-Heterocyclic carbene (NHC) metal complexes are attracting scientists' interest as an alluring class of metallodrugs. Indeed, the versatile functionalization of NHC ligands makes them optimal scaffolds to be developed in medicinal chemistry. Besides, amino acids are great biological ligands for metals, such as silver and gold, even though their use is still under-investigated. Aiming to shed light on the anticancer properties of this kind of complex, we investigated a series of silver and gold complexes, stabilized by NHC ligands and bearing carboxylate salts of -butyloxycarbonyl (Boc)--protected glycine and l-phenylalanine as anionic ligands. The most active complexes, and , powerfully affect the growth of MDA-MB-231 breast cancer cells, with IC values in the low nanomolar range. Further studies demonstrated the blockade of the human topoisomerase I activity and actin polymerization reaction at 0.001 μM. These unique features make these complexes very interesting and worthy to be used for future studies.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10641922 | PMC |
http://dx.doi.org/10.1021/acsmedchemlett.3c00360 | DOI Listing |
J Phys Chem B
January 2025
Single Molecule Analysis Group, Department of Chemistry, The University of Michigan, Ann Arbor, Michigan 48109, United States.
Single-molecule fluorescence resonance energy transfer (smFRET) has emerged as a pivotal technique for probing biomolecular dynamics over time at nanometer scales. Quantitative analyses of smFRET time traces remain challenging due to confounding factors such as low signal-to-noise ratios, photophysical effects such as bleaching and blinking, and the complexity of modeling the underlying biomolecular states and kinetics. The dynamic distance information shaping the smFRET trace powerfully uncovers even transient conformational changes in single biomolecules both at or far from equilibrium, relying on trace idealization to identify specific interconverting states.
View Article and Find Full Text PDFFront Psychol
November 2024
Department of Neurosurgery, Massachusetts General Hospital and Harvard Medical School, Boston, MA, United States.
Introduction: The social characteristics of others can powerfully influence our decisions. They can also be broadly impacted by the social context in which these choices are made, making the effects of these characteristics on decision-making especially challenging to understand.
Methods: Here, we developed a Generative Narrative Survey that provided participants with naturalistic scenarios that richly varied in social context and theme but that also systematically varied the characteristics of the social agents involved, followed by a question.
J Physiol
January 2025
University of Exeter Medical School, Hatherly Labs, Exeter, Devon, UK.
The pituitary gland produces and secretes a variety of hormones that are essential to life, such as for the regulation of growth and development, metabolism, reproduction, and the stress response. This is achieved through an intricate signalling interplay between the brain and peripheral feedback signals that shape pituitary cell excitability by regulating the ion channel properties of these cells. In addition, endocrine anterior pituitary cells spontaneously fire action potentials to regulate the intracellular calcium ([Ca]) level, an essential signalling conduit for hormonal secretion.
View Article and Find Full Text PDFEnviron Res
January 2025
Sino-Dutch R&D Centre for Future Wastewater Treatment Technologies/Beijing Advanced Innovation Centre of Future Urban Design, Beijing University of Civil Engineering & Architecture, Beijing, 100044, China. Electronic address:
Climate change and carbon emissions are increasingly becoming a global concern, and thus wastewater treatment plants (WWTPs) are also receiving extensive attention due to direct greenhouse gas (GHG) emissions of methane (CH) and nitrous oxide (NO). Although there have been many emission factors (EFs) of CH and NO in literature, they are changeful due to different processes and boundaries, which limits their values for reference and comparison. With this study, in situ monitored CH and NO data reported in literature were retrieved for recalculating their EFs.
View Article and Find Full Text PDFSci Adv
September 2024
Department of Medicine and Moores Cancer Center, School of Medicine, University of California San Diego, San Diego, CA, USA.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!