Results 31 to 40 of about 1,238 (123)
SLAS DiscoveryTargeting transforming growth factor-β (TGF-β) receptors is a promising pharmacological approach to normalize aberrant signaling in genetic and non-genetic TGF-β associated diseases including fibrosis, cancer, cardiovascular and musculoskeletal disorders.
Marius Wits +3 more
doaj +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
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
Visualizing Ligand Binding to a GPCR In Vivo Using NanoBRET
iScience, 2018 Summary: The therapeutic action of a drug depends on its ability to engage with its molecular target in vivo. However, current drug discovery strategies quantify drug levels within organs rather than determining the binding of drugs directly to their ...
Diana C. Alcobia +9 more
doaj +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
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
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
Pharmaceuticals, 2023 The concept of photocaging represents a promising approach to acquire spatiotemporal control over molecular bioactivity. To apply this strategy to pyridinylimidazole-based covalent JNK3 inhibitors, we used acrylamido-N-(4-((4-(4-(4-fluorophenyl)-1-methyl-
Beate Sandra Hoffelner +3 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