Wiskunde en Natuurwetenschappen, Instituut Biologie Leiden (IBL)

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

Wiskunde en Natuurwetenschappen, Leids Instituut voor Chemisch Onderzoek (LIC)

During the course of drug discovery translational steps are made.

M van der Stelt

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).

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

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.

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.

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.

Op donderdag 26 januari 2017 verdedigt Anouk Bosma haar proefschrift ‘Targeting recidivism: An evaluation study into the functioning and effectiveness of a prison-based treatment program’. Promotor is prof. dr. Paul Nieuwbeerta, en copromotor dr. mr. Maarten Kunst.

Oratie

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

Op 27 mei 2021 verdedigde Hirad Abtahi zijn proefschrift 'Adjudicating Attacks Targeting Culture'. Het promotieonderzoek is begeleid door promotor prof.dr. C. Stahn.

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.

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

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-…

The present thesis focuses on the pharmacological concept of drug-target interaction, which dates back to the beginning of modern pharmacology.

The chemical synthesis of inhibitors and probes targeting endo-glycosidases.

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

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.

Large parts of the research described in this Thesis aims at the development of oligopeptide-masked toxins and their in situ immunoproteasome-mediated activation.

This thesis explores different avenues to develop insurmountable antagonists for CC Chemokine Receptors, such as CCR1, CCR2 and CCR5.

In this thesis, a system pharmacology approach, integrating metabolomics, pharmacology and chemical biology, was applied to understand and modulate the endocannabinoid system across different model systems (cells, zebrafish, mice and humans).

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

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

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…

The objective of this study was to investigate the expression and function of GRHL2 in different breast cancer subtypes.

Stelt

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.

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…

Wiskunde en Natuurwetenschappen, Leiden Academic Centre for Drug Research (LACDR), LACDR PhD Portal

Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: L.H. Heitman

Promotor: M. Danhof, Co-promotor: E.C.M. de Lange

Promotor: B. van de Water

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

Wiskunde en Natuurwetenschappen, Leiden Academic Centre for Drug Research (LACDR)

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

Promotie

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.

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: …

Promotie

Promotie

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.

In vitro disease models play a fundamental role in drug research. They enable the systemic identification and validation of disease mechanisms and the discovery of possible drug targets. However, more than often, drug candidates that are identified in vitro fail in the later clinical stages of drug…

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…