A molecular simplification approach of previously reported 2-arylpyrazolo [3, 4-c] quinolin-4-
ones was applied to design 2-arylpyrazolo [4, 3-d] pyrimidin-7-one derivatives as new …

To further investigate new potent and selective human A1 adenosine receptor agonists, we
have synthesized a series of 5′-chloro-5′-deoxy-and 5′-(2-fluorophenylthio)-5′-deoxy …

Activation of a number of class AG protein-coupled receptors (GPCRs) is thought to involve
two molecular switches, a rotamer toggle switch within the transmembrane domain and an …

Abstract The Gs-coupled A2A adenosine receptor (A2AAR) has been explored extensively
as a pharmaceutical target, which has led to numerous clinical trials. However, only one …

A three-dimensional model of the human adenosine A 2B receptor was generated by means
of homology modelling, using the crystal structures of bovine rhodopsin, the β 2-adrenergic …

Like other G-protein coupled receptors with hydrophobic ligands, the human cannabinoid
receptor 1 (CB1) is thought to bind its ligands within the transmembrane region of the …

The transmembrane G-protein coupled receptor GPR109A has been previously shown to
function as a receptor for niacin in mediating antilipolytic effects. Although administration of …

G protein coupled receptors for prostaglandins are activated when agonists are bound to a
binding pocket formed in part by the seven transmembrane domains. Recent studies have …

The cystic fibrosis transmembrane conductance regulator (CFTR) is an ion channel protein
that is defective in individuals with cystic fibrosis (CF). To advance the rational design of CF …

Because they represent attractive drug targets, adrenoceptors have been widely studied.
Recent progress in structural data of β-adrenoceptors allows us to understand and predict …