British Journal of Pharmacology, EarlyView.Theorized mechanism of dopamine homeostasis restoration in the nucleus accumbens core induced by a psychedelic intervention. Abstract Psychedelics have garnered great attention in recent years as treatments for major depressive disorder (MDD) and treatment‐resistant depression because of their ability to alter consciousness and afflicted cognitive ...
Lucas Wittenkeller +3 more
wiley +1 more source
Is there a role for cannabidiol in obesity, metabolic syndrome and binge eating?
British Journal of Pharmacology, EarlyView.Cannabidiol (CBD) is one of the most abundant phytocannabinoids isolated from the Cannabis sativa plant. CBD is a lipophilic, non‐intoxicating substance that differently from Δ9‐tetrahydrocannabinol (Δ9‐THC) does not present the typical profile of a drug of abuse.
Luca Botticelli +7 more
wiley +1 more source
The mechanism of allosteric regulation of calcium-independent phospholipase A<sub>2</sub> by ATP and calmodulin binding to the ankyrin domain. [PDF]
Proc Natl Acad Sci U S AMouchlis VD +6 more
europepmc +1 more source
The potential for biased signalling in the P2Y receptor family of GPCRs
British Journal of Pharmacology, EarlyView.The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk +2 more
wiley +1 more source
British Journal of Pharmacology, EarlyView.Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz +8 more
wiley +1 more source
Novel approaches for drug development against chronic primary pain: A systematic review
British Journal of Pharmacology, EarlyView.Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus +5 more
wiley +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
British Journal of Pharmacology, EarlyView.Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Purine nucleosides replace cAMP in allosteric regulation of PKA in trypanosomatid pathogens. [PDF]
ElifeOber VT +8 more
europepmc +1 more source
Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries
British Journal of Pharmacology, EarlyView.Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley +1 more source
Allosteric regulation of Keap1 by 8β-hydroxy-α-cyclocostunolide for the treatment of acute lung injury. [PDF]
Acta Pharm Sin BZhang J +7 more
europepmc +1 more source