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 …
critical role in numerous human physiological and pathological conditions. Thus …
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 …
GPCR activation mechanisms across classes and macro/microscales
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 …
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 …
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
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 …
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …
Structural basis of CXC chemokine receptor 2 activation and signalling
Chemokines and their receptors mediate cell migration, which influences multiple
fundamental biological processes and disease conditions such as inflammation and cancer …
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 …
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 …
(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 …
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 …
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …