GPCRs exhibit a common architecture of seven transmembrane helices (TMs) linked by
intracellular loops and extracellular loops (ECLs). Given their peripheral location to the site …

During evolution, mammals have developed remarkably similar molecular mechanisms to
respond to external challenges and maintain survival. Critical regulators of these …

Molecular determinants regulating the activation of class B G-protein-coupled receptors
(GPCRs) by native peptide agonists are largely unknown. We have investigated here the …

The extracellular loops (ECLs) of G protein-coupled receptors (GPCRs) can bind directly to
docked orthosteric or allosteric ligands, they can contain transient contact points for ligand …

Corticotropin-releasing hormone (CRH) is a key player of basal and stress-activated
responses in the hypothalamic–pituitary–adrenal axis (HPA) and in extrahypothalamic …

Although family BG protein-coupled receptors (GPCRs) contain only 15 members, they play
key roles in transmembrane signal transduction of hormones. Family B GPCRs are drug …

The important and diverse biological functions of β-adrenergic receptors (βARs) have
promoted the search for compounds to stimulate or inhibit their activity. In this regard …

Recent solved structures of G protein-coupled receptors (GPCRs) provide insights into
variation of the structure and molecular mechanisms of GPCR activation. In this review, we …

The calcitonin receptor (CTR) and calcitonin receptor‐like receptor (CLR) are two of the 15
human family B (or Secretin‐like) GPCRs. CTR and CLR are of considerable biological …

The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR
ADGRF5/GPR116 have not been completely deciphered. We set out to investigate the …