Peptides are widely used in pharmaceutical industry as active pharmaceutical ingredients,
versatile tools in drug discovery, and for drug delivery. They find themselves at the …

G protein-coupled receptors (GPCRs) allosterically activate heterotrimeric G proteins and
trigger GDP release. Given that there are∼ 800 human GPCRs and 16 different Gα genes …

Class A G-protein-coupled receptors (GPCRs) are a large family of membrane proteins that
mediate a wide variety of physiological functions, including vision, neurotransmission and …

G-protein-coupled receptors do not only feature the orthosteric pockets, where most
endogenous agonists bind, but also a multitude of other allosteric pockets that have come …

Many biological functions of peptides are mediated through G protein-coupled receptors
(GPCRs). Upon ligand binding, GPCRs undergo conformational changes that facilitate the …

Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs)
bind to extracellular ligands and drugs and modulate intracellular responses through …

Abstract β‐arrestins (βarr1 and βarr2) are ubiquitous regulators of G protein‐coupled
receptor (GPCR) signaling. Available data suggest that β‐arrestins dock to different …

We present comprehensive maps at single–amino acid resolution of the residues stabilizing
the human Gαi1 subunit in nucleotide-and receptor-bound states. We generated these maps …

Understanding the molecular basis of arrestin-mediated regulation of GPCRs is critical for
deciphering signaling mechanisms and designing functional selectivity. However, structural …

Site-directed scanning mutagenesis is a powerful protein engineering technique which
allows studies of protein functionality at single amino acid resolution and design of stabilized …