Results 41 to 50 of about 488 (104)
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
Strategies for Target Identification and Mechanism Elucidation in Phytochemicals
Phytochemicals in Food and Medicine, Volume 1, Issue 3, September 2026.Strategies for Target Identification of Phytochemicals: Labeling Methods VS. Non‐Labeling Methods ABSTRACT Drug targets serve as the fundamental biological basis through which phytochemicals exert their therapeutic effects, and target discovery represents both the core challenge and the rate‐limiting step in elucidating the mechanisms of action of ...
Jialing Chen +4 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
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
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 to probe ligand-receptor and receptor-receptor interactions in living cells [PDF]
, 2019 This thesis describes a novel technique known as NanoBRET to monitor direct binding of a drug to its cognate receptor in living mice. It also describes the application of this technology to investigate interactions between two major transmembrane ...
Diana Carvalheira Alcobia (6427269) +1 more
core +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
ChemMedChem, Volume 21, Issue 10, 27 May 2026.We developed a targeted covalent inhibitor for the p300/CBP‐associated factor (PCAF) bromodomain. Our lead molecule, 10, labeled a unique lysine residue in the PCAF bromodomain, demonstrated potent inhibition in biophysical/biochemical assays, and engaged the PCAF bromodomain in cells.
Richard R. Ede +9 more
wiley +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