Results 141 to 150 of about 14,379 (215)

Dosing PPARγ Activation With Light Using Fast Relaxing Photoswitches

Angewandte Chemie International Edition, Volume 65, Issue 40, 28 September 2026.
To achieve spatiotemporal control over PPARγ activity, we designed the fast‐relaxing photoswitchable agonist 6 that selectively activates PPARγ in its light‐induced Z‐state and relaxes within seconds (t1/2 47 s) to the inactive E‐state. This unique profile allowed light‐dosed receptor activation in in vitro settings, enabling biological studies on ...
Loris Knümann, Alba Rodriguez‐Paniagua, Martin Reynders, Silke Duensing‐Kropp, Oliver Thorn‐Seshold, Vasily Morozov, Julian A. Marschner, Daniel Merk   +7 more
wiley   +1 more source

A Comprehensive 19F NMR Framework for Fragment‐Based Drug Discovery: The Validated Screening Library OpenFL600 and Efficient Affinity Ranking by CSAR

Angewandte Chemie, Volume 138, Issue 39, 21 September 2026.
NMR screening is a powerful method for hit detection in drug‐discovery. We designed and validated the OpenFL600 19F$^{19}{\rm F}$ NMR library to probe diverse targets, including RNA, GPCRs, kinases, and proteases. This library yields target‐specific ligands without generating promiscuous binders.
Simon H. Rüdisser, Gabriela Stadler, Giacomo Padroni, Daria Barbash, Marco M. Ruckstuhl, Nils Lorz, Christina Jordan, Sarah Skibinski, Timo T. Stühlinger, Sarah E. Kratzwald, Katharina M. Siess, Sven Brüschweiler, Gerald Platzer, Antoine Cléry, Robert Konrat, Frédéric H.‐.T. Allain, Alvar D. Gossert   +16 more
wiley   +2 more sources

Artificial Intelligence and Virtual Screening to Identify Small Molecules Inhibiting Transglutaminase 2 for Investigation and Treatment of Breast Cancer

ChemBioChem, Volume 27, Issue 18, 28 September 2026.
Artificial Intelligence (AI)‐guided screening of nearly 10 million molecules hit the bull’s‐eye: G11, a new nonpeptidic inhibitor of transglutaminase 2. A stepwise path from in silico ranking to cell and biochemical assays identified G11 as the top hit. It induced apoptosis in transglutaminase 2 (TG2)‐rich breast cancer cells and inhibited purified TG2,
Carlo M. Bergamini, Niel M. Henriksen, Brianna Ryan, Taylor A. Prince, Anna Terrazzan, Pietro Ancona, Cristina Zuccato, Gianluca Aguiari, Valentina Rosta, Jeffrey W. Keillor, Alessandro Trentini, Nicoletta Bianchi   +11 more
wiley   +1 more source

Mechanistic Perspectives From Genomics and Pangenomics of Medicinal and Aromatic Plants: Linking Genome Architecture to Phytochemical Diversity. [PDF]

Int J Genomics
Saini H, Yadav J, Johar V, Vyas S, Jaryan V, Kumar A, Nanda D, Kumar A, Kaushik JJ, Shamkuwar S, Singh S.   +10 more
europepmc   +1 more source

Design, Synthesis, and Biological Evaluation of Pyrazolyl Thioureas (PTUs) as SIRT1 and SIRT2 Inhibitors

ChemMedChem, Volume 21, Issue 18, 28 September 2026.
Pyrazolyl thioureas were designed and synthesized as sirtuin 1 (SIRT1) and sirtuin 2 (SIRT2) inhibitors. 6a (IC50 (SIRT1) = 5.3 µM; IC50 (SIRT2) = 2.2 µM) and 7f (IC50 (SIRT1) = 12.4 µM; IC50 (SIRT2) = 13.6 µM) showed micromolar inhibition on target enzymes and HepG2‐based assays confirmed a SIRT2‐mediated effect on tubulin acetylation. Docking studies
Matteo Lusardi, Cecilia Astigiano, Deianira Bellitto, Matteo Raineri, Giorgia Guccione, Annalisa Salis, Elena Cichero, Chiara Brullo, Marco Ponassi, Santina Bruzzone, Andrea Spallarossa   +10 more
wiley   +1 more source

Strain-resolved metabolomic chemotyping identifies tryptophan and γ-glutamyl peptides as MGO-AGEs breaking postbiotic compounds for carbonyl stress mitigation. [PDF]

Gut Microbes
Kim SH, Hong SM, Lee EY, Kim SA, Han NS, Kim SY, Lee CH.   +6 more
europepmc   +1 more source

Beyond the Active Site: First‐In‐Class Leishmania Infantum Trypanothione Reductase Dimerization Disruptors as Antileishmanial Leads

ChemMedChem, Volume 21, Issue 18, 28 September 2026.
This review outlines a pioneering strategy to inhibit Leishmania infantum trypanothione reductase by disrupting its dimer interface. From peptides to small‐molecule proteomimetics, multiple chemotypes achieved potent enzymatic inhibition and notable cellular antileishmanial activity, highlighting a new therapeutic paradigm.
María‐José Camarasa, Miguel Maldonado, Alvaro de la Cruz‐Potenciano, Sonia de Castro   +3 more
wiley   +1 more source

Essential Oil Quality in Medicinal and Aromatic Plants: Linking Plant Biosynthesis, Matrix Selection and Extraction Strategy. [PDF]

Plants (Basel)
Youchret-Zallez OB, Spigarelli R, Kouki A, Mbirki L, Ben-Attia M, Bernacchi A, Valerii MC, Spisni E.   +7 more
europepmc   +1 more source

π‐Extended Silyl Enolates as Emerging Platforms in Radical Chemistry

European Journal of Organic Chemistry, Volume 29, Issue 36, 24 September 2026.
This review covers the emerging role of π‐extended silyl polyenol ethers in radical chemistry. It highlights their versatile roles as electron‐rich SOMOphiles, silyl radical cation precursors, and nucleophilic partners in radical–polar crossover manifolds, while considering recent advances in photoredox catalysis, electrochemistry, and transition metal‐
Debora Guazzetti, Kelly Bugatti, Claudio Curti, Franca Zanardi   +3 more
wiley   +1 more source

Revisiting the PCR-Based Molecular Approaches for Mycotoxigenic Fusarium Species Detection and Quantification in Wheat. [PDF]

Compr Rev Food Sci Food Saf
Vijeandran K, Larionov A, Cervini C, Campbell K, Walkowiak S, Pasquali M, Richard-Forget F, Brown N, Rose LJ, Verheecke-Vaessen C.   +9 more
europepmc   +1 more source