Due to the modern techniques of combinatorial chemistry and high-throughput screening, data on the biological activity of many millions of compounds is known. However, it is still very difficult to transfer this data into knowledge: if we know that compounds A and B bind to a certain protein with high…

Dr. at the Department of organic chemistry, Wageningen University - the Nederlands

The studies presented in the work show the potential of the integrative use of biophysical data in defining the structural basis of protein interactions.

Enzymes are innately sensitive to changes in the amino acid sequence, which largely constrains their evolutionary potential, i.e., evolvability. This evolutionary burden can be alleviated in the presence of stabilizing mutations, which increase the buffering capacity of enzymes to tolerate mutations…

A key step in the synthesis of oligosaccharides and glycoconjugates is the formation of the glycosidic bond.

This dissertation explores new chemical strategies for the synthesis of self-adjuvanting peptide conjugates and immunomodulatory ligands aimed at targeted activation of the immune system.

Promotor: M. Ubbink, Co-promotor: G. Siegal

Glycoside hydrolases (glycosidases/GHs) are widely abundant enzymes in all kingdoms of life and are important biocatalysts that catalyze the hydrolysis of glycosidic linkages in oligo/polysaccharides, glycoproteins and glycolipids with tremendous efficiency

In this thesis unconventional tools based on fluidic interfaces were developed to study the surface and interfacial chemistry of graphene, to characterize the intrinsic properties of graphene, to disentangle the effects of substrate and of the environmental factors, and to improve handling protocols…

This thesis focuses on developing wafer-scale two-dimensional (2D) materials by combining synthesis, transfer, characterization, and device integration of graphene, hexagonal boron nitride (h-BN), and BN-doped amorphous carbon.

Neurodegenerative diseases pose a large medical and societal challenge. The etiology of these diseases is still poorly understood, which makes drug discovery for these diseases difficult.

Lipid nanoparticles (LNPs) have enabled the success of mRNA vaccines but remain limited in broader therapeutic use by challenges in delivery efficiency, targeting, and mechanistic understanding.

Bioarchaeology covers the study of all biological remains from archaeological sites.

This thesis describes the evaluation of novel natural products with antibacterial activity enabled by total chemical synthesis.

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The drug BIA 10-2474 inhibits fatty acid amide hydrolase (FAAH), a lipase that degrades a specific endocannabinoid. On the basis of this activity, BIA 10-2474 was being developed as a potential treatment for anxiety and pain. In a phase 1 trial of the drug, one subject died, and four others suffered…

A high-end label: Cyclophellitol aziridine-type activity-based probes allow for ultra-sensitive visualization of mammalian β-glucosidases (GBA1, GBA2, GBA3, and LPH) as well as several non-mammalian β-glucosidases (see picture). These probes offer new ways to study β-exoglucosidases, and configurational…

Three at the same time: a ligation strategy combining tetrazine–norbornene cycloaddition, Staudinger–Bertozzi ligation, and copper(I)-catalyzed click reaction was used to label the three catalytic activities of the proteasome simultaneously in a single experiment. The orthogonality of the three ligation…

The main research theme in the group of Dennis Hetterscheid is to understand and mimic bioinorganic multi-electron processes that are relevant to our future energy infrastructure. Reduction of protons generates hydrogen that can be used as a chemical fuel. Alternatively to gaseous hydrogen, the reduction…

The Leiden Institute of Chemistry (LIC) offers a unique tailor-made programme in Life Science and Technology. You can customize the programme to your own interests and ambitions with the help of your own personal mentor. Your study will focus on either a biomedical, molecular or biophysical approach…

The thesis describes the development, synthesis and biological evaluation of several proteasome inhibitor designs. Mainly, this work focusses on designing proteasome inhibitors that selectively inhibit the immunoproteasome, while leaving the constitutive proteasome mostly, if not completely, untouch…

There are eight institutes at the Faculty of Mathematics and Natural Sciences:

This thesis describes the design and synthesis of novel small molecules based on sulfur-containing heterocycles for the inhibition of glycosidases and glycosyltransferases related to Fabry and Pompe disease.

The cannabinoid receptor type 2 (CB2R) is associated with several inflammatory diseases with an unmet medical need (e.g. Alzheimers, multiple sclerosis, reumatoid arthritis). Development of new chemical biology strategies to study this protein is essential to aid future development of drugs for these…

A deceptively simple, complicated paper

The aim of the research described in this thesis was to use structure-based design to optimise multiple properties of aryl sulfoxide monoacylglycerol lipase inhibitors as anti-inflammatory analgesics.

Thesis focused on uncovering the underlying mechanisms of the lysosomal storage disorders Gaucher's disease using chemical tools, biochemical assays and lipidomics.

An overview of awards and prizes granted to our staff and students in 2017, as well as special appointments and royal distinctions.

If you are interested in Life Science and you are looking for a programme with ample opportunities to put together your own study path, our Life Science and Technology programme is the right choice. The programme focuses on societal problems at the molecular and cellular level.

Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel

Promotores: H.S. Overkleeft; G.A. van der Marel Co-Promotor: B.I. Florea

The polypept(o)ide hybrid material attracted more and more attention over the past decade by combining the multifunctional characteristics of polypeptides with the shielding characteristics of polypeptoid-pSar possessing similar properties as a shielding material as polvethylene glycol(PEG). Polysarcosine…

Microbial rhodopsins are photosensitive pigments implemented in the growth and adaptation of a large population of microorganisms.

Bacteria often experience external challenges, such as changes in environmental conditions or attacks by bacteriophages.

While bioinformatics methods deal with the analysis of sequence information (be it proteins or DNA), the field of cheminformatics is concerned with the analysis of small-molecule datasets.

In this thesis, the discovery and optimization is described of chemical tools to study the N-acylethanolamine (NAE) biosynthetic pathway.

The Business Studies specialisation is for science students who consider employment opportunities in industry, and who are looking to acquire knowledge of business principles and training in managerial skills. The specialisation can be followed by students doing a two-year Masters degree in one of…

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

Source: Mol Psychiatry (2015)

Nanodiscs are small, disc-shaped structures designed to mimic biological cell membranes, composed of a lipid bilayer stabilized by scaffold proteins. Membrane proteins play crucial roles in essential processes such as nutrient and waste transport, molecular recognition, and cell signalling, making them…

Synthetic cells, also known as artificial cells or protocells, have wide ranging applications from drug delivery vectors to cell models. In biotechnology they can function as micro- or nanoreactors with possible applications in biocatalysis and photocatalysis. Phospholipids are by far the most commonly…

Chapter 2 describes a post-synthetic methodology to introduce a fluorescent label in highly lipophilic, Pam3Cys based conjugates.

Artificial photosynthesis has recognised potential to produce green and sustainable fuels from earth-abundant resources such as water, carbon dioxide (CO2), and sunlight.

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