Work from K4DD partner Heptares has resulted in a publication in the high-impact journal Structure. The comprehensive study describes the structure of the Adenosine A1 and A2A receptors with xanthine-based ligands.
The Adenonsine receptors are expressed in many cell types and have been suggested to be good therapeutic targets in treating a wide variety of CNS, cardiovascular, respiratory, and renal disorders. Through comparison of the structures of the A1 and A2A receptors with xanthine-based ligands, the Heptares researchers identified important selectivity determinants for xanthine-based ligands. The identification of the selectivity determinants within the different Adenosine subtypes can be utilized in the design of new subtype-selective antagonist. The article was also selected as an inspiration for the cover of the Journal. Both caffeine and chocolate are well known xanthine like substance, hence the cover design.