Accès ouvert
2026
article
OpenAlex
Richard J. B. H. N. van den Berg, Adrianus M. C. H. van den Nieuwendijk, Bing Liu, Maria J. Ferraz et autres
Deoxynojirimycin is the archetypal iminosugar, from which many structural and configurational isosteres have been derived and studied in past decades. In total, 16 configurational isomers of deoxynojirimycin exist, but these have not yet been collected in a single library. This paper describes …
in
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Accès ouvert
2024
article
OpenAlex
Melissa Thaler, Tim P. Ofman, Ken Kok, Jurriaan J. A. Heming et autres
High Resolution Image Download MS PowerPoint Slide 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 protein quality control. We found, by screening a …
nl, gb
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Accès ouvert
2023
article
OpenAlex
Yurong Chen, Adrianus M. C. H. van den Nieuwendijk, Liang Wu, E. J. MORAN et autres
High Resolution Image Download MS PowerPoint Slide Siastatin B is a potent and effective iminosugar inhibitor of three diverse glycosidase classes, namely, sialidases, β- d -glucuronidases, and N -acetyl-glucosaminidases. The mode of inhibition of glucuronidases, in contrast to sialidases, has long been …
nl, gb
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Accès ouvert
2023
article
OpenAlex
C.J. Kuo, Qin Su, Adrianus M. C. H. van den Nieuwendijk, Thomas J. M. Beenakker et autres
Acid β-galactosidase (GLB1) and galactocerebrosidase (GALC) are retaining exo-β-galactosidases involved in lysosomal glycoconjugate metabolism. Deficiency of GLB1 may result in the lysosomal storage disorders GM1 gangliosidosis, Morquio B syndrome, and galactosialidosis, and deficiency of GALC may result in Krabbe disease. Activity-based protein …
nl, gb
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Accès ouvert
2021
article
OpenAlex
Rhianna J. Rowland, Yurong Chen, Imogen Breen, Liang Wu et autres
Gaucher disease (GD) is a lysosomal storage disorder caused by inherited deficiencies in β-glucocerebrosidase (GBA). Current treatments require rapid disease diagnosis and a means of monitoring therapeutic efficacy, both of which may be supported by the use of GBA-targeting activity-based probes (ABPs). …
gb, nl
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Accès ouvert
2019
article
OpenAlex
Sebastian H. Grimm, Jordi F. Keijzer, Nora Liu, Ruud H. M. Wijdeven et autres
Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as a driver mutation in cancer progression in a subgroup of AML patients. Clinical trials have shown …
nl
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Accès ouvert
2018
article
OpenAlex
Marta Artola, Shirley Wouters, Sybrin P. Schröder, Casper de Boer et autres
Cyclophellitol aziridine and its configurational and functional isomers are powerful covalent inhibitors of retaining glycosidases, and find application in fundamental studies on glycosidases, amongst others in relation to inherited lysosomal storage disorders caused by glycosidase malfunctioning. Few direct and stereoselective aziridination methodologies …
nl
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Accès ouvert
2018
article
OpenAlex
Bing Liu, Jeanine van Mechelen, Richard J. B. H. N. van den Berg, Adrianus M. C. H. van den Nieuwendijk et autres
Iminosugars are an important class of natural products and have been subject to extensive studies in organic synthesis, bioorganic chemistry and medicinal chemistry, yet only a limited number of these studies are on glycosylated iminosugars. Here, a general route of synthesis is …
nl
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Accès ouvert
2018
article
OpenAlex
Eva J. van Rooden, M. Kohsiek, Roy M. Kreekel, Annelot C. M. van Esbroeck et autres
Diacylglycerol lipases (DAGL) are responsible for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol. The fluorescent activity-based probes DH379 and HT-01 have been previously shown to label DAGLs and to cross-react with the serine hydrolase ABHD6. Here, we report the synthesis and characterization of …
nl
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Accès ouvert
2017
article
OpenAlex
D. Lahav, Bing Liu, Richard J. B. H. N. van den Berg, Adrianus M. C. H. van den Nieuwendijk et autres
Human nonlysosomal glucosylceramidase (GBA2) is one of several enzymes that controls levels of glycolipids and whose activity is linked to several human disease states. There is a major need to design or discover selective GBA2 inhibitors both as chemical tools and as …
nl, sg, gb, in
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Accès ouvert
2017
article
OpenAlex
Gerjan de Bruin, Eva J. van Rooden, David Ward, Charlotte M. J. Wesseling et autres
Most known β2‐selective proteasome inhibitors suffer from relatively poor cell permeability as the result of a net positive charge caused by the basic moiety at P1. In this paper, we describe the synthesis of oligopeptide vinyl sulfones that contain different amino acids …
nl, ch, us
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Accès ouvert
2017
article
OpenAlex
Hui Deng, Tom van der Wel, Richard J. B. H. N. van den Berg, Adrianus M. C. H. van den Nieuwendijk et autres
Inhibitors of diacylglycerol lipases and α,β-hydrolase domain containing protein 6 (ABHD6) are potential leads for the development of therapeutic agents for metabolic and neurodegenerative disorders. Here, we report the enantioselective synthesis and structure activity relationships of triazole ureas featuring chiral, hydroxylated 2-benzylpiperidines …
nl
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