Results 221 to 230 of about 22,949 (304)

Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells. [PDF]

Nat Commun
Uguen M, Shell DJ, Silva M, Deng Y, Li F, Szewczyk MM, Yang K, Zhao Y, Stashko MA, Norris-Drouin JL, Waybright JM, Beldar S, Rectenwald JM, Mordant AL, Webb TS, Herring LE, Arrowsmith CH, Ackloo S, Gygi SP, McGinty RK, Barsyte-Lovejoy D, Liu P, Halabelian L, James LI, Pearce KH, Frye SV.   +25 more
europepmc   +1 more source

Non‐canonical PKG1 regulation in cardiovascular health and disease

British Journal of Pharmacology, EarlyView.
It is well established that the cyclic GMP‐dependent protein kinase I (PKG1) is canonically activated by cyclic guanosine monophosphate (cGMP), enabling its regulation of vascular tone, cardiac function and smooth muscle homeostasis. However, diverse non‐canonical stimuli of PKG1 have also been identified.
Jie Su, Joseph Robert Burgoyne
wiley   +1 more source

Application of Deuterium in an M₁ Positive Allosteric Modulator Back-Up Program: The Discovery of VU6045422. [PDF]

ACS Chem Neurosci
Engers JL, Li J, Han C, Long MF, Gregro AR, Presley CC, Dickerson JW, Peng W, Cho HP, Rodriguez AL, Xiang Z, Boutaud O, O'Carroll C, Dey PM, Burstein ES, Niswender CM, Rook JM, Conn PJ, Engers DW, Lindsley CW.   +19 more
europepmc   +1 more source

Psychedelics as pharmacotherapeutics for substance use disorders: A scoping review on clinical trials and perspectives on underlying neurobiology

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, Gary Gudelsky, T. John Winhusen, Davide Amato   +3 more
wiley   +1 more source

The efficacy of an allosteric modulator of the alpha 7 nicotinic acetylcholine receptor in a murine model of stroke. [PDF]

Front Neurosci
Hernandez K, Jones N, Ortega SB.
europepmc   +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, Emanuela Micioni Di Bonaventura, Giacomo Einaudi, Gustavo Provensi, Alessia Costa, Claudio D'Addario, Carlo Cifani, Maria Vittoria Micioni Di Bonaventura   +7 more
wiley   +1 more source

Formulation and characterization of CMPI nanoparticles for enhanced targeting of brain nicotinic receptors by positive allosteric modulator. [PDF]

Sci Rep
Aly R, Sulthana S, Beaudoin R, Hamouda AK, Aryal S.   +4 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, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

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, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source