1,205 search results for “activity-based profiling” in the Public website
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Activity-Based Proteasome Profiling
Promotor: H.S. Overkleeft, Co-promotor: B.I. Florea
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Activity-based protein profiling of diacylglycerol lipases
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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Activity-based protein profiling in drug discovery
In the last decades, activity-based protein profiling (ABPP) has emerged as a powerful chemical tool that may aid the ever-challenging drug discovery process.
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Fluorescence Polarization Activity-Based Protein Profiling on Retaining Glycosidases
Glycosidases are important enzymes in the turnover of polysaccharides and glycoconjugates, and are involved in a range of human pathologies including genetic disorders such as Gaucher and Pompe disease, but also in various cancers.
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Activity-based protein profiling of glucosidases, fucosidases and glucuronidases
Promotores: H.S. Overkleeft, G.A. van der Marel, Co-promotor: B.I. Florea
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Bioorthogonal Chemistry: Applications in Activity-Based Protein Profiling
The close interaction between organic chemi stry and biology goes back to the late 18th century, when the modern natural sciences began to take shape. After synthetic organic chemistry arose as a discipline, organic chemists almost immediately began to pursue the synthesis of naturally occurring compounds,…
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Activity-based protein profiling for drug discovery
Activity-based protein profiling (ABPP, also termed chemical proteomics), is one of the pillars of chemical biology, and at LED3 we have taken it to the next level. ABPP allows the assessment of protein function in live cells and tissues, which means that the activity of a complete protein family can…
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Direct and two-step activity-based profiling of proteases and glycosidases
Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel
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Relative quantification of proteasome activity by activity-based protein profiling and LC-MS/MS
Activity-based protein profiling (ABPP) is a functional proteomics technique for directly monitoring the expression of active enzymes in cell extracts and living cells. The technique relies on irreversible inhibitors equipped with reactive groups (warheads) that covalently attach to the active site…
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Activity-based proteomics of the endocannabinoid system
This thesis describes the use of an activity-based proteomics method to study the endocannabinoid system.
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Design and development of conformational inhibitors and activity-based probes for retaining glycosidases
Glycosidases are essential in fundamental biological processes and are responsible for the degradation of most (oligo)saccharides, glycolipids and glycoproteins.
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Development of kinase inhibitors and activity-based probes
Promotor: H.S. Overkleeft, J. Neefjes, Co-promotor: M. van der Stelt
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Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474, SCIENCE, 2017
The drug BIA 10-2474 inhibits fatty acid amide hydrolase (FAAH), a lipase that degrades a specific endocannabinoid. On the basis of this activity, BIA 10-2474 was being developed as a potential treatment for anxiety and pain. In a phase 1 trial of the drug, one subject died, and four others suffered…
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Novel Activity-Based Probes for Broad-Spectrum Profiling of Retaining β-Exoglucosidases In Situ and In Vivo
A high-end label: Cyclophellitol aziridine-type activity-based probes allow for ultra-sensitive visualization of mammalian β-glucosidases (GBA1, GBA2, GBA3, and LPH) as well as several non-mammalian β-glucosidases (see picture). These probes offer new ways to study β-exoglucosidases, and configurational…
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Inhibitor Selectivity: Profiling and Prediction
Less than 1 in 10 drug candidates that enter phase 1 clinical trials actually gets approved for human use.
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Applications for activity-based probes in biomedical research on glycosidases
Lysosomal glycosidases are acid hydrolases that fragment glycoconjugates in lysosomes.
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Cyclophellitol analogues for profiling of exo- and endo-glycosidases
To this day, all cyclophellitol-based inhibitors and ABPs have been close analogues of their natural substrate counterparts. As a result, these probes showed high selectivity towards their target glycosidases.
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Inhibitors and probes targeting endo-glycosidases
The chemical synthesis of inhibitors and probes targeting endo-glycosidases.
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Hermen Overkleeft
Science
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Berend Gagestein
Science
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Chi-Lin Kuo
Science
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Visualization of Vitamin A Metabolism
Vitamin A or retinol is essential in embryonic development, the visual cycle and the immune system.
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Profile
What are the values that Leiden University cherishes? What does the University stand for and what does it consider important?
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International profile
Leiden University has been an international university from its founding in 1575.
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The use of activity based protein profiling to study proteasome biology
Promotor: H.S. Overkleeft, Co-Promotor: B.I. Florea
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Profile of students
Students are educated to become academic professionals and responsible and engaged citizens who are internationally and interculturally competent
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The reintegration of high profile ex-offenders
The reintegration of high profile ex-offenders frequently receives great political and public attention. While this attention, more often than not in the form of negative sentiments, may be understandable from a moral perspective, it raises several important questions: how do such offenders reintegrate…
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Chemical tools to study lipid signaling
Synthesis and application of chemical biology tools to study immunomodulatory signaling lipids.
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Determining the kinetic profile of ENT1 inhibitors
Supervisor: Anna Vlachodimou
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Profile 3. Sources on Frisian medieval history
Due to the fact that the Frisian lands lacked major political centers in the Middle Ages and also because most of its monasteries suffered complete destruction in the second half of the 16th century, relatively few written documents concerning medieval Frisian history have survived. To analyze them…
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Profile 1. State formation in medieval Frisia
Politically speaking, the Frisian coastal area constitutes a special case in late medieval Europe since it was not subject to an overlord as it withstood feudalization in the 13th century. Its many sub regions, which were dominated by elites of small noblemen and freeholders, long time succeeded in…
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High-throughput profiling of small molecules using mass spectrometry
Promotor: Prof.dr. T. Hankemeier, Co-Promotor: R.J. Vreeken
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Kinetic profiling of positive allosteric modulators of the mGlu2 receptor
Supervisor: Maarten Doornbos
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Profiling Endophenotypes in Social Anxiety Disorder – a family study
The key question addressed in this family study is whether the psychophysiological and neurocognitive abnormalities often reported in SAD patients are heritable and can thus be found in family members of SAD patients as well. Determination of heritability of these deficiencies is essential for endophenotyping.…
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Post-doctoral researcher, social media analytics for algorithmic profiling
Science, Leiden Institute of Advanced Computer Science (LIACS)
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Chemical tools to modulate endocannabinoid biosynthesis
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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Profile 4. Monasteries and society in the Northern Netherlands
Since my master's thesis on the landed property of the Frisian monasteries in the Middle Ages I am highly interested in the do ut des-aspects of the relation between religious houses and the lay world. Key words here are: property, power, patronage and the role of religious institutions in the 'salvation…
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Fluorescence Polarization Activity-Based Protein Profiling on Retaining Glycosidases
PhD Defence
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Cyclophellitol and its derivatives: synthesis and application as beta-glycosidase inhibitors
Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel
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'Authentic Islam': The Religious Profile of Taqī al-Dīn al-Hilālī (1893-1987) as Reflected in his Fatwas
Abdessamad El Amraoui defended his thesis on 6 Mai 2015.
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Activity-based Protein Profiling of the Diacylglycerol Lipases
PhD Defence
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Activity-based protein profiling in drug discovery
PhD Defence
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Activity-based protein profiling of glucosidases, fucosidases and glucuronidases
PhD Defence
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Digitizing security: How digital risk-profiling is developed in practice
How are digital risk-profiles developed and used in practice?
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A chemical biology approach for targeting of ligand-drug conjugates
Promotores: Prof.dr. H. S. Overkleeft, Prof.dr. G. A. van der Marel
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Activity-based protein profiling and bio-orthogonal chemistry
Conference
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Cannabinoid receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands
Supervisor: Andrea Martella
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Immunoproteomic Profiling of Bordetella pertussis Outer Membrane Vesicle Vaccine Reveals Broad and Balanced Humoral Immunogenicity
The current resurgence of whooping cough is alarming, and improved pertussis vaccines are thought to offer a solution. Outer membrane vesicle vaccines (omvPV) are potential vaccine candidates, but omvPV-induced humoral responses have not yet been characterized in detail.
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LC/MS-platform for analysis of all major stratum corneum lipids, and the profiling of skin substitutes
Ceramides (CERs), cholesterol, and free fatty acids (FFAs) are the main lipid classes in human stratum corneum (SC, outermost skin layer), but no studies report on the detailed analysis of these classes in a single platform.
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New cellular imaging paves way for cancer treatment
A new technique using fluorescent imaging to track the actions of enzymes might aid drug design for new anti-cancer, inflammation and kidney disease treatments. Researchers at the University of York and Leiden University have published these findings in Nature Chemical Biology.