Lauren T. May

TL;DR: Because of their ability to modulate receptor conformations in the presence of orthosteric ligand, allosteric modulators can "fine-tune" classical pharmacological responses, which is advantageous in terms of a potential for engendering greater GPCR subtype-selectivity, but represents a significant challenge for detecting and validating allosterIC behaviors.

TL;DR: The cryo-electron microscopy structure of the humanAdenosine A1 receptor in complex with adenosine and heterotrimeric Gi2 protein provides molecular insights into receptor and G-protein selectivity.

TL;DR: These findings provide a molecular basis for AR subtype selectivity with implications for understanding the mechanisms governing allosteric modulation of these receptors, allowing the design of more selective agents for the treatment of ischemia-reperfusion injury, renal pathologies, and neuropathic pain.

TL;DR: The apelin receptor (APJ) is often co‐expressed with the angiotensin II type‐1 receptor (AT1) and acts as an endogenous counter‐regulator and understanding this interaction may lead to new therapies for the treatment of cardiovascular disease.

TL;DR: The concept of kinetic context, at the level of both ligand-receptor and receptor-signal pathway kinetics, can have a profound impact on the observation and quantification of these phenomena.