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.

Wiskunde en Natuurwetenschappen, Leiden Academic Centre for Drug Research (LACDR)

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.

Supervisor: Andrea Martella

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

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.

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.

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

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

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).

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

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…

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.

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…

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…

Promotores: Wim Jiskoot; Ferry Ossendorp

Supervisor: Lizi Xia

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…

Promotor: A.P. IJzerman

Promotor: A.P. IJzerman

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.

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.

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…

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

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: 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…

Central in coordination and organometallic chemistry is the synthesis of new chelating ligands, the synthesis and characterization of metal complexes with these ligands, and the study of their properties. An important goal in my research is to create understanding of the relation between the structures…

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