Allosteric modulation has long been recognized as a general and widespread mechanism for the control of protein function. Modulators bind to regulatory sites distinct from the active site on the protein, resulting in conformational changes that may profoundly influence protein function. This concept…

Supervisor: Natalia Ortiz Zacarías

Supervisor: Maarten Doornbos

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

Promotor: A.P. IJzerman

Promotor: A.P. IJzerman

Source: Mediators Inflamm (2014)

The recognition that there may be more, so-called allosteric binding sites on a given receptor has also fueled our synthetic efforts. Over the last few years we have focused on many drug targets (adenosine A1, A2A and A3 receptors, the mGlu2 receptor and a classic ‘anti-target’, the hERG channel) to…

Supervisor: Gerard van Westen

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

VIPP/VIPP-SD (the basic module) can be applied to most family situations. However, some modules have been adapted to suit specific target groups. After completing the four-day basic training for the VIPP-SD, professionals can be trained to apply these specific modules. We work together with various…

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

In two out of six electives, you will acquire substantive and in-depth knowledge and skills relating to specific leadership themes. The elective modules consist of 3 EC (6 EC in total).

Participation in the matching module is a compulsory part of the admission and application procedure for all applying students of this programme.

Promotores: Prof.dr. H Lenstra, Prof.dr. A Facchini (Padova University)

Cardiovascular disease is a major global burden and atherosclerosis is the main underlying pathological process.

The receptor nomenclature committee of IUPHAR, the International Union of Pharmacology, has several subgroups. Among these are a few that our division is involved in, those for adenosine, nicotinic acid, and GnRH receptors.

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Promotores: Prof.dr. M.K. Richardson, Prof.dr. H.P. Spaink

The Graduate School Management (GSM) module is a registration and monitoring module for you and your supervisor(s). All information is stored in a uniform way and made accessible in one place. Converis is the software behind LUCRIS.

Promotores: Prof.dr. E.A.L. Biessen, Prof.dr. T.J.C. van Berkel

Unraveling the immune-suppressive actions of drugs like prednisone.

Plant-microbe interaction resulted in different physio/chemical responses by host plant and interacting rhizobacteria.

Promotores: Prof.dr. J. Kuiper, Prof.dr. P.H.A. Quax

Glucocorticoids (GCs) are widely prescribed as anti-inflammatory drugs due to their well-established immunosuppressive effects.

Source: Mol Pharmacol, Volume 87, Issue 2, pp. 305-13 (2015)

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

Cardiovascular diseases are the primary cause of death in the world with atherosclerosis as primary underlying cause.

The discovery of new medicines is a tedious and lengthy process. On average, over 10,000 molecules need to be studied for one to become a drug and reach the patient. Part of that process are the very costly clinical trials in humans, and candidate drugs often fail due to side effects or lack of efficacy.…

This dissertation examines what network in the human brain is involved in the perception of prosody and whether activity within this network is modulated by the personality trait alexithymia.

In this research project, we aimed to obtain more insight in the role of mast cells in the immune driven disorders rheumatoid arthritis and atherosclerosis.

Promotor: Prof.dr. T. Schmidt, Co-Promotor: Dr. ir. S.J.T. van Noort

The mission in this research group, headed by Ad IJzerman, is to design and synthesize novel and better ligands for drug targets. Drug discovery is a lengthy but inspiring adventure. It is often an interplay between academic institutes and pharmaceutical industry, in which scientists at university develop…

Our in-house human skin equivalents contain all stratum corneum (SC) barrier lipid classes, but have a reduced level of free fatty acids (FAs), of which a part is mono-unsaturated. These differences lead to an altered SC lipid organization and thereby a reduced barrier function compared to human skin.…

Atherosclerosis is the main underlying pathology of cardiovascular disease. Atherosclerosis is caused by an immune response which is directed against (modified) lipoproteins which accumulate in the vessel wall.

Acute cardiovascular clinical events such as myocardial infarction and cerebral stroke represent the major cause of death in Western societies. These pathologies are primarily resulting from atherosclerosis, a progressive condition characterized by the accumulation of lipids, immune cells, and fibrous…

Promotor: Prof.dr. J. Kuiper

The PID-directed shift in PIN polarity has been broadly accepted as one of the essential mechanisms for the regulation of auxin transport polarity.

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.

Can we link multiple components from herbal extracts with their biological activities?

In this research group, headed by Laura Heitman, novel receptor concepts in drug discovery are studied, aiming to increase the effectivity of medicines. Many drugs act via so-called G protein-coupled receptors (GPCRs) and therefore our research is mainly focused on understanding and improving drug-receptor…

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…

Dong Guo was awarded two poster prizes for his poster ‘Molecular Mechanism of Allosteric modulation at G protein-coupled Receptors: Insight from a Binding Kinetics Study at the Human A1 Adenosine Receptor’ at the FIGON Dutch Medicines Days, October 6th-8th this year.

The goal of hit and lead optimization is to optimize suitable chemical starting points that can modulate a drug target. The methods and technologies used are similar to those in Hit Discovery, but once the compound has shown activity in an animal model, it moves from 'hit' to 'lead.'

The Chemical Probe Facility is part of the Leiden Early Drug Discovery & Development (LED3) center. Activity-based protein profiling (ABPP) is one of the pillars of chemical biology. ABPP determines the activity of entire protein families in living cells and tissues under physiological conditions, such…

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