Results 81 to 90 of about 23,799 (225)

Mitochondria‐Damaging Self‐Reporting Probe for Cancer Therapy

open access: yesAngewandte Chemie, Volume 138, Issue 32, 3 August 2026.
We developed a class of self‐reporting cationic chemotherapeutic probes that selectively induce mitochondrial damage and apoptosis in cancer cells. Their unique mitochondria‐to‐nucleus fluorescence migration enables real‐time visualization of the therapeutic process. ABSTRACT Mitochondrial damage induced by chemotherapeutic agents through disruption of
Hai Xu   +10 more
wiley   +2 more sources

Comprehensive in vitro profiling of traditional and emerging stimulants at monoamine transporters and the 5‐HT2A receptor

open access: yesBritish Journal of Pharmacology, EarlyView.
A pharmacological profiling of 58 synthetic stimulants of various classes at dopamine, norepinephrine, and serotonin transporters and the 5‐HT2A receptor, most showing distinct class‐dependent profiles, with some indicating a high abuse potential. Background and Purpose New psychoactive substances (NPSs) often emerge on the illicit drug market with ...
Darta Stalberga   +9 more
wiley   +1 more source

Chemoproteomic discovery of a brain‐penetrant, covalent NLRP3 inhibitor that binds a novel allosteric pocket

open access: yesBritish Journal of Pharmacology, EarlyView.
NLRP3 is a promising inflammatory target, but existing inhibitors lack diversity and brain penetrance, and none are approved. Using chemoproteomics, we discovered a novel series that binds to Cys463 in a previously uncharacterized pocket. Compounds showed nanomolar potency, brain exposure, and in vivo suppression of IL‐1β, supporting neuroinflammatory ...
Donald C. Rogness   +21 more
wiley   +1 more source

Deciphering Role of Endophytes in Plant Defences and Biotic Stress Resilience Across Families

open access: yesPlant, Cell &Environment, EarlyView.
ABSTRACT Plant families generate distinct repertoires of specialised metabolites that govern their biotic interactions. Endophytes strengthen host plant defence mechanisms and tolerance to biotic challenges by upregulating metabolite biosynthesis, modifying precursor compounds into more potent forms, or by directly synthesising analogous defence ...
S. Aneeqa Noor   +4 more
wiley   +1 more source

Saturating mutagenesis on the Ser118 residue responsible for the spectral tuning mechanism of the orange/green‐reversible cyanobacteriochrome AM1_1499g1

open access: yesPlant Biology, EarlyView.
This graphical abstract illustrates our systematic site‐saturation mutagenesis at the Ser118 position of the AM1_1499g1 GAF domain. By replacing this single residue, we generated a diverse array of variants with distinct spectral properties, demonstrating the remarkable molecular plasticity of cyanobacteriochromes and their customizability for ...
A. Yoneda, T. Suzuki, R. Narikawa
wiley   +1 more source

Metalloamination/Cyclization of Zinc(II) Amides Derived from N,N-Dimethylhydrazinoalkenes—Applications for the Direct C-SP2 Functionalization of Aryl and Vinyl Electrophiles

open access: yesInorganics
Treatment of N,N-dimethylhydrazinoalkenes with diethylzinc followed by exposure of the resulting ethylzinc amides to high vacuum drives a Schlenck redistribution metalloamination/cyclization to generate the corresponding bis(organozinc) intermediates in ...
Jérome Lépeule   +2 more
doaj   +1 more source

Transcriptional Regulation of HSP60, HSP70, and HSP90 in Response to Selenium Nanoparticles and Sodium Selenite in Periparturient Cloned Saanen Goats and Their Offspring

open access: yesVeterinary Medicine and Science, Volume 12, Issue 5, September 2026.
Selenium nanoparticles (SeNPs) outperform sodium selenite in raising serum selenium levels and suppressing HSP60, HSP70, and HSP90 transcription in periparturient goats and their offspring, indicating reduced cellular stress regardless of cloning status.
Gholam‐Ali Kojouri   +2 more
wiley   +1 more source

Effect of Intramolecular Hydrogen Bonds on the Binding Efficiency of Compounds Containing Aminoalcohol‐Based Subunits in Combination with Heterocyclic Groups

open access: yesEuropean Journal of Organic Chemistry, Volume 29, Issue 29, 7 August 2026.
This study broadens our understanding of the role of intramolecular interactions in molecular recognition and highlights the importance of considering their formation when designing artificial receptors, new drugs, and related systems. Aminoalcohols represent an important class of compounds and serve as building blocks for numerous biologically active ...
Manuel Stapf, Monika Mazik
wiley   +1 more source

Mapping Trofinetide Polypharmacology in Rett Syndrome: A Multi‐Stage Computational Analysis

open access: yesJournal of Computational Chemistry, Volume 47, Issue 21, August 5, 2026.
How can a single molecule address the complex symptoms of Rett syndrome? This computational study maps the multi‐target mechanism of trofinetide, revealing diverse modes of binding across five key receptors: GAT1, GABAA, CHRM1, AMPA, and GSK3β. From deep orthosteric anchoring to dynamic surface interactions, these structural insights provide a rational
Luis Felipe Hernández‐Ayala   +2 more
wiley   +1 more source

GK PUA Domain Modulates Cables, Cooperativity, and Proline Feedback

open access: yesAggregate, Volume 7, Issue 8, August 2026.
EcGK tetramers hierarchically assemble into metabolic filaments and bundle into metabolic cables. Upon substrate binding, this dynamic equilibrium shifts from inactive cables to active tetramers to drive catalysis; meanwhile the inhibitor proline stabilizes an X‐shaped conformation, redirecting assembly toward filaments to enable efficient feedback ...
Tianyi Zhang   +4 more
wiley   +1 more source

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