178 zoekresultaten voor “covalent ligands” in de Publieke website
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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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Covalent inhibitors of G protein-coupled receptors: the case of adenosine receptors
Supervisor: Xue Yang
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Natalia Ortiz Zacarias
Wiskunde en Natuurwetenschappen
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Non-covalent Interactions
Many biological processes occur by biomolecules coming together and organizing into specific clusters without being bound to each other. These interactions range from clustering, transiently interacting (kiss and run), or assembling to multimeric units that can only function in conjunction. The hydrogen…
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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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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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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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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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Assistant Professor in Ligand and (Pro)Drug Development
Wiskunde en Natuurwetenschappen, Leiden Academic Centre for Drug Research (LACDR)
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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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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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Aurea? Structure-enabled approaches of identifying and optimizing GPCR ligands
Promotores: A.P. IJzerman, H.W.T. van Vlijmen
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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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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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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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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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Towards improved drug action : target binding kinetics and functional efficacy at the mGlu2 receptor
During the course of drug discovery translational steps are made.
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Lipid bilayers decorated with photosensitive ruthenium complexes
Promotor: E. Bouwman, Co-promotor: S. Bonnet
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Mononuclear spin-transition materials based on the bapbpy scaffold
Promotor: E. Bouwman, Co-Promotor: S. Bonnet
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Chemical tools to monitor and control human proteasome activities
Promotores: H.S. Overkleeft; G.A. van der Marel Co-Promotor: B.I. Florea
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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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Anna Vlachodimou
Wiskunde en Natuurwetenschappen
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Tom van der Wel
Wiskunde en Natuurwetenschappen
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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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Fundamental Research in Chemical Biology
Chemical biology research at the Leiden Institute of Chemistry is aimed at understanding biological processes at the molecular level to strengthen the knowledge base of human health and disease. The approach to achieve this goal is a fundamental chemical one; with the aid of chemical probes biological…
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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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Chemical Biology
Chemical biology research at the Leiden Institute of Chemistry is aimed at understanding biological processes at the molecular level to strengthen the knowledge base of human health and disease. The approach to achieve this goal is a fundamental chemical one; with the aid of chemical probes biological…
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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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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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Supramolecular materials: from biosensors to cell delivery devices
The group of Dr. Roxanne Kieltyka designs and synthesizes molecules that self-assemble into polymeric materials using specific non-covalent interactions. These substrates can be used for numerous applications in medicine ranging from disease detection to cell delivery depending on the (bio)molecular…
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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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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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Chemical genetic approaches for target validation
Drug development is a time- and resource-consuming process that starts with the discovery and validation of a (protein) target that contributes to pathogenesis or disease progression.
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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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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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Supramolecular polymer materials for biomedical applications and diagnostics
Self-assembly is an abundant process in nature and is vital to many processes in living organisms.
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Synthesis of oligosaccharide libraries from GBS capsular polysaccharides for structure-based selection of vaccine candidates
Glycoconjugate vaccines are composed of microbial poly- or oligosaccharides covalently linked to a carrier protein.
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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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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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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