Aim of the course
This Course consists of a general part and a Research Cluster specific part that gives an overview of current research activities within the research cluster Drug & Target Discovery. After the theoretical part, the students will perform their research internship within one (or both) of the divisions of this LACDR research cluster, i.e. Medical Chemistry or Toxicology, and gain in-depth knowledge on one of their research topics.
Cancer is a leading cause of death, which is mainly due to the drug resistant phenotype of metastatic cells. The aim in the cluster is to understand the signalling processes and cellular behavior in metastatic cancer that drive cancer progression and that could be targeted by effective and safe therapy. We therefore focus on understanding cell migration, proliferation, and (resistance to) death by therapeutics or immune cells. Our main emphasis is on the two most important classes of drug targets in cancer, i.e. kinases and G protein-coupled receptors (GPCRs). These targets are highly ‘druggable’, which we try to exploit in our drug discovery efforts. Novel concepts of drug action such as allosteric modulation and target residence time are integrated in our research. This ‘new’ pharmacology enables a thorough preclinical evaluation, leading to a highly educated lead optimisation. We employ a multidisciplinary approach to understand and improve drug action, including (tumor) cell biology, automated fluorescence microscopy, cheminformatics, chemistry, molecular pharmacology and computational biology.
Dr. J.B. Beltman and Dr. L.H. Heitman.
First year Bio-Pharmaceutical Sciences master students
Mode of instruction
The overview of the research activities in the cluster occurs by means of lectures that are supported by computer exercises, all taking place in the first week after the general part. The thus acquired background information fully prepares the participating master students for the third part of the course, which involves the writing of their own project proposal in the third and fourth week. Project proposals are reviewed by individual supervisors and by fellow students. Finally, the students present and defend their proposals, after which they can start their first research project.
Following the general introduction of the LACDR in the first week, the second part of this course specifically introduces the research activities within the cluster ‘Drug & Target Discovery’. The students will study the following topics:
Drug targets involved in cancer
Modelling of signal transduction
(Computational) target discovery
In vitro drug activity
Preclinical animal models
Active participation, a written exam, scientific writing and content of research proposal and presentation skills.