Andrei Zhukov

TL;DR: In vivo pharmacokinetic and efficacy data for compound 4k are presented, demonstrating the potential of this series of compounds for the treatment of Parkinson’s disease.

TL;DR: Crystal structures of PAR2 in complex with two distinct antagonists and a blocking antibody provide a basis for the development of selective PAR2 antagonists for a range of therapeutic uses.

TL;DR: It is demonstrated how protein engineering methods can be used to identify mutations which can both increase the thermostability of receptors, when purified in detergent, as well as biasing the receptor towards a specific physiologically relevant conformational state.

TL;DR: Virtual screening was performed against experimentally enabled homology models of the adenosine A2A receptor, identifying a diverse range of ligand efficient antagonists (hit rate 9%) and optimized to potent and selective lead molecules.

TL;DR: Results of biophysical mapping of the adenosine A2A receptor are presented, which identify key protein–ligand interactions and allow the shape of the site to be refined to produce a high quality three-dimensional picture of ligand binding, thereby facilitating structure based drug design.