2,322 search results for “target validation” in the Public website
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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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Novel chemical tools for target validation in neuroinflammation
In what way can new tools and techniques be used to develop drug candidates for the treatment of neurological disorders?
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Preclinical validation of putative targets in cardiovascular and metabolic disease
Cardiovascular disease is the number one cause of death worldwide. The most important risk factor for developing this disease is high cholesterol levels in the blood.
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Target Discovery
The goal of target discovery is to identify and validate proteins and biological pathways that are involved in the disease process. Modulating these target proteins and pathways with small molecules, therapeutic proteins or other biomolecules (e.g. mRNA) could deliver an effective and safe drug or v…
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reductase inhibitors identified using chemogenomic methods and in vitro validation
Source: PLoS ONE, Volume 10, Issue 3 (2015)
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Discovery of metastasis promoting candidate drug targets
Discovery of metastasis promoting candidate drug targets
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Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis, Nat. Comm. 2020
Chemical tools to monitor drug-target engagement of endogenously expressed protein kinases are highly desirable for preclinical target validation in drug discovery. Here, we describe a chemical genetics strategy to selectively study target engagement of endogenous kinases.
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Cancer Drug Target Discovery
We focus on a better understanding of the mechanisms of cancer drug resistance and metastasis.
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Chemical genetic approaches for target validation
PhD defence
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Tom van der Wel
Science
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VOILA (Validation of Innovative Lipopeptide Antibiotics)
Examining the therapeutic potential of new semisynthetic lipopeptide antibiotics
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Identification of novel targets in prostate cancer progression
Promotor: Prof.dr. B. van de Water, Co-promotor: E.H.J. Danen
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Novel target engagement biomarkers for better drug candidates
Is is possible to better predict the validity of drug candidates?
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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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Cancer Drug Target Discovery
In this research group, headed by Prof. Erik Danen, the aim is to unravel cellular signaling mechanisms in normal and diseased cells, with a long-standing interest in cell adhesion signaling. In complex multicellular organisms such as ourselves, a division of labor emerges where different tissues and…
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Intervention targets in cognitive development
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Adjudicating Attacks Targeting Culture
On 27 May 2021, Hirad Abtahi defended his thesis 'Adjudicating Attacks Targeting Culture'. The doctoral research was supervised by Prof.dr. C. Stahn.
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Efficient gene-targeting during meiosis
Efficient gene-targeting during meiosis
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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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Targeting macrophages in renal transplantation
PhD defence
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Targeted biomolecule production for therapeutic use
We aim to develop a drug-delivery method based on the production of biomolecules directly at the target site.
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Drug-target binding kinetics in vivo
A next, general pharmacological problem to be tackled is how drug-target binding kinetics in vivo, affects target occupancy as an important indicator of the time-course of drug effects.
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Using zebrafish to target the Achilles’ heel of cancer
Exploiting metabolic vulnerabilities to identify anticancer compounds in zebrafish synthetic lethality screens.
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Inhibitors and probes targeting endo-glycosidases
The chemical synthesis of inhibitors and probes targeting endo-glycosidases.
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Targeting Human Proteasomes: Substrates, Inhibitors and Prodrugs
Large parts of the research described in this Thesis aims at the development of oligopeptide-masked toxins and their in situ immunoproteasome-mediated activation.
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LED3 Lecture: Neural system targeting compounds
Lecture
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Validity in teacher assessment. An exploration of the judgement processes of assessors
Assessment of teaching is currently becoming more and more common practice. As such assessment is generally based on complex, qualitative data from multiple sources (e.g., lesson plans, video-taped lessons, written reflections of the teacher on his or her performance), the overall quality of the assessment…
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Targeting gun violence & trafficking in Europe
To assess the impact of illicit firearms trafficking on gun violence, this research looks at the scope, characteristics and contexts of firearm violence, and also the scope and nature of firearms trafficking in Europe since the new millennium. Nils Duquet, Dennis Vanden Auweele and Marieke Liem created…
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Targeted Therapy for Triple-Negative Breast Cancer
The research described in this thesis focused on identifying novel drug targets and synergistic combinations for triple-negative breast cancer (TNBC), a virulent subtype of breast cancer with a dismal prognosis and limited therapeutic options.
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evaluation of video portfolios: reliability, generalizability, and validity of an authentic performance assessment for teachers
The research study presented in this dissertation focuses on issues pertaining to the reliability, generalizability, and validity of authentic performance assessments of teachers.
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Efficient targeting of the Trichoderma genome for industrial protein engineering
The research is aimed at development of an efficient gene targeting method that allows controlled integration of DNA at a preselected site in the Trichoderma genome.
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Non-target effects of GM potato: an eco-metabolomics approach
Promotors: Prof.dr. P.G.L. Klinkhamer, Prof.dr. P.M. Brakefield
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Computational Approaches to Disease, Signaling and Drug Targets
The Minor Computational Approaches to Disease, Signaling and Drug Targets (CADSDT) is focused on fundamental scientific research required for discovery of new drug targets and development of new drugs.
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Epilepsy and anxiety: targeting a vicious cycle
How effective is eye movement desensitization and reprocessing therapy in targeting epilepsy-related anxiety?
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Exploring Grainyhead-like 2 target genes in breast cancer
The objective of this study was to investigate the expression and function of GRHL2 in different breast cancer subtypes.
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Targeting of antigen-presenting cells with mannosylated conjugates
This thesis describes the development of a variety of mannosylated conjugates. Antigen presenting cells bear mannoside recognizing receptors that actively transport antigen into the cell. This thesis exploits this feature for the development of improved vaccines.
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Project TARGET: gun violence and firearms trafficking in Europe”
Project TARGET aims to improve our understanding of gun violence in Europe and the relationship between gun violence and firearms trafficking.
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The Role of Target Binding Kinetics in Drug Discovery
Source: ChemMedChem (2015)
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Grants & Awards
Grants awarded to molecular physiology research
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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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Oxidants and antioxidants as targets for cardiovascular disease prevention
PhD defence
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Tumor-specific targets for imaging in vulvar cancer
PhD defence
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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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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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Bayesian Statistics in Infinite Dimensions: Targeting Priors by Mathematical Analysis
Novel methods for understanding key aspects that are essential to the future of Bayesian inference for high- or infinite-dimensional models and data.
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Exploring the mechanism of targeted nanoparticle-mediated drug delivery using the zebrafish model
Exploring the mechanism of targeted nanoparticle-mediated drug delivery using the zebrafish model
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Systems Pharmacology
The Systems Pharmacology group is headed by Prof. Piet Hein van der Graaf. Systems Pharmacology is the quantitative analysis of the dynamic interactions between drugs and a biological system to understand the behaviour of the system as a whole, as opposed to the behaviour of its individual constituents;…
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Discovery of antibiotics and their targets in multidrug-resistant bacteria
Global healthcare is on the verge of an antibiotic availability crisis as bacteria have evolved resistance to nearly all known antibacterials. Identifying new antibiotics that operate via novel modes-of-action is therefore of high priority.
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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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Systems microscopy-based drug target discovery in pathogen-meidated inflammatory respons signalling
Establishing human induced pluripotent stem cell (iPSC) CRISPR-Cas9-based fluorescent reporter cell lines for NF-kB signalling. We will use this to enable studying the dynamic activation and downstream signalling of Toll-like receptor and cytokine signalling in iPSC-derived differentiated cells in a…