Biophysical sensors in studies on pharmacologically-dark G protein-coupled receptors | Insights from Pawel Kozielewicz

The class F (Frizzled, FZD) GPCRs are important in development and signalling and are implicated in a diverse range of diseases. However the FZDs have been very challenging to investigate with limited number of high-throughput biological assays available.

Pawel Kozielewicz is Assistant Professor at the Karolinska Institutet and is currently setting up his own research team working on Molecular Pharmacology of G protein-coupled receptors (GPCRs).

He will be talking about the development of biophysical techniques used to research conformational changes, ligand / receptor interactions and signalling in in vitro models. One aim of this work was to develop a set of tools to be later used in a high-throughput screen to identify small molecules for potential therapeutic uses as the current large molecule therapeutics do not show good selectivity. In the longer term, these techniques are to be applied to orphan GPCRs opening up new druggable targets.

Pawel will be speaking at ELRIG’s Advances in Cell-based Screening in Drug Discovery conference in Gothenburg, on 16th May in the scientific track ‘Maximising outputs – how next-generation endpoints, and the use of biosensor are feeding a new wave of multiparametric data generation.’

Pawel will be discussing his talk “Biophysical sensors in studies on pharmacologically-dark G protein-coupled receptors” at the Advances in Cell-based Screening 2024 Conference in Gothenburg to find out more.

Join him on 16 May in the scientific track ‘New Technologies – a look under the hood of new leading technological platforms and how they are revolutionising drug discovery.’

More about Pawel Kozielewicz

I graduated with a Master’s of Pharmacy degree from the Medical University of Warsaw, Poland. Next, I did my PhD as a Marie Curie Fellow with Prof. Nicholas M. Barnes at the University of Birmingham and Celentyx Ltd., UK (immunological and neuropharmacological studies on therapeutical drugs and targets, including orphan G protein-coupled receptors, GPCRs). I had my first post-doctoral stay in the lab of Prof. Agnieszka Chacinska at the IIMCB, Warsaw, Poland (protein biogenesis in synaptoneurosomes). In August 2017, I joined Prof. Gunnar Schulte’s lab for my second post-doc. In my post-doctoral research in the Schulte lab, I focused on exploring the pharmacology of class F (Frizzleds) GPCRs by employing structural-functional analysis. It can be argued that, given certain ambiguities which exist about the molecular mechanism of action of these proteins, Frizzleds are similar to another class of the seven transmembrane-spanning receptors: orphan GPCRs. I am currently setting up my independent team and line of research to investigate the role of orphan GPCRs in health and diseases.