187 zoekresultaten voor “activity” in de Publieke website
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Activity-Based Proteasome Profiling
Promotor: Prof.dr. H.S. Overkleeft
- Interdisciplinary Activity Grants
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Photocleavable activity-based acid glucosylceramidase probes
Lysosomal acid glucosylceramidase (GBA1) is a lysosomal enzyme that degrades glucolipids with its main substrate being glucosylceramide (GlcCer). Defects in the GBA1 gene lead to glycosphingolipidosis Gaucher disease (GD), in which the hydrolysis of GlcCer is impaired and therefore, it accumulates in…
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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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Increased striatal activity in adolescence benefits learning
De verhoogde activatie van het striatum, die adolescenten laten zien bij beloning, wordt meestal in verband gebracht met risicogedrag en negatieve gezondheidseffecten. In dit artikel in Nature Communications wordt een mogelijke positieve kant van die verhoogde activatie onderzocht. De activatiepiek…
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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 of glucosidases, fucosidases and glucuronidases
Promotores: H.S. Overkleeft, G.A. van der Marel, Co-promotor: B.I. Florea
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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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Development of kinase inhibitors and activity-based probes
Promotor: H.S. Overkleeft, J. Neefjes, Co-promotor: M. van der Stelt
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Pair configurations to molecular activity coefficients: PAC-MAC
This thesis provides an overview of the development of the Pair Configuration to Molecular Activity Coefficient (PAC-MAC) model.
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biosynthesis in Streptomyces: engineering, resistance and antimicrobial activity
Actinobacteria are well known for the production of bioactive natural products, many of which have applications in the fields of human, animal and plant health. Subject of this thesis are the anthracyclines, glycosylated aromatic polyketides with potent anticancer activity.
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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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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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Applications for activity-based probes in biomedical research on glycosidases
Lysosomal glycosidases are acid hydrolases that fragment glycoconjugates in lysosomes.
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The relation between dynamics and activity of phospholipase A/acyltransferase homologs
Phospholipase A/acyltransferase 3 (PLAAT3) and PLAAT4 are enzymes involved in the synthesis of bioactive lipids. Despite sequential and structural similarities, the two enzymes differ in activity and specificity.
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metallo-proteins for photocatalytic water splitting: stability and activity in artificial photosynthesis
Climate change is one of the largest challenges faced by humanity. To combat this research into alternatives to fossil fuels is ongoing. Dihydrogen is considered a good alternative fuel, since its burning only forms water.
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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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Inhibitors and activity-based probes for β-D-glucuronidases, heparanases and β-L-arabinofuranosidases
Glycosidases (GHs) are enzymes responsible for the degradation of carbohydrates and play many roles in human health and pathophysiology. Often, abnormal levels of glycosidase activity are markedly linked to human pathologies.
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Exploring and exploiting activity-based protein profiling in chemical biology and medicinal chemistry
Overkleeft
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Development of Quantitative Nanostructure Activity Relationship (QNAR) Models Predicting the Toxicity of Metal-based Nanoparticles to Aquatic
Describe and identify what dosimetry parameters are of importance to interpret dose-response relationships (eg., mortality, sub-lethal, growth or reproduction inhabitation, DNA damage and reactive oxygen species, etc. ) for metal-based nanoparticles? How to develop quantitative models that enable to…
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S/N-functionalized NHC ligands: structures, redox properties and electrocatalytic activity
The research described in this thesis focused on the preparation of S/N functionalized carbene ligands and their transition metal complexes, and the exploration of their application as electrocatalysts for proton reduction.
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the AT-HOOK MOTIF NUCLEAR LOCALIZED 15 gene in Arabidopsis meristem activity and longevity
Plant architecture has distinct forms in different plant species, but also within a species the finalarchitecture of a plant is determined by its gradual development and changes therein induced by environmental conditions during the plant’s life cycle.
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Exploring chemical space in covalent and competitive glycosidase inhibitor design
Glycoside hydrolases (glycosidases/GHs) are widely abundant enzymes in all kingdoms of life and are important biocatalysts that catalyze the hydrolysis of glycosidic linkages in oligo/polysaccharides, glycoproteins and glycolipids with tremendous efficiency
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Chemical tools to modulate endocannabinoid biosynthesis
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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444 Interdisciplinary Activity Grant voor Alex Brandsen en Wouter Verschoof-van der Vaart
Alex Brandsen en Wouter Verschoof-van der Vaart, promovendi bij de onderzoeksgroep Digital Archaeology en het Data Science Research Programme, hebben een 444-beurs van de Young Academy Leiden ontvangen. Hiermee gaan ze in Oxford een sessie houden om de samenwerking te verbeteren tussen onderzoekers…
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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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Chemical Tools to Illuminate N-acylphosphatidylethanolamine Biosynthesis
This thesis describes the development and optimization of the first molecular tools to study the enzyme PLA2G4E.
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Environmental and metabolomic study of antibiotic production by actinomycetes
Promotor: Prof.dr. G.P. van Wezel
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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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Do fungi differ? Understanding the mechanisms of mycorrhizal fungal impacts on soil C sequestration
How presence, abundance and enzymatic activities of AM and EM fungi differently affect soil carbon sequestration processes?
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Inhibitors and probes targeting endo-glycosidases
The chemical synthesis of inhibitors and probes targeting endo-glycosidases.
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Inhibitors and probes targeting mannanases
This thesis describes the synthesis and biochemical evaluation of a variety of cyclophellitol based activity-based probes and inhibitors targeting various endo- and exo-acting retaining glycosidases. In the last two decades a variety of probes and inhibitors for (hemi)cellulose degrading enzymes have…
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Semisynthetic glycopeptide antibiotics
Vancomycin is a last-resort antibiotic for the treatment of many Gram-positive bacterial infections, while remaining inactive against Gram-negative strains.
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Applications of Natural Deep Eutectic Solvents to Extraction and Preservation of Biomolecules
The recently introduced nature-originated deep eutectic solvents, so-called natural deep eutectic solvents (NADES) are considered as truly green solvents, which composed of natural ingredients found abundantly in organisms.
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Mechanism-based inhibitors and probes for neuraminidases
Neuraminidases are enzymes that cleave glycosidic linkages of sialic acid. These enzymes are involved in influenza infections as well as in many cellular processes in mammals and micro-organisms.
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Chemical functionalization of the graphene surface for electrical and electrochemical sensing application
Advanced sensing techniques require graphene with high quality and well-controlled surface chemistry.
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Macrophages inhibit human osteosarcoma cell growth after activation with the bacterial cell wall derivative liposomal muramyl tripeptide in combination
CONCLUSION: This study demonstrates that human macrophages can be induced to exert direct anti-tumor activity against osteosarcoma cells. Our observation that the induction of macrophage anti-tumor activity by L-MTP-PE required IFN-gamma may be of relevance for the optimization of L-MTP-PE therapy in…
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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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Using soil inoculations for ecological restorations
How soil microbial composition impacts structure and composition of the aboveground plant and animal communities?
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Inhibitor discovery of phospholipases and N-acyltransferases
In this thesis an activity-based probe was discovered that could visualize the activity of PLAATs. With an optimized gel-based ABPP assay in hand, screening of a compound library led to the discovery of alpha-ketoamides as a hit for PLAAT3.
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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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Peptide-based probes for protein N-Methyltransferases
The work described in this thesis focuses on the development of linear or cyclized peptide probes against protein N-methyltransferases to characterize their specific binding behavior, providing further binding details for inhibitory activity study.
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More JAZ in the orchestration of jasmonate-mediated plant defense
Prof.dr. J. Memelink
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New polymyxin antibiotics for old problems: addressing nephrotoxicity and resistance
Polymyxins are clinically used antibiotics, discovered in mid-20th century. Once abandoned due to excessive nephrotoxicity, they are now used increasingly to address infections caused by multi-drug resistant Gram-negative bacteria.In this thesis, we describe the development and synthesis of analogues…
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Substrate adaptability of β-lactamase
The research aims to explore the evolutionary adaptability of enzymes and the impact of temperature on protein evolution pathways, using M. tuberculosis β-lactamase BlaC as the object of study. Enzymes inherently embody a delicate balance between activity and stability, and the acquisition of new enzymatic…
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Illuminating N-acylethanolamine biosynthesis with new chemical tools
In this thesis, the discovery and optimization is described of chemical tools to study the N-acylethanolamine (NAE) biosynthetic pathway.
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Discovery of Reversible Monoacylglycerol Lipase Inhibitors
Monoacylglycerol lipase (MAGL) is the principal enzyme responsible for hydrolysis of the endocannabinoid 2-arachidonoylglycerol (2-AG). MAGL inhibition provides several potential therapeutic opportunities, including anti-nociceptive, anti-inflammatory and anti-cancer activity.
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Next generation lipopeptide antibiotics
This thesis describes the evaluation of novel natural products with antibacterial activity enabled by total chemical synthesis.
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Structural and functional analysis of proteins involved in natural product biosynthesis and morphological differentiation in Streptomyces
Streptomyces present a valuable platform for natural product discovery. Lugdunomycin is a novel angucycline-derived polyketide from Streptomyces sp QL37, with unprecedented skeleton and antimicrobial activity.