A novel role of protein tyrosine kinase2 in mediating chloride secretion in human airway epithelial cells. [PDF]
Ca(2+) activated Cl(-) channels (CaCC) are up-regulated in cystic fibrosis (CF) airway surface epithelia. The presence and functional properties of CaCC make it a possible therapeutic target to compensate for the deficiency of Cl(-) secretion in CF ...
Lihua Liang +4 more
doaj +1 more source
Modulation of bleomycin-induced lung fibrosis by pegylated hyaluronidase and dopamine receptor antagonist in mice. [PDF]
Hyaluronidases are groups of enzymes that degrade hyaluronic acid (HA). To stop enzymatic hydrolysis we modified testicular hyaluronidase (HYAL) by activated polyethylene oxide with the help of electron-beam synthesis.
Evgenii Germanovich Skurikhin +10 more
doaj +1 more source
Psychotropic Drugs Show Anticancer Activity by Disrupting Mitochondrial and Lysosomal Function
Background and Purpose: Drug repositioning is a promising strategy for discovering new therapeutic strategies for cancer therapy. We investigated psychotropic drugs for their antitumor activity because of several epidemiological studies reporting lower ...
Marco Varalda +13 more
doaj +1 more source
The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors
The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands.
Stephen P. H. Alexander +165 more
wiley +1 more source
Improved PIEZO1 agonism through 4‐benzoic acid modification of Yoda1
Background and Purpose The protein PIEZO1 forms mechanically activated, calcium‐permeable, non‐selective cation channels in numerous cell types from several species. Options for pharmacological modulation are limited and so we modified a small‐molecule agonist at PIEZO1 channels (Yoda1) to increase the ability to modulate these channels.
Gregory Parsonage +18 more
wiley +1 more source
Chewing the fat: How lipidomics is changing our understanding of human health and disease in 2022
Abstract Lipids are biological molecules that play vital roles in all living organisms. They perform many cellular functions, such as 1) forming cellular and subcellular membranes, 2) storing and using energy, and 3) serving as chemical messengers during intra‐ and inter‐cellular signal transduction.
Caroline Géhin +2 more
wiley +1 more source
Myopia control in Mendelian forms of myopia
Abstract Purpose To study the effectiveness of high‐dose atropine for reducing eye growth in Mendelian myopia in children and mice. Methods We studied the effect of high‐dose atropine in children with progressive myopia with and without a monogenetic cause. Children were matched for age and axial length (AL) in their first year of treatment.
Emilie van der Sande +11 more
wiley +1 more source
Synthesis of novel 2-(piperazino-1-yl-alkyl)-1H-benzimidazole derivates and assessment of their interactions with the D2 dopamine receptor [PDF]
A total of 14 novel arylpiperazines were synthesized, and pharmacologically evaluated by measuring their affinities towards the D2 dopamine receptor (DRD2) in a [3H]spiperone competition assay.
Penjišević Jelena Z. +5 more
doaj +1 more source
Dopaminergic regulation of inflammation and immunity in Parkinson's disease: friend or foe?
The present review aims to collect and critically summarise available evidence regarding the immune effects of dopamine and their mimics and to put dopaminergic agents used as antiparkinsonian drugs in the perspective of current knowledge about the involvement of immunity and inflammation in Parkinson's disease (PD).
Alessia Furgiuele +4 more
wiley +1 more source
Motions around conserved helical weak spots facilitate GPCR activation
Abstract G protein‐coupled receptors (GPCRs) participate in most physiological processes and are important drug targets in many therapeutic areas. Recently, many GPCR X‐ray structures became available, facilitating detailed studies of their sequence‐structure‐mobility‐function relations.
Janne M. Bibbe, Gert Vriend
wiley +1 more source

