Pharmaceutical companies, governments and the general public have become increasingly aware that animal models used in drug testing lack vital aspects to serve as an accurate representation of human biology. As models of the human body should become more physiologically relevant, animal models no longer…

In this thesis, we will utilize embryonic zebrafish tumour models to understand the interaction between engrafted human cancer cells and macrophages from the host, test drug administration modalities and anti-cancer efficacies of newly-developed PDT and PACT compounds, and test a light-triggered liposomal…

Promotor: E. Bouwman, Co-promotor: S. Bonnet

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-…

There is an urgent need for more physiologically relevant cell culture methods to guide compound selection in pre-clinical stages of the drug development pipeline.

Traditional drug discovery approaches have been hampered by (in vitro) cell-culture models that poorly represent the situation in the human body.

Promotor: B.van de Water, Co-promotor: L.S.Price

Hoe kun je met robots en automatische herkenning van microscopische beelden uitzonderlijk snel het effect van medicijnen testen?

O-Nitrobenzyl groepen worden veel gebruikt als moleculaire beschermgroepen die je met licht kunt verwijderen.

Promotores: Prof.dr. P.C.W. Hogendoorn & Prof.dr. H.P. Spaink Co-promotor: Dr. B.E. Snaar-Jagalska

PhD Defence

Drug-target binding kinetics determine the time course of the central event in pharmacotherapy: Drug-target interaction.

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.

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.

Promotor: A.P.IJzerman Co-promotor: A. Bender

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.

Promotor: Prof.dr. B. van de Water

Promotor: Prof.dr. R. Verpoorte, Co-Promotor: Dr. Young Hae Choi

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…

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…

Science, Leiden Academic Centre for Drug Research (LACDR), LACDR PhD Portal

This thesis describes the importance of being able to control the selectivity of potential drug candidates.

Promotor: Prof.dr. M. Danhof, Co-Promotor: J. de Jongh

During the course of drug discovery translational steps are made.

Science, Leiden Academic Centre for Drug Research (LACDR)

M van der Stelt

Clinical development of drugs for central nervous system (CNS) disorders has been particularly challenging and still suffers from high attrition rates.

Science, Leiden Institute of Chemistry (LIC)

Discovery and development of Central Nervous System (CNS) drugs is hampered by high attrition rates.

The aim of this thesis is to expedite and ensure the systematic accuracy of clearance scaling from adults to paediatric patients, with a special focus on drugs undergoing hepatic metabolism.

Promotores: H.S. Overkleeft, G.A. van der Marel, Co-Promotor: R.G. Boot

The path to rational drug and dose selection

Model based approaches, integrating physiological parameters or linking exposure with response, are powerful tools to quantify and evaluate the impact of genetic differences that are reflected as variability of drug exposure and/or clinical response(s). This thesis “Pharmacogenomics in Drug Development: …

Science, Institute of Biology Leiden (IBL)

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.

Promotor: B. van de Water

Promotores: Prof.dr. C.A.J. Knibbe, Prof.dr. M. Danhof, Prof.dr. K. Allegaert (Leuven)

Promovenda Luisa Prochazkova deed samen met haar collega's van cognitieve psychologie onderzoek naar de effecten van microdoseringen psychedelische drugs op creativiteit. Hun eerste voorzichtige conclusie: je wordt inderdaad creatiever van een klein beetje LSD.

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.

Glucocorticoids (GCs) are widely prescribed as anti-inflammatory drugs due to their well-established immunosuppressive effects.

PhD Defence

The molecular mechanisms that instigate a healthy cell to become malignant are fueled by (epi)genetic alterations in so-called driver genes.

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.

Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt

In photoactivated chemotherapy (PACT), a biologically active compound is caged by a light-cleavable protecting group.

Vitamin A or retinol is essential in embryonic development, the visual cycle and the immune system.

In this thesis, we have studied the potential of the zebrafish larval model in studying the ECS, as a complementary model to the existing rodent models.

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.

Psychedelische drugs zoals paddo’s en LSD worden door de één omarmd, en door de ander gezien als levensgevaarlijk. Cognitief psycholoog Michiel van Elk dook in de wereld van de psychedelica en schreef er een opvallend nuchter boek over. ‘Zonder ervaring uit eerste hand vond ik mijn verhaal niet comp…