Universiteit Leiden

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Leiden Academic Centre for Drug Research

Medicinal Chemistry

What do we see as our main research areas for the years to come?

Well, perhaps we should say here that next to being our "pet" receptors, adenosine receptors are also prototypic receptors to us. They serve as templates for more general questions regarding e.g., novel concepts in receptor research, the search for ligand selectivity, cheminformatics approaches for de novo ligand design, and bioinformatics of G protein-coupled receptors. Our ultimate goal is to achieve an atomic understanding of the interaction between a drug and its receptor. 

We focus on three research-themes:

Research Theme: Novel Receptor Concepts

G protein-coupled receptors (GPCRs) constitute an important protein family of drug targets. Many drugs have been developed over the years for a range of diseases, varying from increased stomach acid secretion to depression, from asthma and high blood pressure to migraine. Today, it is estimated that approximately half of the marketed medicines act through members of this protein class.

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Research Theme: Better ligands for G Protein Coupled Receptors

A concept that has emerged in our recent research is the one of binding kinetics. Binding kinetics is notably embodied through residence time (RT), which is a direct reflection of how long a drug stays bound to its target. This parameter is of crucial importance, because drug action lasts only as long as the receptor-ligand complex exists. 

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Research Theme: Chem- and Bioinformatics of Drug Targets

Over the last five decades computers have gradually started to play a more important part in our daily lives. Science, and in particular drug discovery, is no different. Computers are invaluable in the complex process that is drug discovery, from playing a supportive role through documentation and publications of the results, to hard-core research projects being run completely in silico. In fact, this term has been added to the traditional in vitro and in vivo.

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