1720 search results for “activity-based protein profiling” in the Public website
-
Activity-based protein profiling of diacylglycerol lipases
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
-
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.
-
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.
-
Activity-based protein profiling of glucosidases, fucosidases and glucuronidases
Promotores: H.S. Overkleeft, G.A. van der Marel, Co-promotor: B.I. Florea
-
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,…
-
Activity-Based Proteasome Profiling
Promotor: H.S. Overkleeft, Co-promotor: B.I. Florea
-
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…
-
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…
-
Activity-based proteomics of the endocannabinoid system
This thesis describes the use of an activity-based proteomics method to study the endocannabinoid system.
-
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.
-
Direct and two-step activity-based profiling of proteases and glycosidases
Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel
-
Development of kinase inhibitors and activity-based probes
Promotor: H.S. Overkleeft, J. Neefjes, Co-promotor: M. van der Stelt
-
Inhibitor Selectivity: Profiling and Prediction
Less than 1 in 10 drug candidates that enter phase 1 clinical trials actually gets approved for human use.
-
Applications for activity-based probes in biomedical research on glycosidases
Lysosomal glycosidases are acid hydrolases that fragment glycoconjugates in lysosomes.
-
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.
-
Hermen Overkleeft
Science
-
Berend Gagestein
Science
-
Development of an Activity-Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase-α in Brain, Angew. Chem
A model method: A strategy that combines a knowledge-based in silico design approach and the development of novel activity-based probes (ABPs) for the detection of endogenous diacylglycerol lipase-α (DAGL-α) is presented. This approach resulted in the rapid identification of new DAGL-α inhibitors with…
-
The use of activity based protein profiling to study proteasome biology
Promotor: H.S. Overkleeft, Co-Promotor: B.I. Florea
-
Chi-Lin Kuo
Science
-
Visualization of Vitamin A Metabolism
Vitamin A or retinol is essential in embryonic development, the visual cycle and the immune system.
-
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…
-
Chemical tools to study lipid signaling
Synthesis and application of chemical biology tools to study immunomodulatory signaling lipids.
-
Protein Facility
The Protein Centre can supply you with purified proteins that are essential for many experiments, ranging from in vitro inhibitor screening and enzymatic analysis to manipulation of life cells.
-
Spin-label EPR Approaches to Protein Interactions
Promotor: Prof.dr. E.J.J. Groenen
-
Unravelling proteins by touch
How can we develop a new microscope that can distinguish individual atoms in proteins?
-
Morphogenesis and protein production in Aspergillus niger
Promotor: Prof.dr. C.A.M.J.J. van den Hondel, Dr. ir. V. Meyer, Co-promotor: Dr. A.F.J. Ram
-
A chemical biology approach for targeting of ligand-drug conjugates
Promotores: Prof.dr. H. S. Overkleeft, Prof.dr. G. A. van der Marel
-
Oxidation of Therapeutic Proteins and Peptides: Structural and Biological Consequences
Oxidation is a common degradation pathway that affects therapeutic proteins and peptides during production, purification, formulation, transportation, storage and handling of solid and liquid preparations. In the present work we review the scientific literature about structural and biological consequences…
-
Profile
What are the values that Leiden University cherishes? What does the University stand for and what does it consider important?
-
Profile
The philosophers at the Institute of Philosophy develop new perspectives and insights not only on fundamental philosophical questions, but also on topical and interdisciplinary themes such as secrecy, migration, and climate change.
-
NMR studies of protein-small molecule and protein-peptide interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
-
International profile
Since its beginning, Leiden University has been one of Europe's leading international research-intensive universities.
-
NMR structural studies of protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
-
Determining the kinetic profile of ENT1 inhibitors
Supervisor: Anna Vlachodimou
-
Fluorescence Polarization Activity-Based Protein Profiling on Retaining Glycosidases
PhD Defence
-
Molecular engineering of plant development using Agrobacterium-mediated protein translocation
Supervisor: P.J.J. Hooykaas Co-Supervisor: R. Offringa
-
Pharmaceutical Aspects of Subvisible Particles in Protein Formulations
Promotor: W. Jiskoot, Co-promotor: A. Hawe
-
Activity-based Protein Profiling of the Diacylglycerol Lipases
PhD Defence
-
Activity-based protein profiling in drug discovery
PhD Defence
-
Activity-based protein profiling of glucosidases, fucosidases and glucuronidases
PhD Defence
-
Biophysical characterization of membrane protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
-
Visualization of effector protein translocation from Agrobacterium tumefaciens into host cells
In our research protein translocation from Agrobacterium into yeast and plant cells is studied to obtain fundamental insights in the translocation process
-
Activity-based protein profiling and bio-orthogonal chemistry
Conference
-
solvent free supercritical fluid spray drying process for producing dry protein formulations
In this study, we evaluated the influence of supercritical carbon dioxide (scCO2) spray drying conditions, in the absence of organic solvent, on the ability to produce dry protein/trehalose formulations at 1:10 and 1:4 (w/w) ratios.
-
Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors
The present thesis focuses on the pharmacological concept of drug-target interaction, which dates back to the beginning of modern pharmacology.
-
Protein motions revealed by paramagnetic NMR spectroscopy
Hass
-
CRISPR Cas-induced targeted mutagenesis with Agrobacterium mediated protein delivery
The RNA guided endonuclease based on the CRISPR/Cas system of Streptococcus pyogenus is a potent new tool for genome engineering in plants.
-
between the adenosine A2B receptor and the C-terminus of different G protein α-subunits.
Source: Purinergic Signal., Volume 10, Issue 3, pp. 441-53 (2014)
-
Molecular Physiology
Molecular Physiology is a research group at the Leiden Institute of Chemistry, headed by Prof. Mario van der Stelt. The research aim is to design, synthesize and apply new chemical tools to answer important biological and medical questions. We use activity-based protein profiling, assay development,…