Biased ligands at opioid receptors: Current status and future directions

T Che, H Dwivedi-Agnihotri, AK Shukla, BL Roth - Science signaling, 2021 - science.org
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 …

Molecular basis of opioid receptor signaling

T Che, BL Roth - Cell, 2023 - cell.com
Opioids are used for pain management despite the side effects that contribute to the opioid
crisis. The pursuit of non-addictive opioid analgesics remains unattained due to the …

Structure, function and pharmacology of human itch GPCRs

C Cao, HJ Kang, I Singh, H Chen, C Zhang, W Ye… - Nature, 2021 - nature.com
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 …

Molecular mechanism of biased signaling at the kappa opioid receptor

A El Daibani, JM Paggi, K Kim, YD Laloudakis… - Nature …, 2023 - nature.com
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 …

Structure determination of inactive-state GPCRs with a universal nanobody

MJ Robertson, MM Papasergi-Scott, F He… - Nature Structural & …, 2022 - nature.com
Cryogenic electron microscopy (cryo-EM) has widened the field of structure-based drug
discovery by allowing for routine determination of membrane protein structures previously …

Ligand and G-protein selectivity in the κ-opioid receptor

J Han, J Zhang, AL Nazarova, SM Bernhard… - Nature, 2023 - nature.com
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 …

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 …

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 …

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 …

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 …