Results 41 to 50 of about 1,298 (145)
The Pharmacology of the SLC15A4‐TASL Complex, an Emerging Target for the Treatment of Lupus
Pharmacology Research &Perspectives, Volume 14, Issue 4, August 2026.ABSTRACT SLC15A4 is a member of the solute carrier superfamily that has been strongly linked to the pathogenesis of the auto‐immune disease SLE. The endo‐lysosomally localized SLC15A4 has traditionally been considered a proton‐dependent histidine and peptide transporter, but has also been shown to facilitate TLR7, 8, and 9 induced IFN‐alpha signaling ...
Alex L. Wilkinson +5 more
wiley +1 more source
Molecules, 2020 In recent years, new drug discovery approaches based on novel pharmacological concepts have emerged. Allosteric modulators, for example, target receptors at sites other than the orthosteric binding sites and can modulate agonist-mediated activation ...
Víctor Fernández-Dueñas +6 more
doaj +1 more source
Integrative Insights Into DYRK1A From Molecular Function to Therapeutic Advancement
Chemical Biology &Drug Design, Volume 108, Issue 1, July 2026.At the center the 3D structure of DYRK1A has been displayed. The dual‐function of DYRK1A involved in cancer and neurodegeneration, i.e., its overexpression drives Down syndrome, neurodegenerative disease etc., and underexpression causes intellectual disability, seizures, etc.
Sampriti Paul +2 more
wiley +1 more source
NanoBRET binding assay for histamine H2 receptor ligands using live recombinant HEK293T cells [PDF]
Scientific Reports, 2020 AbstractFluorescence/luminescence-based techniques play an increasingly important role in the development of test systems for the characterization of future drug candidates, especially in terms of receptor binding in the field of G protein-coupled receptors (GPCRs).
Lukas Grätz +5 more
openaire +3 more sources
The FASEB Journal, Volume 40, Issue 11, 15 June 2026.Bitter taste receptors (T2Rs) play an important role in physiological and cellular responses. Bitter tasting chemicals and microbial metabolites can bind to T2R14, which enables interactions between T2R14 and specific intracellular domains of the cystic fibrosis transmembrane conductance regulator (CFTR) anion channel.
Tejas Gupte +8 more
wiley +1 more source
From Pharmacophore to Warhead: NAD+‐Targeting Triazoles as Mechanism‐Based Sirtuin Inhibitors
Angewandte Chemie, Volume 137, Issue 52, December 22, 2025.We report “Sirtuin Trapping Ligands” (SirTraps), mechanism‐based 1,2,3‐triazole inhibitors that hijack sirtuin (SIRT) catalysis to form covalent triazolium– or triazole–ADP‐ribose (ADPR) adducts from NAD+. These trapped intermediates stall the enzyme in an inactive state, providing a biocompatible alternative to thiocarbonyl inhibitors and a blueprint ...
Florian Friedrich +16 more
wiley +2 more sources
Advanced Science, Volume 13, Issue 23, 23 April 2026.Hybrid FRET–BRET biosensors were developed to monitor RAF–KRAS interactions in living cells. These sensors enable real‐time visualization of interaction dynamics, quantitative spectral analysis, and validation of mutation‐selective inhibitors, providing a versatile platform for probing KRAS regulation and therapeutic responses. ABSTRACT The RAS–RAF–MEK–
Jeong‐Min Go +12 more
wiley +1 more source
ChemistryOpen, Volume 15, Issue 4, April 2026.Targeting a nucleotide‐sensitive groove on Hsp70 that binds the Bim BH3 helix, we integrate structures, biophysics, and SAR from peptides, fragments, and phenalene‐dicarbonitrile “wedges.” These disrupt the Hsp70–Bim complex with sub‐µM cellular engagement and in vivo activity while sparing Hsp90/mortalin.
Emadeldin M. Kamel +5 more
wiley +1 more source
A Setmelanotide-like Effect at MC4R Is Achieved by MC4R Dimer Separation
Biomolecules, 2022 Melanocortin 4 receptor (MC4R) is part of the leptin-melanocortin pathway and plays an essential role in mediating energy homeostasis. Mutations in the MC4R are the most frequent monogenic cause for obesity.
Nanina Reininghaus +7 more
doaj +1 more source
The GPCR Connection: Linking Alzheimer's Disease and Glioblastoma
Journal of Cellular and Molecular Medicine, Volume 30, Issue 7, April 2026.ABSTRACT Alzheimer's disease (AD) and glioblastoma multiforme (GBM) are biologically distinct age‐related brain disorders with opposing clinical phenotypes. AD is characterised by progressive neurodegeneration and cognitive decline, whereas GBM is characterised by aggressive cellular proliferation and a poor prognosis.
Ana B. Caniceiro +4 more
wiley +1 more source