“Magic chloro”: profound effects of the chlorine atom in drug discovery
D Chiodi, Y Ishihara - Journal of Medicinal Chemistry, 2023 - ACS Publications
Chlorine is one of the most common atoms present in small-molecule drugs beyond carbon,
hydrogen, nitrogen, and oxygen. There are currently more than 250 FDA-approved chlorine …
hydrogen, nitrogen, and oxygen. There are currently more than 250 FDA-approved chlorine …
CB1 cannabinoid receptor signaling and biased signaling
LM Leo, ME Abood - Molecules, 2021 - mdpi.com
The CB1 cannabinoid receptor is a G-protein coupled receptor highly expressed throughout
the central nervous system that is a promising target for the treatment of various disorders …
the central nervous system that is a promising target for the treatment of various disorders …
The Magic Methyl and Its Tricks in Drug Discovery and Development
One of the key scientific aspects of small-molecule drug discovery and development is the
analysis of the relationship between its chemical structure and biological activity …
analysis of the relationship between its chemical structure and biological activity …
The endocannabinoid system as a putative target for the development of novel drugs for the treatment of psychiatric illnesses
Cannabis is well established to impact affective states, emotion and perceptual processing,
primarily through its interactions with the endocannabinoid system. While cannabis use is …
primarily through its interactions with the endocannabinoid system. While cannabis use is …
Endocannabinoid signaling in the central nervous system
CE Martinez Ramirez, G Ruiz‐Pérez, TM Stollenwerk… - Glia, 2023 - Wiley Online Library
It is hard to overestimate the influence of the endocannabinoid signaling (ECS) system on
central nervous system (CNS) function. In the 40 years since cannabinoids were found to …
central nervous system (CNS) function. In the 40 years since cannabinoids were found to …
Targeting the endocannabinoid system: Structural determinants and molecular mechanism of allosteric modulation
Highlights•This review paper presents an overview of the recent findings on the allosteric
modulation of cannabinoid receptors.•Six categories of allosteric modulators have new …
modulation of cannabinoid receptors.•Six categories of allosteric modulators have new …
Modulation of type 1 cannabinoid receptor activity by cannabinoid by-products from Cannabis sativa and non-cannabis phytomolecules
A Zagzoog, A Cabecinha, H Abramovici… - Frontiers in …, 2022 - frontiersin.org
Cannabis sativa contains more than 120 cannabinoids and 400 terpene compounds (ie,
phytomolecules) present in varying amounts. Cannabis is increasingly available for legal …
phytomolecules) present in varying amounts. Cannabis is increasingly available for legal …
In Vitro Characterization of 6-Methyl-3-(2-nitro-1-(thiophen-2-yl)ethyl)-2-phenyl-1H-indole (ZCZ011) at the Type 1 Cannabinoid Receptor: Allosteric Agonist or …
Orthosteric activation of CB1 is known to cause a plethora of adverse side effects in vivo.
Allosteric modulation is an exciting therapeutic approach and is hoped to offer improved …
Allosteric modulation is an exciting therapeutic approach and is hoped to offer improved …
Structure-based identification of a G protein–biased allosteric modulator of cannabinoid receptor CB1
S Shen, C Wu, G Lin, X Yang, Y Zhou… - Proceedings of the …, 2024 - National Acad Sciences
Cannabis sativa is known for its therapeutic benefit in various diseases including pain relief
by targeting cannabinoid receptors. The primary component of cannabis, Δ9 …
by targeting cannabinoid receptors. The primary component of cannabis, Δ9 …
Progress on the development of Class A GPCR‐biased ligands
P Morales, MM Scharf, M Bermudez… - British Journal of …, 2024 - Wiley Online Library
Class AG protein‐coupled receptors (GPCRs) continue to garner interest for their essential
roles in cell signalling and their importance as drug targets. Although numerous drugs in the …
roles in cell signalling and their importance as drug targets. Although numerous drugs in the …