529 zoekresultaten voor “drug discovery” in de Publieke website
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Modern Drug Discovery
How are new drugs developed? This question is central to the Minor Modern Drug Discovery (MDD), which covers the entire trajectory from disease to drug molecule and vice versa. The various research groups involved offer a complementary and interdisciplinary perspective by connecting the diverse subjects…
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Drug Discovery & Safety
In het onderzoeksprogramma Drug Discovery & Safety zijn we geïnteresseerd in de werkzaamheid en veiligheid van nieuwe medicijnen en nieuwe manieren om deze aspecten te bepalen. Daarvoor combineren we geavanceerde imaging en high-throughput screening technieken met computationele aanpakken zoals chem-…
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Drug Discovery and Safety (MSc)
In deze opleiding ontwikkel je je onderzoek skills en verbreed je je kennis over de meest moderne en geavanceerde technieken die je nodig hebt als onderzoeker op het gebied van target finding en het ontwerp en de synthese van nieuwe geneesmiddelen.
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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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Microengineered Human Blood Vessels For Next Generation Drug Discovery
Heart failure is a major health care problem with high mortality.
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Proteins in harmony: Tuning selectivity in early drug discovery
This thesis describes the importance of being able to control the selectivity of potential drug candidates.
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Transforming data into knowledge for intelligent decision-making in early drug discovery
Promotor: A.P.IJzerman Co-promotor: A. Bender
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Image-based phenotypic screening for breast cancer metastasis drug target discovery
The main aim of this thesis was to unravel the signaling and regulatory networks that drive tumor cell migration during breast cancer metastasis.
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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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Cancer Drug Discovery Initiative maakt nieuwe therapieën tegen kanker mogelijk
Het Antoni van Leeuwenhoek/Nederlands Kanker Instituut, het Leids Instituut voor de Chemie en het Pivot Park Screening Centre gaan kennis en infrastructuur delen in het Cancer Drug Discovery Initiative. Vrijdag 11 oktober tekenden ze een letter of intent.
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Mechanistic modelling of drug target binding kinetics as determinant of the time course of drug action in vivo
Drug-target binding kinetics determine the time course of the central event in pharmacotherapy: Drug-target interaction.
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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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Discovery of FLT3 inhibitors for the treatment of acute myeloid leukemia
The disease acute myeloid leukemia (AML) is characterized by fast progression and low survival rates.
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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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To explore the drug space smarter: Artificial intelligence in drug design for G protein-coupled receptors
Over several decades, a variety of computational methods for drug discovery have been proposed and applied in practice. With the accumulation of data and the development of machine learning methods, computational drug design methods have gradually shifted to a new paradigm, i.e. deep learning methods…
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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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Leiden Academic Centre for Drug Research
Het ontwikkelen van nieuwe medicijnen is een complex proces waarbij veel partijen samenwerken. De onderzoekers van het LACDR zetten zich dagelijks in voor nieuwe, betere, efficiëntere en makkelijker produceerbare medicijnen. Het instituut werkt nauw samen met het LUMC, met bedrijven op het Leiden Bio-Science…
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Discovery of BUB1 kinase inhibitors for the treatment of cancer
The spindle-assembly checkpoint (SAC) is a safety mechanism which secures accurate chromosome segregation during mitosis.
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Erik Danen benoemd tot hoogleraar Cancer drug target discovery
Met ingang van 1 april 2018 is Erik Danen benoemd tot hoogleraar Cancer drug target discovery bij het Leiden Academic Centre for Drug Research (LACDR). Zijn vakgebied is celbiologie van kanker, waarin hij zich richt op de achterliggende mechanismen bij uitzaaiingen en resistentie voor behandelingen.
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Medical Delta café: translation models for drug discovery and development, 8 oktober 2013
Onze gemiddelde leeftijd gaat omhoog en de behoefte naar goede gezondheidszorg wordt steeds groter. Nieuwe medicijnen moeten op de markt komen maar kosten voor de ontwikkeling daarvan moeten omlaag. Tijdens het Medical Delta café op 8 oktober presenteren o.a. dr. Leo Price, dr. Jan de Sonneville en…
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NMR structural studies of protein-small molecule interactions
Promotor: Prof.dr. M. Ubbink, Co-promotor: G. Siegal
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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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A pharmacognostic study of Vernonia guineensis Benth. (Asteraceae): bioactivity, safety, and phytochemical analysis
Promotor: Prof.dr. R. Verpoorte, Co-Promotor: Dr. Young Hae Choi
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namic Relationships of Central Nervous Systems Active Dopaminergic Drugs
Discovery and development of Central Nervous System (CNS) drugs is hampered by high attrition rates.
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Drug-target residence time: a case for the adenosine A1 and A2A receptors
Promotor: A.P.IJzerman, Co-Promotor: L.H. Heitman
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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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Biophysical characterization of membrane protein-small molecule interactions
Promotor: Prof.dr. M. Ubbink
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Sensing Transport
Solute carrier (SLC) transporters are a large and diverse class of relatively understudied transmembrane proteins.
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Chemical tools to study the cannabinoid receptor type 2
The cannabinoid receptor type 2 (CB2R) is associated with several inflammatory diseases with an unmet medical need (e.g. Alzheimers, multiple sclerosis, reumatoid arthritis). Development of new chemical biology strategies to study this protein is essential to aid future development of drugs for these…
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Postdoc Computational Modeling for Drug Safety Prediction
Wiskunde en Natuurwetenschappen, Leiden Academic Centre for Drug Research (LACDR)
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Antibiotic Discovery: From mechanistic studies to target ID
The investigations described in this thesis lay out strategies aimed at advancing antibiotic research and development. The examples presented revolve around two main approaches: understanding drug-target interactions and target identification.
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Affinity-based profiling of the adenosine receptors
The adenosine receptors are proteins that reside in the extracellular membranes of cells. Activation of adenosine receptors plays a role in many physiological and pathological processes, such as immune responses and cancers.
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Photo-activated drug delivery systems
O-Nitrobenzyl groepen worden veel gebruikt als moleculaire beschermgroepen die je met licht kunt verwijderen.
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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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Harnessing zebrafish xenograft models for ocular melanoma treatment discovery
The aim of this thesis was to develop novel treatment strategies for different types of eye melanoma utilizing zebrafish models. We first establish orthotopic and ectopic xenograft models for uveal and conjunctival melanoma by engraftment of the immortalized cells derived from these tumors into zebrafish…
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Small changes for long term impact: optimization of structure kinetic properties: a case of CCR2 antagonists
Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: L.H. Heitman
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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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Dynamics of TNFalpha signaling and drug-related toxicity
In previous studies at our laboratory it was demonstrated that drug exposure of HepG2 cells can lead to an altered TNFα-induced NF-κB oscillatory phenotype, concurrent with a synergistically increased sensitivity for TNFα-induced apoptosis.
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Clavis Aurea? Structure-enabled approaches of identifying and optimizing GPCR ligands
Promotores: A.P. IJzerman, H.W.T. van Vlijmen
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Reverse engineering of drug induced QT(c) interval prolongation: Towards a systems pharmacology approach
Promotor: M. Danhof Co-promotor: O.E. Della Pasqua
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Translational pharmacokinetics-pharmacodynamics in zebrafish: integration of experimental and computational methods
The zebrafish is a promising vertebrate model organism in early drug discovery and development.
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The activation mechanisms of G protein-coupled receptors: the case of the adenosine A2B and HCA2/3 receptors
Promotor: A.P. IJzerman
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Ginsenosides as selective glucocorticoid drugs: agonists, antagonists, and prodrugs
Glucocorticoids are potent anti-inflammatory drugs widely used clinically to treat various inflammatory and immune conditions. However, two main clinical problems limit their use. GCs trigger severe side effects and they induce acquired glucocorticoid resistance, especially during chronic systemic treatment…
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Knowledge discovery from patient forums: gaining novel medical insights from patient experiences
Patients share valuable advice and experiences with their peers in online patient discussion groups.
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Phenotypic screening with 3D cell-based assays
Traditional drug discovery approaches have been hampered by (in vitro) cell-culture models that poorly represent the situation in the human body.
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Mario van der Stelt
Wiskunde en Natuurwetenschappen
m.van.der.stelt@chem.leidenuniv.nl | +31 71 527 4768
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Discovery and characterization of new glucosylated metabolites: pathophysiological consequences
Within this thesis the central stage is taken by the discovery and investigation of transglycosylation of sterols. First, investigation focuses on the development of a method to accurately detect and quantify glucosylated metabolites in biological materials.
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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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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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Prediction of spatial-temporal brain drug distribution with a novel mathematical model
A novel mathematical model describes spatial-temporal drug distribution within one or more brain units, which are cubic representations of a piece of brain tissue with brain capillaries at the edges.