The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …

G protein-coupled receptors (GPCRs) are of considerable interest due to their importance in
a wide range of physiological functions and in a large number of Food and Drug …

Carvedilol is among the most effective β-blockers for improving survival after myocardial
infarction. Yet the mechanisms by which carvedilol achieves this superior clinical profile are …

The introduction of β-adrenergic receptor blockers,“β-blockers”, as a treatment for heart
failure decades ago was a major advance in cardiovascular medicine 1–4. Moreover, it has …

Activation of β2-adrenoceptors (β2ARs) causes airway smooth muscle (ASM) relaxation and
bronchodilation, and β2AR agonists (β-agonists) are front-line treatments for asthma and …

Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs)
and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions …

G protein-coupled receptors (GPCRs), comprising the largest superfamily of cell surface
receptors, serve as fundamental modulators of cardiac health and disease owing to their key …

Among β-blockers that are clinically prescribed for heart failure, carvedilol is a first-choice
agent with unique pharmacological properties. Carvedilol is distinct from other β-blockers in …

Heart failure (HF) carries the highest mortality in the western world and β-blockers [β-
adrenergic receptor (AR) antagonists] are part of the cornerstone pharmacotherapy for post …

Introduction Strong scientific evidence and large experience support the use of β2-agonists
for the symptomatic alleviation of COPD. Therefore, there is considerable effort in …