Over the past decade, several novel types of spatially resolved

Is is possible to better predict the validity of drug candidates?

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

The lack of success of new CNS drugs in clinical development is in part due to the complexity of the CNS, unexpected side effects, difficulties for drugs to penetrate the brain, but also by the lack of biomarkers.

Promotor: J. Kuiper

Adverse drug reactions (ADRs) remain one of the major reasons for patient mortality and (early) drug withdrawal. Currently, different in vivo and in vitro models are used to assess the toxic potential of drugs in the pre-clinical phase. Unfortunately, the predictive value of this model does not fit…

Atherosclerosis is a progressive disease resulting in the formation of an arterial plaque. Despite lipid lowering, recurrent cardiovascular events remain a risk. While atherosclerosis is primarily lipid-driven, the immune system plays a critical role in the pathophysiology.

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.

PhD defence

We are interested in the efficacy and safety of new drugs and novel means to decipher these aspects. Hence, we employ advanced imaging and high-throughput screening techniques next to computational approaches such as chem- and bioinformatics.

Heart failure is a major health care problem with high mortality.

Former masterstudent Bio-Pharmaceutical Sciences Maddalena Centanni will be awarded the 2020 Arenberg Coimbra Prize for Erasmus Students. Centanni spent her six month Erasmus exchange at Uppsala Universiy in Sweden where she looked for ways to improve anti-cancer drug dosing.

Ontwikkeling van resistentie tegen antibiotica kan optreden als patiënten onnodig of te lang met antibiotica behandeld worden. Diagnostiek waarmee snel een bacteriële infectie vastgesteld kan worden, of de response op antibiotica bepaald kan worden, zijn daarom belangrijk om therapie te optimaliseren…

The goal of hit discovery is to identify suitable chemical starting points to modulate a drug target. A hit can be, a.o., a small molecule, a protein or mRNA. Hit identification is performed via rational design, genome mining, (targeted) library screening, or in silico approaches.

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…

From the Big Bang to superconductivity. Many ground-breaking discoveries have been made in Leiden University’s long history.

Is EEG theta\beta ratio predictive towards the negative effects of stress on cognitive performance in individuals suffering from performance anxiety? Can we improve resilience to performance anxiety by using a theta\beta ratio neurofeedback intervention?

From nanoparticles to colliding ice planets and from biological origami to new x-ray scanner techniques: this year again, our scientists have made wonderful discoveries. From the largest numbers to the smallest molecules and from the oldest galaxies up to the latest algorithms, take a look at each institute's…

The Data-Driven Drug Discovery Network (D4N) is an initiative by researchers from Leiden University and collaborators to join efforts in applying and developing novel techniques from data science to drug discovery and related topics from bioinformatics.

The drug discovery pipeline is used to describe the stages in drug discovery. The earliest stage concerns with the identification of potential targets and molecules ('hits') that can modulate their function, while more advanced stages are about developing these hits into viable experimental drugs and…

The aim of this project is to explore the use of statistical interaction models to quantify cross-omics and omics-drug interactions in large-scale clinical and experimental datasets

PhD defence

The Night of Discoveries is an annual event in Leiden, focusing on science and culture. The Young Academy Leiden is a recurring contributor to the Night of Discoveries.

Research in this group, headed by Gerard van Westen, focusses on computational methods integrated in different parts of the drug discovery process. More specifically, topics include innovative treatments for cancer, selectivity modeling, translational research, allosteric modulation, drug resistance…

In the research programme Drug Discovery & Safety, we are interested in the efficacy and safety of new drugs and novel means to decipher these aspects. Hence, we employ advanced imaging and high-throughput screening techniques next to computational approaches such as chem- and bioinformatics.

Sepsis is a life-threatening condition caused by a dysregulated host response to infection, it is associated with significant morbidity, mortality, and with a high financial burden on global healthcare systems. Bacterial infections are the primary cause of sepsis, but the growing prevalence of antimicrobial…

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…

PhD defence

We focus on a better understanding of the mechanisms of cancer drug resistance and metastasis.

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…

The master's specialisation Drug Discovery and Safety at Leiden University provides students with research-oriented education into the discovery of new drug targets and new lead molecules, particularly in the field of cancer, through a combination of advanced imaging techniques (‘systems microscopy’),…

Despite recent advances in medicine, many devastating disorders like cancer and cardiovascular, neurodegenerative and infectious diseases still lack effective treatments. In order to address this challenge, we, as scientists from Leiden University, joined hands in the LED3 network. LED3, for Leiden…

To get a feeling of how we operate at LED3 when it comes to Early Drug Discovery, please browse through our case studies. When you select a case study you’ll find relevant contacts.

We cover the entire spectrum from target identification to the evaluation of the efficacy and safety of novel medicines in clinical practice.

Do understudied animals contain hidden species?

A new research line is the development of liquid biopsy fingerprints to predict early Alzheimer’s disease (AD) stage in human in readily accessible body fluids in human (in collaboration with: Dr. Geert-Jan Groeneveld, CHDR; Prof. Elga de Vries, Free University Medical Center; and others).

Discovery of metastasis promoting candidate drug targets

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.

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.

Science, Institute of Biology Leiden (IBL), Leiden Academic Centre for Drug Research (LACDR)

Supervisor: Indira Nederpelt

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.

The focus of the described research in this thesis is on the oxidative stress response (Nrf2 pathway). The aim of the research presented in this thesis is to obtain more information concerning microRNAs which are involved in the Nrf2 pathway, to determine and evaluate the application of microRNAs for…

Can we develop a generic method for Quan/Qual analysis of small molecule drugs, their metabolites and endogenous metabolites in (pre-)clinical samples?

Medical Biochemistry is a section of the Leiden Institute of Chemistry at Leiden University. The section is headed by Prof. Dr. Hans Aerts.

Source: ChemMedChem (2015)

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.

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.

The spindle-assembly checkpoint (SAC) is a safety mechanism which secures accurate chromosome segregation during mitosis.