Recent advances in structural biology and computational techniques have revealed
allosteric mechanisms for an abundance of targets leading to the establishment of rational …

The benzoxazole moiety is widely found in various natural compounds, which are often
found to be biologically active. Due to its versatile biological properties, benzoxazole has …

Genetically-encoded dopamine (DA) sensors enable high-resolution imaging of DA release,
but their ability to detect a wide range of extracellular DA levels, especially tonic versus …

A variety of G protein-coupled receptors (GPCRs) have been implicated in the pathogenesis
of pulmonary fibrosis, largely through their promotion of profibrotic fibroblast activation. By …

Dopamine controls diverse behaviors and their dysregulation contributes to many disorders.
Our ability to understand and manipulate the function of dopamine is limited by the …

The five dopamine receptor subtypes (D1–5) are activated by the endogenous
catecholamine dopamine. Sustained research has sought to identify selective ligands for …

Clinical development of catechol-based orthosteric agonists of the dopamine D1 receptor
has thus far been unsuccessful due to multiple challenges. To address these issues, we …

Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in
medicinal chemistry. Allosteric modulators, ie, compounds which bind in a receptor site …

Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major
mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in …

Our understanding of the structural biology of G protein-coupled receptors has undergone a
transformation over the past 5 years. New protein–ligand complexes are described almost …