Herman S Overkleeft
Affiliation: Leiden University
Country: The Netherlands
Jiang J, Kallemeijn W, Wright D, van den Nieuwendijk A, Rohde V, Folch E, et al
. In vitro and in vivo comparative and competitive activity-based protein profiling of GH29 ?-l-fucosidases. Chem Sci. 2015;6:2782-false pubmed publisher
..Competitive activity-based protein profiling identified l-fuconojirimycin as the single GH29 ?-l-fucosidase inhibitor from eight configurational isomers. ..
Stolze S, Liu N, Wijdeven R, Tuin A, van den Nieuwendijk A, Florea B, et al
. Photo-crosslinking of clinically relevant kinases using H89-derived photo-affinity probes. Mol Biosyst. 2016;12:1809-17 pubmed publisher
..A labelling protocol was established for recombinant kinases and more complex protein mixtures using gel-based techniques. We also show that the probes act in a competitive manner with other kinase inhibitors. ..
Jiang J, Beenakker T, Kallemeijn W, van der Marel G, van den Elst H, CodÃ©e J, et al
. Comparing Cyclophellitol N-Alkyl and N-Acyl Cyclophellitol Aziridines as Activity-Based Glycosidase Probes. Chemistry. 2015;21:10861-9 pubmed publisher
..Alkyl aziridines can therefore be an attractive alternative in retaining glycosidase ABP design, but in targeting a new retaining glycosidase both N-alkyl and N-acyl aziridines are best considered at the onset of a new study. ..
Li K, Jiang J, Witte M, Kallemeijn W, Donker Koopman W, Boot R, et al
. Exploring functional cyclophellitol analogues as human retaining beta-glucosidase inhibitors. Org Biomol Chem. 2014;12:7786-91 pubmed publisher
Kallemeijn W, Witte M, Voorn Brouwer T, Walvoort M, Li K, CodÃ©e J, et al
. A sensitive gel-based method combining distinct cyclophellitol-based probes for the identification of acid/base residues in human retaining Î²-glucosidases. J Biol Chem. 2014;289:35351-62 pubmed publisher
..The described method is highly sensitive, requiring only femtomoles (nanograms) of ABP-labeled enzymes. ..
Ouairy C, Ferraz M, Boot R, Baggelaar M, Van Der Stelt M, Appelman M, et al
. Development of an acid ceramidase activity-based probe. Chem Commun (Camb). 2015;51:6161-3 pubmed publisher
..Deficiency in acid ceramidase is the molecular basis of Farber disease. Here we report the synthesis and characterization of an activity-based acid ceramidase probe. ..
Liu N, Hoogendoorn S, van de Kar B, Kaptein A, Barf T, Driessen C, et al
. Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study. Org Biomol Chem. 2015;13:5147-57 pubmed publisher
..The work described here complements this existing methodology and pertains a comparative study on the efficacy of direct and two-step bioorthogonal ABPP of BTK. ..
van den Berg R, van Rijssel E, Ferraz M, Houben J, Strijland A, Donker Koopman W, et al
. Synthesis and Evaluation of Hybrid Structures Composed of Two Glucosylceramide Synthase Inhibitors. ChemMedChem. 2015;10:2042-62 pubmed publisher
de Bruin G, Xin B, Kraus M, Van Der Stelt M, van der Marel G, Kisselev A, et al
. A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities. Angew Chem Int Ed Engl. 2016;55:4199-203 pubmed publisher
..Furthermore, we show that selective and complete inhibition of Î²5i and Î²1i is cytotoxic to primary cells from acute lymphocytic leukemia (ALL) patients. ..