Herman S Overkleeft


Affiliation: Leiden University
Country: The Netherlands


  1. 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. ..
  2. 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. ..
  3. Jiang J, Beenakker T, Kallemeijn W, van der Marel G, van den Elst H, Codée 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. ..
  4. 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
  5. Kallemeijn W, Witte M, Voorn Brouwer T, Walvoort M, Li K, Codée J, et al. A sensitive gel-based method combining distinct cyclophellitol-based probes for the identification of acid/base residues in human retaining β-glucosidases. J Biol Chem. 2014;289:35351-62 pubmed publisher
    ..The described method is highly sensitive, requiring only femtomoles (nanograms) of ABP-labeled enzymes. ..
  6. 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. ..
  7. 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. ..
  8. 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
  9. 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 β5i and β1i is cytotoxic to primary cells from acute lymphocytic leukemia (ALL) patients. ..

More Information


  1. Xin B, Schimmack G, Du Y, Florea B, van der Marel G, Driessen C, et al. Development of new Malt1 inhibitors and probes. Bioorg Med Chem. 2016;24:3312-29 pubmed publisher
    ..Furthermore, two of our inhibitors (9, apparent IC50 3.0?M, and 13, apparent IC50 2.1?M) show good inhibitory activity against Malt1 and outperform MI-2 (apparent IC50 7.8?M) in our competitive activity-based protein profiling assay. ..
  2. Schröder S, van de Sande J, Kallemeijn W, Kuo C, Artola M, van Rooden E, et al. Towards broad spectrum activity-based glycosidase probes: synthesis and evaluation of deoxygenated cyclophellitol aziridines. Chem Commun (Camb). 2017;53:12528-12531 pubmed publisher
    ..Here, a set of deoxygenated cyclophellitols are presented which enable inter-class profiling of β-glucosidases and β-galactosidases. ..