutical research. Traditionally, most research efforts have been devoted towards the…”
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Nanomolar affinity, iminosugar-based chemical probes for specific labeling of lysosomal glucocerebrosidase by Scherpenzeel, Monique van, van den Berg, Richard J.B.H.N., Donker-Koopman, Wilma E., Liskamp, Rob M.J., Aerts, Johannes M.F.G., Overkleeft, Herman S., Pieters, Roland J.

“…Three different photoprobes were synthesized to label β-glucosidases; one probe was based on glucose, two probes on the iminosugar deoxynojirimycin. The…”
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Preparation of 1-Thio Uronic Acid Lactones and Their Use in Oligosaccharide Synthesis by van den Bos, Leendert J, Litjens, Remy E. J. N, van den Berg, Richard J. B. H. N, Overkleeft, Herman S, van der Marel, Gijsbert A

“…The chemo- and regioselective TEMPO/BAIB-mediated oxidation of 2,6- and 3,6-dihydroxy 1-thio glycopyranosides to the corresponding 1-thio uronic acid lactones…”
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Structure–Activity Relationship Studies of Aryl Sulfoxides as Reversible Monoacylglycerol Lipase Inhibitors by Jiang, Ming, Huizenga, Mirjam C. W., Mohr, Florian, Amedi, Avand, Bakker, Renze, van den Berg, Richard J. B. H. N., Deng, Hui, van der Wel, Tom, van Boeckel, Constant A.A., van der Stelt, Mario

“…Monoacylglycerol lipase (MAGL) is the key enzyme for the hydrolysis of endocannabinoid 2-arachidonoylglycerol (2-AG). The central role of MAGL in the…”
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