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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.

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.

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 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 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.

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…

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?

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.

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.

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.

PhD defence

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.

Source: ChemMedChem (2015)

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

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 disease acute myeloid leukemia (AML) is characterized by fast progression and low survival rates.

Data analysis with Python and R are rapidly becoming essential skills for modern scientists. Therefore, we are offering courses to develop your scientific computing skills. Those courses are optional for LACDR PhD candidates.

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

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

Activity-based protein profiling (ABPP, also termed chemical proteomics), is one of the pillars of chemical biology, and at LED3 we have taken it to the next level. ABPP allows the assessment of protein function in live cells and tissues, which means that the activity of a complete protein family can…

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…

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

This project develops a scientific method to extract clinically relevant new information from patient forum websites that discuss patient experiences concerning e.g. medication, nutrition, co-morbidities, genetic factors etc.

Developing robust algorithms and theory for establishing cause-effect relationships from observational data that scale up to large data sets

Promotor: G.P. van Wezel, Co-promotor: Y.H. Choi

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…

Over the past decade, several novel types of spatially resolved

Festival

An interdisciplinary and innovative research group combining History, underwater archaeology, GIS and wood provenancing methods.

Promotor: Prof.dr. T. Hankemeier, Co-promotor: R.J. Vreeken