One of the main challenges in the development of an effective anti-cancer vaccine is the generation of an adequate and directed cellular immune response.

Supervisor: Xue Yang

Many biological processes occur by biomolecules coming together and organizing into specific clusters without being bound to each other. These interactions range from clustering, transiently interacting (kiss and run), or assembling to multimeric units that can only function in conjunction. The hydrogen…

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

Description of Biotic ligand models: making an inventory of available models & assessment of the variability of the predicted HC5 using the BLMs in different Dutch water types (2005 - 2007)

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

Promotor: Prof.dr. G.R. de Snoo, Co-promotores: Dr. ing. M.G. Vijver, J.P.M. Vink

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.

The main goal of the research described in this thesis was the development of new photoactivated chemotherapy (PACT) ruthenium(II) complexes bearing a non-toxic photolabile ligand.

The research described in this thesis focused on the preparation of S/N functionalized carbene ligands and their transition metal complexes, and the exploration of their application as electrocatalysts for proton reduction.

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

Supervisor: Andrea Martella

The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB2R, their selectivity, molecular mode of action and pharmacokinetic properties have…

Promotores: A.P. IJzerman, H.W.T. van Vlijmen

The present thesis focuses on the pharmacological concept of drug-target interaction, which dates back to the beginning of modern pharmacology.

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

Detection of cerebral beta-amyloid (Abeta) by targeted contrast agents remains of great interest to aid the in vivo diagnosis of Alzheimer's disease (AD). Bis-styrylbenzenes have been previously reported as potential Abeta imaging agents.

The indane (2,3-dihydro-1H-indene) ring system is an attractive scaffold for biologically active compounds due to the combination of aromatic and aliphatic properties fused together in one rigid system.

During the course of drug discovery translational steps are made.

Promotor: E. Bouwman, Co-promotor: S. Bonnet

Promotor: E. Bouwman, Co-Promotor: S. Bonnet

Cyclic peptides are investigated as a platform to induce different orientations between various ligands.

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

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

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

Adenosine is an endogenous ligand which exerts its action by activating adenosine receptors (ARs), while its circulating levels are controlled via a variety of mechanism and proteins, amongst others the equilibrative nucleoside transporters (ENTs).

Grants awarded to molecular physiology research

Promotor: Prof.dr. W.J.G.M. Peijnenburg, Co-promotor: Dr. ing. M.G. Vijver

The current projects of the Molecular Physiology group focus on proteins of the endocannabinoid system, kinases and antibacterial targets. MSc- and BSc-students can contact Jessica van Krimpen-Kraaijenoord to apply for research internships.

Dendritic cells (DC) play a prominent role in the priming of CD8(+) T cells. Vaccination is a promising treatment to boost tumor-specific CD8(+) T cells which is crucially dependent on adequate delivery of the vaccine to DC.

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.…

Chemical biology research at the Leiden Institute of Chemistry is aimed at understanding biological processes at the molecular level to strengthen the knowledge base of human health and disease. The approach to achieve this goal is a fundamental chemical one; with the aid of chemical probes biological…

Chemical biology research at the Leiden Institute of Chemistry is aimed at understanding biological processes at the molecular level to strengthen the knowledge base of human health and disease. The approach to achieve this goal is a fundamental chemical one; with the aid of chemical probes biological…

Promotores: Wim Jiskoot; Ferry Ossendorp

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…

Drug development is a time- and resource-consuming process that starts with the discovery and validation of a (protein) target that contributes to pathogenesis or disease progression.

The group of Dr. Roxanne Kieltyka designs and synthesizes molecules that self-assemble into polymeric materials using specific non-covalent interactions. These substrates can be used for numerous applications in medicine ranging from disease detection to cell delivery depending on the (bio)molecular…

Supervisor: Lizi Xia

In the last decade, the redox interconversion between metal thiolate and disulfide compounds has been extensively investigated for copper, but not for other transition metal ions.

Promotor: A.P. IJzerman

Promotor: A.P. IJzerman

Leiden chemists have proposed a new model for enzymatic reactions, in which the flexibility of the substrate is much more important than previously thought. Their results are paradigm-shifting and could have major implications for drug research and enzyme engineering. Publication in Angewandte Chemi…

Self-assembly is an abundant process in nature and is vital to many processes in living organisms.

Glycoconjugate vaccines are composed of microbial poly- or oligosaccharides covalently linked to a carrier protein.

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

Source: Eur J Med Chem, Volume 101, pp. 681-91 (2015)

Source: Structure , Volume 22, Issue 8, pp. 1120-1139 (2014)

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…