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.

Discovery of metastasis promoting candidate drug targets

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

Antimicrobial resistance is one of the biggest threats to human health worldwide in the coming decennia.

Diacylglycerol lipases (DAGLα and DAGLβ) are responsible for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the brain and peripheral tissues. Selective DAGLβ inhibitors have been proposed as a potential treatment for inflammatory diseases with reduced potential for central…

Uncover novel antimicrobials with prospective health benefits for sea turtles.

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

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.

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

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

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

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

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.

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…

N-acylethanolamines (NAEs), which include the endocannabinoid anandamide, represent an important family of signaling lipids in the brain. The lack of chemical probes that modulate NAE biosynthesis in living systems hamper the understanding of the biological role of these lipids.

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.

Many important and extraordinary discoveries have been made in Leiden. Roam the city and discover the fascinating stories behind them. All you need is your smartphone!

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.

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 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…

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…

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…

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.

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…

The Discovery of El Greco: The Nationalization of Culture Versus the Rise of Modern Art (1860-1915)

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.

New or improved treatments for chronic and acute illness.

Leiden Early Drug Discovery & Development (LED3) is a multidisciplinary research network at Leiden University dedicated to advancing innovative approaches in early drug discovery and development. The initiative brings together 58 principal investigators from four institutes—the Institute of Biology…

From the largest numbers to the smallest molecules and from the oldest galaxies up to the latest algorithms, explore our standout discoveries and most inspiring collaborations from the past year!

In Germany, the United States and even in Vietnam: all over the world, the Leiden discovery of the birth of two planets was shared. Astronomer Sebastiaan Haffert and his team were able to record multiple planets in the making for the first time and published their findings in Nature Astronomy. A unique…

'A spectacular new Philippine monitor lizard reveals a hidden biogeographic boundary and a novel flagship species for conservation' . CML-researcher Merlijn van Weerd has participated in a new article in Biology Letters about this discovery.

Lecture

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

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…

Lecture

It was her original Salterio from 1725, built by Michele Barbi, which Franziska Fleischanderl could coincidentally acquire in 2014 that ignited her passion for this special string instrument. Before, she was focussed on contemporary music with modern Hackbrett.

How can the combination of sound composition, astrochemistry, and epistemological analysis provide new and unexpected insights into interstellar chemical reactivity?

Do understudied animals contain hidden species?

For the first time, scientists have traced back a high-energy neutrino to its source in space. It was produced by a so-called blazar—a supermassive black hole. Researchers from neutrino detector IceCube report this in Science. ‘This is a milestone for neutrino science,’ says physicist Dorothea Samtleben…

On an excavation site in Oegstgeest Leiden University archaeologists discovered a very rare silver bowl from the first half of the seventh century. The bowl is decorated with gold-plated representations of animals and plants and inlaid with semi-precious stones. The discovery suggests the existence…

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.