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 …

An update on the clinical pharmacology of kratom: uses, abuse potential, and future considerations

CR McCurdy, A Sharma, KE Smith… - Expert Review of …, 2024 - Taylor & Francis
ABSTRACT Introduction Kratom (Mitragyna speciosa) has generated substantial clinical and
scientific interest as a complex natural product. Its predominant alkaloid mitragynine and …

Structures of the entire human opioid receptor family

Y Wang, Y Zhuang, JF DiBerto, XE Zhou, GP Schmitz… - Cell, 2023 - cell.com
Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …

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 …

Ligand recognition and G-protein coupling of trace amine receptor TAAR1

Z Xu, L Guo, J Yu, S Shen, C Wu, W Zhang, C Zhao… - Nature, 2023 - nature.com
Trace-amine-associated receptors (TAARs), a group of biogenic amine receptors, have
essential roles in neurological and metabolic homeostasis. They recognize diverse …

Cryo-EM structures of human GPR34 enable the identification of selective antagonists

A Xia, X Yong, C Zhang, G Lin, G Jia… - Proceedings of the …, 2023 - National Acad Sciences
GPR34 is a functional G-protein-coupled receptor of Lysophosphatidylserine (LysoPS), and
has pathogenic roles in numerous diseases, yet remains poorly targeted. We herein report a …

Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation

C Zhao, H Wang, Y Liu, L Cheng, B Wang, X Tian, H Fu… - Molecular Cell, 2023 - cell.com
Summary Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …

Time-resolved cryo-EM of G-protein activation by a GPCR

MM Papasergi-Scott, G Pérez-Hernández, H Batebi… - Nature, 2024 - nature.com
G-protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by stimulating
guanine nucleotide exchange in the Gα subunit. To visualize this mechanism, we developed …

Structure–Activity Relationship Study of Cannabidiol-Based Analogs as Negative Allosteric Modulators of the μ-Opioid Receptor

T Bosquez-Berger, JA Gudorf, CP Kuntz… - Journal of Medicinal …, 2023 - ACS Publications
The US faces an unprecedented surge in fatal drug overdoses. Naloxone, the only antidote
for opiate overdose, competes at the mu opioid receptor (μOR) orthosteric site. Naloxone …

[HTML][HTML] IUPHAR themed review: Opioid efficacy, bias, and selectivity

N Ramos-Gonzalez, B Paul, S Majumdar - Pharmacological research, 2023 - Elsevier
Drugs acting at the opioid receptor family are clinically used to treat chronic and acute pain,
though they represent the second line of treatment behind GABA analogs, antidepressants …