Targeting cannabinoid receptors: current status and prospects of natural products

D An, S Peigneur, LA Hendrickx, J Tytgat - International journal of …, 2020 - mdpi.com
Cannabinoid receptors (CB1 and CB2), as part of the endocannabinoid system, play a
critical role in numerous human physiological and pathological conditions. Thus …

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 …

GPCR activation mechanisms across classes and macro/microscales

AS Hauser, AJ Kooistra, C Munk… - Nature structural & …, 2021 - nature.com
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …

Structural basis of selective cannabinoid CB2 receptor activation

X Li, H Chang, J Bouma, LV de Paus… - Nature …, 2023 - nature.com
Abstract Cannabinoid CB2 receptor (CB2R) agonists are investigated as therapeutic agents
in the clinic. However, their molecular mode-of-action is not fully understood. Here, we report …

GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors

S Huang, P Xu, DD Shen, IA Simon, C Mao, Y Tan… - Molecular cell, 2022 - cell.com
Summary Serotonin (or 5-hydroxytryptamine, 5-HT) is an important neurotransmitter that
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …

Structural basis of CXC chemokine receptor 2 activation and signalling

K Liu, L Wu, S Yuan, M Wu, Y Xu, Q Sun, S Li, S Zhao… - Nature, 2020 - nature.com
Chemokines and their receptors mediate cell migration, which influences multiple
fundamental biological processes and disease conditions such as inflammation and cancer …

Structural basis for strychnine activation of human bitter taste receptor TAS2R46

W Xu, L Wu, S Liu, X Liu, X Cao, C Zhou, J Zhang, Y Fu… - Science, 2022 - science.org
Taste sensing is a sophisticated chemosensory process, and bitter taste perception is
mediated by type 2 taste receptors (TAS2Rs), or class TG protein–coupled receptors …

Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1

X Yang, X Wang, Z Xu, C Wu, Y Zhou, Y Wang… - Nature Chemical …, 2022 - nature.com
Given the promising clinical value of allosteric modulators of G protein-coupled-receptors
(GPCRs), mechanistic understanding of how these modulators alter GPCR function is of …

THC and CBD: Similarities and differences between siblings

N Stella - Neuron, 2023 - cell.com
Summary Δ 9-tetrahydrocannabinol (THC) and its sibling, cannabidiol (CBD), are produced
by the same Cannabis plant and have similar chemical structures but differ dramatically in …

Structural basis for activation of CB1 by an endocannabinoid analog

K Krishna Kumar, MJ Robertson, E Thadhani… - Nature …, 2023 - nature.com
Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …