Andrew S. Doré

TL;DR: The structures of a thermostabilized adenosine A(2A) receptor in complex with the xanthines xanthine amine congener and caffeine, as well as the A( 2A) selective inverse agonist ZM241385 are reported, providing new insight into the features that define the ligand binding pocket of theAdenosine receptor for ligands of diverse chemotypes aswell as the cytoplasmic regions that interact with signal transduction proteins.

TL;DR: The crystal structure of the transmembrane domain of the human corticotropin-releasing factor receptor type 1 in complex with the small-molecule antagonist CP-376395 is reported and provides detailed insight into the architecture of class B receptors.

TL;DR: It is demonstrated that serial millisecond crystallography at a synchrotron beamline equipped with high-viscosity injector and high frame-rate detector allows typical crystallographic experiments to be performed at room-temperature.

TL;DR: The structure of a thermostabilized human A1 receptor at 3.3 Å resolution with PSB36, an A1-selective xanthine-based antagonist is reported, and the structural differences confirmed to lead to selectivity can be utilized in the design of new subtype- selective A1R or A2AR antagonists.

TL;DR: Light is shed on a structural determinant of ligand dissociation kinetics and a means by which this property may be optimized in G protein-coupled receptors.