Seven talented female scientists join the fight against cancer of the Oncode Insitute. Laura Heitman of the Leiden Academic Centre for Drug Research is one of the new Junior Investigators. ‘I hope to discover new druggable targets’.

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…

A novel mathematical model describes spatial-temporal drug distribution within one or more brain units, which are cubic representations of a piece of brain tissue with brain capillaries at the edges.

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.

Promotor: Prof.dr. H.V.J. Linnartz, Co-Promotores: H.M. Cuppen, S. Ioppolo

Promotores: Prof.dr. G.W. Canters, Prof.dr. T.J. Aartsma

Promotores: G.W. Canters, T.J. Aartsma

Here you can find our most recent research publications

As of 1 November, Laura Heitman has been appointed full Professor of Molecular Pharmacology at the Leiden Academic Centre for Drug Research (LACDR). Heitman has been working on the understanding and improvement of drug-receptor interactions in early drug discovery. ‘My ultimate aim is to make medicines…

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…

Designing and synthesizing high-affinity ligands for a given drug target have always been among the more important challenges in the drug discovery process.

Supervisor: Natalia Ortiz Zacarías

From 3-6 December 2019 the conference “The Ties that Bind”: Mechanisms and Structures of Social Dependency in the Early Islamic Empire will take place. Deadline for sending in your abstract: 31 January 2019.

Key publications of the Predictive Pharmacology group.

Α-synuclein, a protein associated with Parkinson’s disease, proves to bind with membranes in a surprisingly efficient way. It confirms scientists’ suspicion of the protein’s leading role in the transmission of neurotransmitters between nerve cells in the brain. Publication in PLoS ONE.

Chemical tools to monitor drug-target engagement of endogenously expressed protein kinases are highly desirable for preclinical target validation in drug discovery. Here, we describe a chemical genetics strategy to selectively study target engagement of endogenous kinases.

The discovery in 2001 of the importance of microRNAs turned the world of molecular biology upside down. The small particles of RNA also attracted the attention of university lecturer Erno Vreugdenhil. Vreugdenhil: ‘Within five to ten years the first microRNA-directed medicines will come onto the mar…

Prof. Elizabeth de Lange is concerned with the allocation of resources for the conduct of science towards the goal of best serving the public interest. Also, while she underscores that there is still the need for using animals in drug research, she is concerned about this use, and advocates the use…

Target selectivity is an important aspect of any drug molecule, and certainly a parameter to be optimized. That is not trivial for a number of reasons. First of all hundreds of drug targets (receptors, enzymes, ion channels) exist, and no single lab in the world has assays for all of them.

PhD Defence

Promotor: A.P. IJzerman

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…

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…

‘Huis van het Boek/Museum Meermanno in The Hague exhibits book bindings by leading Dutch Art-Nouveau artists from the period 1890-1910. The exhibition will be open from March 22 to June 23 2019. The title of the exhibition is De Bijzondere Band: Art Nouveau-boeken van Dijsselhof, Lion Cachet en Nieu…

Promotores: Prof.dr. C.A.M.J.J. van den Hondel, Prof.dr. V. Meyer (Technische Universität Berlin)

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.

PhD Defence

Tin electrodeposition applications have rapidly evolved in the past 25 years.

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…

Promotor: M.T.M. Koper, Co-Promotor: F. Calle-Vallejo

Research at the Macromolecular Biochemistry group is comprised of the following research themes:

The purpose of this study was to investigate the formation and growth kinetics of complexes between proteins and oppositely charged polyelectrolytes.

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

Laura Heitman has been awarded a VIDI grant for her innovative drug research. Heitman strives to optimize a drug’s binding kinetics at its target in order to ultimately fight diseases effectively. She even pleads for a paradigm shift in drug discovery.

Research projects for students of the University of Leiden and other Dutch Universities are often available at the MacBio group. The research lines are also described in the Research section. For details of specific projects contact the supervisor (Ubbink, Dame, Boyle).

Nature Reviews Drug Discovery volume 18, pages 82–84 (2019). The implications of target saturation for the use of drug–target residence time Wilbert de Witte, Meindert Danhof, Piet van der Graaf, and Elizabeth de Lange

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.'

Traditional drug discovery approaches have been hampered by (in vitro) cell-culture models that poorly represent the situation in the human body.

Finding structure in disordered proteins and developing drugs for undruggable diseases: it might sound like mission impossible, but pharmacologist Alireza Mashaghi and his team are right on top of it. Their project was awarded by NWO through the Open Competition Domain Science -XS, a competition that…

Promotor: A.P. IJzerman

Promotor: A.P. IJzerman

Promotor: J.P. Abrahams, Co-Promotor: N.S. Pannu

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.

Science, Leiden Institute of Chemistry (LIC)

Promotor: M.T.M. Koper, Co-promotor: L. Juurlink

Promotors: Prof.dr. J. Zaanen, Prof.dr.ir. H. Hilgenkamp

The objective is to develop in vitro antigen degradation assays in order to mimic the fate of the antigen in vivo.

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

Lecture