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 …
an important class of drug targets, play a role in maintaining numerous physiological …
Structures of the entire human opioid receptor family
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 …
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 …
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 …
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 …
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 …
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
Piperine is a natural alkaloid that possesses a variety of therapeutic properties, including
anti-inflammatory, antioxidant, antibacterial, and anticarcinogenic activities. The present …
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 …
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 …
applications. The fluorinated fentanyl derivative N-(3-fluoro-1-phenethylpiperidin-4-yl)-N …