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 …
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …
Overview of recent strategic advances in medicinal chemistry
G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
Introducing novel strategies, concepts, and technologies that speed up drug discovery and
the drug development cycle is of great importance both in the highly competitive …
the drug development cycle is of great importance both in the highly competitive …
Structure of an allosteric modulator bound to the CB1 cannabinoid receptor
The CB1 receptor mediates the central nervous system response to cannabinoids, and is a
drug target for pain, anxiety and seizures. CB1 also responds to allosteric modulators, which …
drug target for pain, anxiety and seizures. CB1 also responds to allosteric modulators, which …
Enantiospecific allosteric modulation of cannabinoid 1 receptor
RB Laprairie, PM Kulkarni, JR Deschamps… - ACS chemical …, 2017 - ACS Publications
The cannabinoid 1 receptor (CB1R) is one of the most widely expressed metabotropic G
protein-coupled receptors in brain, and its participation in various (patho) physiological …
protein-coupled receptors in brain, and its participation in various (patho) physiological …
Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets
S Mallipeddi, DR Janero, N Zvonok… - Biochemical …, 2017 - Elsevier
The phenomenon of functional selectivity, whereby a ligand preferentially directs the
information output of a G-protein coupled receptor (GPCR) along (a) particular effector …
information output of a G-protein coupled receptor (GPCR) along (a) particular effector …
Allosteric modulation: an alternate approach targeting the cannabinoid CB1 receptor
The cannabinoid CB1 receptor is a G protein coupled receptor and plays an important role
in many biological processes and physiological functions. A variety of CB1 receptor agonists …
in many biological processes and physiological functions. A variety of CB1 receptor agonists …
Visible‐Light‐Mediated Synthesis of β‐Chloro Ketones from Aryl Cyclopropanes
D Petzold, P Singh, F Almqvist… - Angewandte Chemie …, 2019 - Wiley Online Library
We report the visible‐light‐mediated synthesis of β‐chloro ketones from aryl cyclopropanes,
oxygen, hydrochloric acid, and nitric acid. The operationally simple and catalyst‐free method …
oxygen, hydrochloric acid, and nitric acid. The operationally simple and catalyst‐free method …
Impact of allosteric modulation in drug discovery: innovation in emerging chemical modalities
B Han, FG Salituro, MJ Blanco - ACS Medicinal Chemistry Letters, 2020 - ACS Publications
Recent years have seen an unprecedented level of innovation in allosteric drug discovery
and development, with multiple drug candidates advancing into clinical studies. From early …
and development, with multiple drug candidates advancing into clinical studies. From early …
The role of cannabinoids in allergic diseases: Collegium Internationale Allergologicum (CIA) update 2020
A Angelina, M Pérez-Diego, J López-Abente… - International archives of …, 2020 - karger.com
The human endocannabinoid system (ECS) is a complex signalling network involved in
many key physiological processes. The ECS includes the cannabinoid receptors, the …
many key physiological processes. The ECS includes the cannabinoid receptors, the …
Opioid receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
Opioid and opioid-like receptors are activated by a variety of endogenous peptides including
[Met] enkephalin (met),[Leu] enkephalin (leu), β-endorphin (β-end), α-neodynorphin …
[Met] enkephalin (met),[Leu] enkephalin (leu), β-endorphin (β-end), α-neodynorphin …