Results 91 to 100 of about 11,582 (221)
Novel approaches for drug development against chronic primary pain: A systematic review
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus +5 more
wiley +1 more source
Covalent fluorescent probes for 2‐arachidonoylglycerol metabolic pathways
Abstract Covalent fluorescent probes have emerged as versatile chemical tools to visualise active enzymes in complex biological systems. When tailored for specific applications, ranging from activity‐based protein profiling for drug development to high spatiotemporal resolution imaging of enzymatic activities, these probes provide unique insights into ...
Nick D. F. Puijmbroeck +1 more
wiley +1 more source
DNA aptamers, Apt 60 and Apt 173, target the BamA protein to compromise outer membrane integrity in Pseudomonas aeruginosa, making it susceptible to Azithromycin, an antibiotic that is otherwise poorly effective due to the low‐permeability membrane.
Rupany Selvam +4 more
wiley +1 more source
Divergent roles of ent‐kaurene oxidase paralogs in rice momilactone biosynthesis
Rice contains a five‐gene tandem array of genes encoding members of the ent‐kaurene oxidase (KO) family, with OsKOL4 and OsKOL5 playing divergent roles in momilactone metabolism, but both acting in the production of antifungal and antibacterial phytoalexins, which are important for disease resistance.
Zhibiao Wang +8 more
wiley +1 more source
Iron oxide nanoparticles influence the growth, antioxidant capacity, and gene activity of Melissa officinalis subsp. officinalis plants in vitro, revealing their potential as modulators of secondary metabolism. Abstract Application of iron oxide nanoparticles (NP) (Fe3O4‐NPs) in plant biotechnology presents new opportunities for enhancing metabolic ...
E. Bektaş +5 more
wiley +1 more source
Unveiling the chemical and biological properties of Litsea cubeba essential oil. ABSTRACT Litsea cubeba essential oil (LCEO) is recognised for its broad spectrum of biological activities, including antimicrobial and insecticidal effects, making it a promising natural alternative to synthetic agents.
Miroslava Kačániová +10 more
wiley +1 more source
A cryptic allosteric pocket shapes isoform‐selective inhibition of human malic enzymes
Abstract Malic enzymes (ME) regulate central carbon metabolism and cellular redox balance, and the mitochondrial isoform ME2 is frequently upregulated in aggressive cancers to support metabolic flexibility and stress resistance. Isoform‐selective inhibition has remained out of reach because the catalytic machinery is essentially invariant across the ...
Ben A. Krinkel +14 more
wiley +1 more source
Four series of 20 (het)aryl substituted 7‐deazapurine nucleobases were synthesized. Several potent antagonists of all four subtypes of adenosine receptors were identified by functional assay. High‐throughput screening of the IMTM compound library for modulatory activity on adenosine receptors (ARs) identified two deazapurine hits based on 2,6‐diaryl‐7 ...
Ugnė Šinkevičiūtė +9 more
wiley +1 more source
Antimicrobial resistance highlights the urgent need for novel FabI inhibitors. Using an integrated computational approach combining ConPhar pharmacophore modeling, FTMap surface mapping, and PLIP interaction profiling across experimental structures and structures from MD simulations, we identified a conserved binding core (Y156/Y157, A95) and ...
Pedro Tenório T. F. Leite +10 more
wiley +1 more source
A structure‐informed, fragment‐based approach was used to identify non‐peptidomimetic inhibitors of plasmepsin V. Pyrrolidine, piperidine, and piperazine containing fragments showed activity in a FRET assay. The optimization of the pyrrolidine scaffold resulted in N‐sulfonamide analogs with potency up to ~10 µM, establishing a promising scaffold for ...
Marija Skvorcova +4 more
wiley +1 more source

