During the congress of the Royal Dutch Association for the Advancement of Pharmacy (Koninklijke Nederlandse Maatschappij ter bevordering der Pharmacie, KNMP) Jacqueline Gerritsen, former student Bio-Pharmaceutical Sciences at Leiden University, was awarded the KNMP student prize.

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…

The Oncode Institute is a new international network organisation that focuses on making sure that new scientific findings on cancer are implemented in patients as rapidly as possible. Two young female researchers at Leiden University have been selected to join Oncode: Laura Heiman (Leiden Academic…

On Friday May 3rd 2013 NWO has announced that Dr. Mario van der Stelt, Division of Bio-Organic Synthesis (LIC) and Dr. Laura Heitman, Division of Medicinal Chemistry (LACDR), have been awarded with an ECHO-STIP grant for their project, entitled: “Novel target engagement biomarkers for better drug ca…

Fundamental and clinical knowledge is needed to develop new, groundbreaking drugs. Physicians, pharmacists, biochemists, chemists and mathematicians from Leiden University and the Leiden University Medical Center (LUMC) work closely together in the hunt for the clues and building blocks that could lead…

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.

Potential drugs that seem promising in the lab, but don’t show any activity in a person: they cost the industry an incredible amount of time and money. That’s why Indira Nederpelt focuses on a more efficient search for new drugs in her PhD, by determining the kinetics of a potential drug earlier on…

Pharmaceutical research should make more use of data science, says Gerard van Westen, postdoctoral fellow at the Leiden Academic Centre for Drug Research (LACDR). ‘If we want to have better drugs, we should start with data.’

Lecture

Lecture

Lecture

Lecture

Conference

Conference

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…

During the course of drug discovery translational steps are made.

Source: Bioorg Med Chem, Volume 23, Issue 14, pp. 4034-49 (2015)

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.

In this study, we evaluated the influence of supercritical carbon dioxide (scCO2) spray drying conditions, in the absence of organic solvent, on the ability to produce dry protein/trehalose formulations at 1:10 and 1:4 (w/w) ratios.

Both psoriasis and atheroslcerosis are diseases characterized by a chronic and systemic inflammatory profile with local lipid disturbances that alter the barrier function of the skin (psoriasis) and cause the development of atherosclerotic plaques (atherosclerosis).

PURPOSE: In the present study we investigated the root-cause of an interference signal (100-200 nm) of sugar-containing solutions in dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA) and its consequences for the analysis of particles in biopharmaceutical drug products.

In this thesis, the focus lies on studying glucocorticoid receptor dynamics in living cells with the aim of understanding how this transcription factor finds its DNA target sites to regulate transcription.

Promotor: Prof.dr. E.J.J. Groenen

An integrated approach for the simultaneous prediction of polypharmacology and binding affinity/potency of small molecules.

Can we determine the 3D structure of a chemotaxis core complex using single-particle reconstructions via cryo-EM?

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

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

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

Supervisor: Gerard van Westen

Promotor: Prof.dr. C.A.M.J.J. van den Hondel, Dr. ir. V. Meyer, Co-promotor: Dr. A.F.J. Ram

Promotor: W. Jiskoot, Co-promotor: A. Hawe

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

Promotores: F.H.J. Redig, W.T.F. den Hollander

Oxidation is a common degradation pathway that affects therapeutic proteins and peptides during production, purification, formulation, transportation, storage and handling of solid and liquid preparations. In the present work we review the scientific literature about structural and biological consequences…

The aim of the research presented in this thesis was to develop new methods forchallenging systems in liquid-state NMR using paramagnetic effects generated by thetwo-armed probe CLaNP-5.

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

Supervisor: P.J.J. Hooykaas Co-Supervisor: R. Offringa

Structure-affinity relationship (SAR) and structure-kinetics relationship (SKR) studies were combined to investigate a series of biphenyl anthranilic acid agonists for the HCA2 receptor.

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

In our research protein translocation from Agrobacterium into yeast and plant cells is studied to obtain fundamental insights in the translocation process

Developing robust and comprehensive analytical methods to size and quantify subvisible particles in biopharmaceutical products.

The main subject of this thesis is the design and synthesis of paramagnetic molecules for protein studies with NMR and EPR spectroscopy.

In the last decades, activity-based protein profiling (ABPP) has emerged as a powerful chemical tool that may aid the ever-challenging drug discovery process.

How can we develop a new microscope that can distinguish individual atoms in proteins?

Promotor: Prof.dr. M. Ubbink