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 …

G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

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 …

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 …

Structural and signaling mechanisms of TAAR1 enabled preferential agonist design

P Shang, N Rong, JJ Jiang, J Cheng, MH Zhang… - Cell, 2023 - cell.com
Trace amine-associated receptor 1 (TAAR1) senses a spectrum of endogenous amine-
containing metabolites (EAMs) to mediate diverse psychological functions and is useful for …

Cryo-EM structure of the endothelin-1-ETB-Gi complex

FK Sano, H Akasaka, W Shihoya, O Nureki - elife, 2023 - elifesciences.org
The endothelin ET B receptor is a promiscuous G-protein coupled receptor that is activated
by vasoactive peptide endothelins. ET B signaling induces reactive astrocytes in the brain …

Snapshot of the cannabinoid receptor 1-arrestin complex unravels the biased signaling mechanism

YY Liao, H Zhang, Q Shen, C Cai, Y Ding, DD Shen… - Cell, 2023 - cell.com
Cannabis activates the cannabinoid receptor 1 (CB1), which elicits analgesic and emotion
regulation benefits, along with adverse effects, via G i and β-arrestin signaling pathways …

Anti-diarrheal effect of piperine possibly through the interaction with inflammation inducing enzymes: In vivo and in silico studies

M Afroz, MS Bhuia, MA Rahman, R Hasan… - European Journal of …, 2024 - Elsevier
Piperine is a natural alkaloid that possesses a variety of therapeutic properties, including
anti-inflammatory, antioxidant, antibacterial, and anticarcinogenic activities. The present …

Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide

MM Vandeputte, MHM Tsai, L Chen… - Drug and alcohol …, 2023 - Elsevier
Background The emergence of novel synthetic opioids (NSOs) is contributing to the opioid
overdose crisis. While fentanyl analogs have historically dominated the NSO market, a shift …

Fentanyl and the fluorinated fentanyl derivative NFEPP elicit distinct hydrogen-bond dynamics of the opioid receptor

S Lešnik, U Bren, T Domratcheva… - Journal of chemical …, 2023 - ACS Publications
The development of safe therapeutics to manage pain is of central interest for biomedical
applications. The fluorinated fentanyl derivative N-(3-fluoro-1-phenethylpiperidin-4-yl)-N …