User profiles for H. S. Overkleeft

HS Overkleeft

Professor of Bio-organic Synthesis, Leiden University
Verified email at lic.leidenuniv.nl
Cited by 31629

[PDF][PDF] Proteasome inhibitors: an expanding army attacking a unique target

AF Kisselev, WA van der Linden, HS Overkleeft - Chemistry & biology, 2012 - cell.com
Proteasomes are large, multisubunit proteolytic complexes presenting multiple targets for
therapeutic intervention. The 26S proteasome consists of a 20S proteolytic core and one or two …

Thioglycosides in sequential glycosylation strategies

…, REJN Litjens, LJ van den Bos, HS Overkleeft… - Chemical Society …, 2005 - pubs.rsc.org
This tutorial review surveys the use of thioglycosides in the development of sequential
glycosylation methodologies, with a focus on chemoselective, orthogonal and iterative …

Glycosphingolipids—nature, function, and pharmacological modulation

…, GA van der Marel, HS Overkleeft… - Angewandte Chemie …, 2009 - Wiley Online Library
The discovery of the glycosphingolipids is generally attributed to Johan LWThudichum, who
in 1884 published on the chemical composition of the brain. In his studies he isolated …

[HTML][HTML] A novel active site‐directed probe specific for deubiquitylating enzymes reveals proteasome association of USP14

…, BM Kessler, R Casagrande, HS Overkleeft… - The EMBO …, 2001 - embopress.org
AC‐terminally modified ubiquitin (Ub) derivative, ubiquitin vinyl sulfone (UbVS), was
synthesized as an active site‐directed probe that irreversibly modifies a subset of Ub C‐terminal …

Pharmacological inhibition of glucosylceramide synthase enhances insulin sensitivity

…, T Wennekes, JK Sethi, S O'Rahilly, HS Overkleeft - Diabetes, 2007 - Am Diabetes Assoc
A growing body of evidence implicates ceramide and/or its glycosphingolipid metabolites in
the pathogenesis of insulin resistance. We have developed a highly specific small molecule …

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474

…, BI Florea, G Hendriks, L De Petrocellis, HS Overkleeft… - Science, 2017 - science.org
A recent phase 1 trial of the fatty acid amide hydrolase (FAAH) inhibitor BIA 10-2474 led to
the death of one volunteer and produced mild-to-severe neurological symptoms in four others…

Ultrasensitive in situ visualization of active glucocerebrosidase molecules

…, RG Boot, GA Van Der Marel, HS Overkleeft… - Nature chemical …, 2010 - nature.com
Deficiency of glucocerebrosidase (GBA) underlies Gaucher disease, a common lysosomal
storage disorder. Carriership for Gaucher disease has recently been identified as major risk …

Ph2SO/Tf2O:  a Powerful Promotor System in Chemoselective Glycosylations Using Thioglycosides

…, REJN Litjens, R den Heeten, HS Overkleeft… - Organic …, 2003 - ACS Publications
Diphenylsulfoxide in combination with triflic anhydride provides a very potent thiophilic
glycosylation promotor system, capable of activating disarmed thioglycosides. The usefulness of …

Analysis of protease activity in live antigen-presenting cells shows regulation of the phagosomal proteolytic contents during dendritic cell activation

…, R Maehr, E Fiebiger, HS Overkleeft… - The Journal of …, 2002 - rupress.org
Here, we describe a new approach designed to monitor the proteolytic activity of maturing
phagosomes in live antigen-presenting cells. We find that an ingested particle sequentially …

[HTML][HTML] Generation of specific deoxynojirimycin-type inhibitors of the non-lysosomal glucosylceramidase

HS Overkleeft, GH Renkema, J Neele… - Journal of Biological …, 1998 - ASBMB
The existence of a non-lysosomal glucosylceramidase in human cells has been documented
(van Weely, S., Brandsma, M., Strijland, A., Tager, JM, and Aerts, JMFG (1993) Biochim. …