Highlights•GPCRs are key players in cell-cell communication and pass the signal via
coordinated action of switches.•There are two types of switches: toggle switches and …

Allosteric signaling in biological molecules, which may be viewed as specific action at a
distance due to localized perturbation upon binding of ligands or changes in environmental …

Many central biological events rely on protein–ligand interactions. The identification and
characterization of protein-binding sites for ligands are crucial for the understanding of …

G protein-coupled receptors (GPCRs) are implicated in nearly every physiological process
in the human body and therefore represent an important drug targeting class. Advances in X …

The pituitary adenylate cyclase-activating polypeptide (PACAP)-selective PAC1 receptor
(PAC1R, ADCYAP1R1) is a member of the vasoactive intestinal peptide (VIP)/secretin …

G protein-coupled receptors (GPCRs) are seven transmembrane (TM) proteins that play a
key role in human physiology. The GPCR superfamily comprises about 800 members …

The CB1 cannabinoid receptor (CB1R) contains one of the longest N termini among class
AG protein-coupled receptors. Mutagenesis studies suggest that the allosteric binding site of …

Pain is both a major clinical and economic problem, affecting more people than diabetes,
heart disease, and cancer combined. While a variety of prescribed or over-the-counter …

Interactions of 21 fentanyl derivatives with μ-opioid receptor (μOR) were studied using
experimental and theoretical methods. Their binding to μOR was assessed with radioligand …

G protein-coupled receptor (GPCR) conformational plasticity enables formation of ternary
signaling complexes with intracellular proteins in response to binding extracellular ligands …