157 search results for “polypyridyl ligands” in the Public website
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Mononuclear spin-transition materials based on the bapbpy scaffold
Promotor: E. Bouwman, Co-Promotor: S. Bonnet
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Synthetic carbohydrate ligands for immune receptors
One of the main challenges in the development of an effective anti-cancer vaccine is the generation of an adequate and directed cellular immune response.
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Biotic ligand models
Description of Biotic ligand models: making an inventory of available models & assessment of the variability of the predicted HC5 using the BLMs in different Dutch water types (2005 - 2007)
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The ins and outs of ligand binding to CCR2
Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: Dr. L.H. Heitman
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Better ligands for G Protein-Coupled Receptors
The receptor nomenclature committee of IUPHAR, the International Union of Pharmacology, has several subgroups. Among these are a few that our division is involved in, those for adenosine, nicotinic acid, and GnRH receptors.
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The power of biotic ligand models : site-specific impact of metals on aquatic communities
Promotor: Prof.dr. G.R. de Snoo, Co-promotores: Dr. ing. M.G. Vijver, J.P.M. Vink
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cobalt(II)-dichalcogenide complexes: correlation between redox conversion and ligand-field strength
The redox-conversion reaction of metal-disulfide and metal-thiolate complexes are important, as they may shed light on electron-transfer reactions that often occur in Nature.
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Caging ruthenium complexes with non-toxic ligands for photoactivated chemotherapy
The main goal of the research described in this thesis was the development of new photoactivated chemotherapy (PACT) ruthenium(II) complexes bearing a non-toxic photolabile ligand.
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Transition metal compounds with 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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receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands
Supervisor: Andrea Martella
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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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Lipid bilayers decorated with photosensitive ruthenium complexes
Promotor: E. Bouwman, Co-promotor: S. Bonnet
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Aurea? Structure-enabled approaches of identifying and optimizing GPCR ligands
Promotores: A.P. IJzerman, H.W.T. van Vlijmen
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Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity, Nat. Commun., 2017
The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB2R, their selectivity, molecular mode of action and pharmacokinetic properties have…
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Corpora Non 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.
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Allosteric modulation and ligand binding kinetics at the Kv11.1 channel
Promotor: Prof.dr. A.P. IJzerman, Co-Promotor: L.H. Heitman
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Polyfluorinated bis-styrylbenzenes as amyloid-beta plaque binding ligands
Detection of cerebral beta-amyloid (Abeta) by targeted contrast agents remains of great interest to aid the in vivo diagnosis of Alzheimer's disease (AD). Bis-styrylbenzenes have been previously reported as potential Abeta imaging agents.
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Indanes-Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors
The indane (2,3-dihydro-1H-indene) ring system is an attractive scaffold for biologically active compounds due to the combination of aromatic and aliphatic properties fused together in one rigid system.
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Imaging of alkyne-functionalized ruthenium complexes for photoactivated chemotherapy
In photoactivated chemotherapy (PACT), a biologically active compound is caged by a light-cleavable protecting group.
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Natalia Ortiz Zacarias
Science
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The road to insurmountability: Novel avenues to better target CC Chemokine receptors
This thesis explores different avenues to develop insurmountable antagonists for CC Chemokine Receptors, such as CCR1, CCR2 and CCR5.
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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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Synthesis of cyclic peptides as bioconjugation platforms
Cyclic peptides are investigated as a platform to induce different orientations between various ligands.
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PhD Theses
A full overview of MCBIM PhD theses.
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NMR studies of protein-small molecule and protein-peptide interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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NMR structural studies of protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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Targeting the adenosinergic system
Adenosine is an endogenous ligand which exerts its action by activating adenosine receptors (ARs), while its circulating levels are controlled via a variety of mechanism and proteins, amongst others the equilibrative nucleoside transporters (ENTs).
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Photo-activation of ruthenium-decorated upconverting nanoparticles
Metal-based prodrugs based on ruthenium(II) polypyridyl complexes have proven to be very suitable for application in both photodynamic therapy (PDT) and photo-activated chemotherapy (PACT).
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Quantitative modelling of the response of earthworms to metals
Promotor: Prof.dr. W.J.G.M. Peijnenburg, Co-promotor: Dr. ing. M.G. Vijver
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CD40-targeted dendritic cell delivery of PLGA-nanoparticle vaccines induce potent anti-tumor responses
Dendritic cells (DC) play a prominent role in the priming of CD8(+) T cells. Vaccination is a promising treatment to boost tumor-specific CD8(+) T cells which is crucially dependent on adequate delivery of the vaccine to DC.
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Medicinal Chemistry
The mission in this research group, headed by Ad IJzerman, is to design and synthesize novel and better ligands for drug targets. Drug discovery is a lengthy but inspiring adventure. It is often an interplay between academic institutes and pharmaceutical industry, in which scientists at university develop…
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The good? The bad? The mutant! Characterization of cancer-related somatic mutations and identification of a selectivity hotspot in adenosine
G protein-coupled receptors (GPCRs), one of the largest families of membrane proteins, are responsive to a diverse set of physiological endogenous ligands including hormones and neurotransmitters.
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Liposome-based synthetic long peptide vaccines for cancer immunotherapy
Promotores: Wim Jiskoot; Ferry Ossendorp
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Kinetics for Drug Discovery: a Case for the Adenosine A3 receptor
Supervisor: Lizi Xia
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Redox Interconversion between Metal Thiolate and Disulfide Compounds
In the last decade, the redox interconversion between metal thiolate and disulfide compounds has been extensively investigated for copper, but not for other transition metal ions.
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Allosteric modulation by sodium ions and amilorides of G protein-coupled receptors
Promotor: A.P. IJzerman
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Allosteric modulation by sodium ions and amilorides of G protein- coupled receptors
Promotor: A.P. IJzerman
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Sodium ion binding pocket mutations and adenosine A2A receptor function
Source: Mol Pharmacol, Volume 87, Issue 2, pp. 305-13 (2015)
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Paradigm-shifting theory highlights the importance of substrate flexibility in enzymatic reactions
Leiden chemists have proposed a new model for enzymatic reactions, in which the flexibility of the substrate is much more important than previously thought. Their results are paradigm-shifting and could have major implications for drug research and enzyme engineering. Publication in Angewandte Chemi…
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Advances in GPCR Modeling Evaluated by the GPCR Dock 2013 Assessment: Meeting New Challenges
Source: Structure , Volume 22, Issue 8, pp. 1120-1139 (2014)
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Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists
Source: Eur J Med Chem, Volume 101, pp. 681-91 (2015)
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Allosteric Modulation
Allosteric modulation has long been recognized as a general and widespread mechanism for the control of protein function. Modulators bind to regulatory sites distinct from the active site on the protein, resulting in conformational changes that may profoundly influence protein function. This concept…
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Metals for Catalysis and Sustainability
Central in coordination and organometallic chemistry is the synthesis of new chelating ligands, the synthesis and characterization of metal complexes with these ligands, and the study of their properties. An important goal in my research is to create understanding of the relation between the structures…
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Drug-target residence time: a case for the adenosine A1 and A2A receptors
Promotor: Prof.dr. A.P. IJzerman, Co-Promotor: Dr. L.H. Heitman
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Determining the kinetic profile of ENT1 inhibitors
Supervisor: Anna Vlachodimou
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Physicochemical analysis of allosteric binding pockets
Supervisor: Gerard van Westen
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Receptor Residence Time
Research question
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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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Upconverting nanovesicles for the activation of ruthenium anti-cancer prodrugs with red light
Promotor: E. Bouwman, Co-promotor: S. Bonnet