Cannabinoids and the expanded endocannabinoid system in neurological disorders

L Cristino, T Bisogno, V Di Marzo - Nature Reviews Neurology, 2020 - nature.com
Anecdotal evidence that cannabis preparations have medical benefits together with the
discovery of the psychotropic plant cannabinoid Δ9-tetrahydrocannabinol (THC) initiated …

New approaches and challenges to targeting the endocannabinoid system

V Di Marzo - Nature Reviews Drug Discovery, 2018 - nature.com
The endocannabinoid signalling system was discovered because receptors in this system
are the targets of compounds present in psychotropic preparations of Cannabis sativa. The …

A guide to targeting the endocannabinoid system in drug design

A Stasiulewicz, K Znajdek, M Grudzień… - International journal of …, 2020 - mdpi.com
The endocannabinoid system (ECS) is one of the most crucial systems in the human
organism, exhibiting multi-purpose regulatory character. It is engaged in a vast array of …

Allosteric modulation of class A GPCRs: targets, agents, and emerging concepts

EA Wold, J Chen, KA Cunningham… - Journal of medicinal …, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

Along the allostery stream: Recent advances in computational methods for allosteric drug discovery

D Ni, Z Chai, Y Wang, M Li, Z Yu, Y Liu… - Wiley …, 2022 - Wiley Online Library
Allostery is a universal, biological phenomenon in which orthosteric sites are fine‐tuned by
topologically distal allosteric sites triggered by perturbations, such as ligand binding, residue …

The endocannabinoid system as a target in cancer diseases: are we there yet?

E Moreno, M Cavic, A Krivokuca, V Casadó… - Frontiers in …, 2019 - frontiersin.org
The endocannabinoid system (ECS) has been placed in the anti-cancer spotlight in the last
decade. The immense data load published on its dual role in both tumorigenesis and …

Targeting endocannabinoid signaling: FAAH and MAG lipase inhibitors

N van Egmond, VM Straub… - Annual Review of …, 2021 - annualreviews.org
Inspired by the medicinal properties of the plant Cannabis sativa and its principal
component (−)-trans-Δ9-tetrahydrocannabinol (THC), researchers have developed a variety …

Biased ligands of G protein-coupled receptors (GPCRs): Structure–functional selectivity relationships (SFSRs) and therapeutic potential

L Tan, W Yan, JD McCorvy, J Cheng - Journal of medicinal …, 2018 - ACS Publications
G protein-coupled receptors (GPCRs) signal through both G-protein-dependent and G-
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …

Positive allosteric modulation of cannabinoid receptor type 1 suppresses pathological pain without producing tolerance or dependence

RA Slivicki, Z Xu, PM Kulkarni, RG Pertwee, K Mackie… - Biological …, 2018 - Elsevier
Background Activation of cannabinoid CB 1 receptors suppresses pathological pain but also
produces unwanted central side effects. We hypothesized that a positive allosteric modulator …

Emerging roles of allosteric modulators in the regulation of protein‐protein interactions (PPIs): A new paradigm for PPI drug discovery

D Ni, S Lu, J Zhang - Medicinal research reviews, 2019 - Wiley Online Library
Protein‐protein interactions (PPIs) are closely implicated in various types of cellular activities
and are thus pivotal to health and disease states. Given their fundamental roles in a wide …