178 search results for “covalent ligands” in the Public website
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Determining the kinetic profile of ENT1 inhibitors
Supervisor: Anna Vlachodimou
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Receptor Residence Time
Research question
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Physicochemical analysis of allosteric binding pockets
Supervisor: Gerard van Westen
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Heterogenized molecular (pre)catalysts for water oxidation and oxygen reduction
Before the large scale use of renewable energy sources can be implemented in our society, the storage of electrical energy needs to be tackled. Storage the energy as hydrogen via the reduction of protons is a good option.
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Synthetic carbohydrate ligands for immune receptors
PhD Defence
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This Week's Discoveries | 12 November 2019
Lecture
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Luminescence and applications of lanthanoid coordination polymers
Promotor: E. Bouwman, Co-Promotor: S. Bonnet
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Iron complexes as electrocatalysts for the water oxidation reaction
In this dissertation, the synthesis and characterization of a series of iron complexes based on different ligand platforms are described.
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Metals in Catalysis, Biomimetics & Inorganic Materials
Coordination chemistry is the chemistry of metal atoms "coordinated" by other atoms, ions or molecules. Important challenges in the research on coordination and organometallic chemistry are to understand the relation between the ligand and metal complex structures and the (catalytic) properties of the…
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Prediction of binding kinetics
Supervisor: Gerard van Westen
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PhD Theses
A full overview of MCBIM PhD theses.
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Binding kinetics
A tantalizing concept that has emerged in our recent research is binding kinetics. An important parameter is residence time (RT), a direct reflection of how long a drug stays bound to its target. This parameter is of crucial importance, because drug action lasts only as long as the receptor-ligand complex…
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Degradome analysis of vaccines
The objective is to develop in vitro antigen degradation assays in order to mimic the fate of the antigen in vivo.
- Facilities
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Light-activatable metallodrugs and metal-functionalized liposomes
Metal-containing molecules combine geometrical features and a reactivity that are inherently different from that of organic molecules. My research focuses on light-activatable metal-based anticancer drugs and metal-functionalized liposomes. Light is a very selective way to activate photosensitive drugs…
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Redox catalysis for a sustainable energy infrastructure
The main research theme in the group of Dennis Hetterscheid is to understand and mimic bioinorganic multi-electron processes that are relevant to our future energy infrastructure. Reduction of protons generates hydrogen that can be used as a chemical fuel. Alternatively to gaseous hydrogen, the reduction…
- Martina Huber Lab (EPR Group)
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Design and application of dextran based cross-linked networks
This thesis describes the design, characterization and application of dextran based crosslinked network.
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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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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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Novel receptor concepts
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Proteochemometric modelling coupled to in silico target prediction
An integrated approach for the simultaneous prediction of polypharmacology and binding affinity/potency of small molecules.
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Light-activatable ruthenium-based anticancer prodrugs
Can light-activatable ruthenium compounds be used as a more selective anticancer treatment?
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Research
Research at the MCBIM group is comprised of the following research themes:
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Proteochemometrics
Research question
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Development of a Transgenic Mouse Model to Study the Immunogenicity of Recombinant Human Insulin
Mouse models are commonly used to assess the immunogenicity of therapeutic proteins and to investigate the immunological processes leading to antidrug antibodies. The aim of this work was to develop a transgenic (TG) Balb/c mouse model for evaluating the immunogenicity of recombinant human insulin (insulin)…
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Structural characterization of bacterial proteins involved in antibiotic resistance and peptidoglycan biosynthesis
This thesis describes the structural and biochemical characterization of the β-lactamase BlaC from Mycobacterium tuberculosis (Mtb), and the Alr and YlmE proteins from Streptomyces coelicolor A3(2).Mtb is the main cause of tuberculosis.
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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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Understanding functional dynamics and conformational stability of beta-glycosidases
Due to their central physiological roles in living organisms, retaining beta-glycosidases have been the subject of tremendous research efforts to examine their structure/function relation using numerous biophysical and biochemical approaches.
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Lipids as therapeutic targets for barrier repair in skin diseases
The skin is our natural barrier and lipids are a key part of this barrier. In the outer skin layer, the stratum corneum (SC), lipids form a densely organized structure dependent on the composition of these lipids.
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Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors
PhD Defence
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Caging ruthenium complexes with non-toxic ligands for photoactivated chemotherapy
PhD Defence
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Transition metal compounds with S/N-functionalized NHC ligands: structures, redox properties and electrocatalytic activity
PhD Defence
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Time is of the essence: investigating kinetic interactions between drug, endogenous neuropeptides and receptor
Promotor: A.P. IJzerman Co-promotor: L.H. Heitman
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Discovery of novel inhibitors to investigate diacylglycerol lipases and α/β hydrolase domain 16A
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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Biophysical characterization of membrane protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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Strategy
The division of Drug Discovery and Safety combines the former divisions Toxicology and Medicinal Chemistry.
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Tools and Data
Tools and Data of the department of Environmental Biology
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PNEC-pro
PNEC-pro is a user-friendly screening tool for professionals dealing with the assessment of surface water quality. The tool calculates local, watertype specific no-effect concentrations (PNEC) of copper, lead, nickel, and zinc based on biotic ligand models (BLMs).
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Development of a universal delivery system for tailor-made cancer vaccines
The potential of liposomal cancer vaccines
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Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor
Animal models suggest that the chemokine ligand 2/CC-chemokine receptor 2 (CCL2/CCR2) axis plays an important role in the development of inflammatory diseases. However, CCR2 antagonists have failed in clinical trials because of a lack of efficacy.
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Chemical tools to modulate endocannabinoid biosynthesis
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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Quantifying the toxicity of mixtures of metals and metal-based nanoparticles to higher plants
Promotores: Prof.dr. W.J.G.M. Peijnenburg & Dr. M.G. Vijver
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Applications of paramagnetic NMR spectroscopy for protein research
The aim of the research presented in this thesis was to develop new methods forchallenging systems in liquid-state NMR using paramagnetic effects generated by thetwo-armed probe CLaNP-5.
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Gold nanoparticle-peptide conjugates for biomedical applications
Despite the fact that gold nanoparticles (GNPs) are one of the most studied nanoparticles, there is still a necessity for new approaches allowing for effective protective coating to enable wider use of GNPs in biomedical applications.
- Vacancies
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Selectivity
Target selectivity is an important aspect of any drug molecule, and certainly a parameter to be optimized. That is not trivial for a number of reasons. First of all hundreds of drug targets (receptors, enzymes, ion channels) exist, and no single lab in the world has assays for all of them.
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Reedijk Symposium 2015 - Guest Lecturers: Prof. Bas de Bruin & Prof. Dame Carol Robinson
On Friday October 30th 2015 the sixth annual Jan Reedijk Symposium will be held. The main lectures of the day will be "Catalytic Radical-Type Transformations; Catalytic Reactivity of Carbene and Nitrene Radicals" by invited speaker Prof. Bas de Bruin (UvA), and "Structural biology in the gas phase –…
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Self adjuvanting immunopeptides: Design and synthesis
Chapter 2 describes a post-synthetic methodology to introduce a fluorescent label in highly lipophilic, Pam3Cys based conjugates.
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Structure-affinity relationships (SARs) and structure-kinetics relationships (SKRs) of Kv11.1 blockers
Source: J Med Chem (2015)