Results 11 to 20 of about 2,118 (153)
Structure of the dopamine D2 receptor in complex with the antipsychotic drug spiperone [PDF]
Nature Communications, 2020 The dopamine D2 receptor (D2R) is a GPCR and an important drug target for schizophrenia treatment. Here, the authors present the crystal structure of human D2R in complex with the antipsychotic drug spiperone, which is of interest for designing ...
Dohyun Im +18 more
doaj +3 more sources
From Single-Cell Clusters to Causality: ITCH Engagement for CKD Uncovered by Integrative Analysis of MR and MAGMA. [PDF]
FASEB JThis graphical abstract illustrates an integrative analysis of single‐cell RNA‐seq data in CKD. DEGs were subsequently identified as candidate genes via Mendelian randomization analysis and combined with MAGMA analysis, ITCH was identified as a key gene.
Zhang X +7 more
europepmc +2 more sources
Genome-Wide Meta-Analysis of Parkinson's Disease Associated Genetic Loci and Validation of Therapeutic Targets. [PDF]
Brain BehavThis study identified genetic loci associated with Parkinson's disease through a genome‐wide meta‐analysis, screened druggable genes significantly linked to PD risk, and assessed the potential of GCLC and GFPT1 as therapeutic targets. ABSTRACT Background To identify genetic loci associated with Parkinson's disease (PD) through a genome‐wide meta ...
Yang S, Wu Q, Yang X.
europepmc +2 more sources
Drug Repurposing Screen Identifies Pimozide as a ROS-Inducing Therapy With Anti-Tumor Efficacy in HNSCC PDX Models. [PDF]
Cancer SciA drug repurposing screen for reactive oxygen species (ROS)‐inducing compounds identified Pimozide as a potent anti‐tumor agent in head and neck squamous cell carcinoma (HNSCC) patient‐derived xenograft (PDX) models. Combined treatment with paclitaxel markedly reduced undifferentiated tumor cells.
Okazaki S +12 more
europepmc +2 more sources
Micellar Hyaluronidase and Spiperone as a Potential Treatment for Pulmonary Fibrosis. [PDF]
Int J Mol Sci, 2021 Concentration of hyaluronic acid (HA) in the lungs increases in idiopathic pulmonary fibrosis (IPF). HA is involved in the organization of fibrin, fibronectin, and collagen. HA has been proposed to be a biomarker of fibrosis and a potential target for antifibrotic therapy.
Skurikhin E +10 more
europepmc +5 more sources
Spiperone: evidence for uptake into secretory granules. [PDF]
Proceedings of the National Academy of Sciences, 1984 Spiperone, a dopamine antagonist widely used as a specific ligand for dopamine and serotonin receptors, is actively accumulated into the F4C1 strain of rat pituitary tumor cells. The accumulation of 10 nM [3H]spiperone was linear for 3 min and reached a steady state after 10 min.
P S, Dannies +3 more
openaire +2 more sources
The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors
British Journal of Pharmacology, Volume 180, Issue S2, Page S23-S144, October 2023., 2023 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
British Journal of Pharmacology, Volume 180, Issue 16, Page 2039-2063, August 2023., 2023 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
Analytical Science Advances, Volume 4, Issue 3-4, Page 104-131, May 2023., 2023 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
Ophthalmic and Physiological Optics, Volume 43, Issue 3, Page 494-504, May 2023., 2023 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