Biased ligands at opioid receptors: Current status and future directions
The opioid crisis represents a major worldwide public health crisis that has accelerated the
search for safer and more effective opioids. Over the past few years, the identification of …
search for safer and more effective opioids. Over the past few years, the identification of …
Structure, function and pharmacology of human itch GPCRs
The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …
Molecular mechanism of biased signaling at the kappa opioid receptor
The κ-opioid receptor (KOR) has emerged as an attractive drug target for pain management
without addiction, and biased signaling through particular pathways of KOR may be key to …
without addiction, and biased signaling through particular pathways of KOR may be key to …
Structure determination of inactive-state GPCRs with a universal nanobody
Cryogenic electron microscopy (cryo-EM) has widened the field of structure-based drug
discovery by allowing for routine determination of membrane protein structures previously …
discovery by allowing for routine determination of membrane protein structures previously …
Ligand and G-protein selectivity in the κ-opioid receptor
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not
only pain but also addiction and affective disorders. However, the development of KOR …
only pain but also addiction and affective disorders. However, the development of KOR …
Subcellular location defines GPCR signal transduction
A Radoux-Mergault, L Oberhauser, S Aureli… - Science …, 2023 - science.org
Intracellular G protein-coupled receptors (GPCRs) can be activated by permeant ligands,
which contributes to agonist selectivity. Opioid receptors (ORs) provide a notable example …
which contributes to agonist selectivity. Opioid receptors (ORs) provide a notable example …
Exploring cellular biochemistry with nanobodies
RW Cheloha, TJ Harmand, C Wijne… - Journal of Biological …, 2020 - ASBMB
Reagents that bind tightly and specifically to biomolecules of interest remain essential in the
exploration of biology and in their ultimate application to medicine. Besides ligands for …
exploration of biology and in their ultimate application to medicine. Besides ligands for …
Compartmentalized GPCR signaling from intracellular membranes
SE Crilly, MA Puthenveedu - The Journal of Membrane Biology, 2021 - Springer
G protein-coupled receptors (GPCRs) are integral membrane proteins that transduce a wide
array of inputs including light, ions, hormones, and neurotransmitters into intracellular …
array of inputs including light, ions, hormones, and neurotransmitters into intracellular …
Structural basis of α1A-adrenergic receptor activation and recognition by an extracellular nanobody
Y Toyoda, A Zhu, F Kong, S Shan, J Zhao… - Nature …, 2023 - nature.com
The α1A-adrenergic receptor (α1AAR) belongs to the family of G protein-coupled receptors
that respond to adrenaline and noradrenaline. α1AAR is involved in smooth muscle …
that respond to adrenaline and noradrenaline. α1AAR is involved in smooth muscle …