ArticleInorganic chemistry2023
Conformationally Preorganized High-Affinity Ligands for Copper Biology with Hinged and Rigid Thiophene Backbones.
Article in Inorganic chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed, 4 citations in OpenAlex.
- Site-Specific Labeling of PD-L1 Fab through Disulfide Rebridging for ImmunoPET Imaging.Chemical & biomedical imaging · 2026Article
- TPEN, a Well-Known Zinc Chelator, Sequesters Attomolar-Buffered Cellular Cu(I) Through an Oxygen-Dependent Mechanism.ACS chemical neuroscience · 2026Article
- Selective removal of copper from complex biological media with an agarose-immobilized high-affinity PSP ligand.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2024Article
- Small-Molecule Fluorescent Probes for Binding- and Activity-Based Sensing of Redox-Active Biological Metals.Chemical reviews · 2024Review
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Copper-selective ligands are essential tools for probing the affinity of cuproproteins or manipulating the cellular copper availability. They also harbor significant potential as antiangiogenic agents in cancer therapy or as therapeutics to combat copper toxicity in Wilson's disease. To achieve the high Cu(I) affinities required for competing effectively with cellular cuproproteins, we recently devised a ligand design based on phosphine-sulfide-stabilized phosphine (PSP) donor motifs. Building on this design strategy, we integrated two PSP donors within preorganized ligand architectures composed of either a hinged bithiophene backbone (bithipPS) or a single rigid thiophene bridge (thipPS). Extensive characterization based on X-ray crystal structures, solution NMR data, spectrophotometric titrations, and electrochemical studies established that bithipPS adapts well to the coordination preferences of Cu(I) to form a discrete air-stable mononuclear Cu(I) complex with a dissociation constant of 4 zM. In contrast, the wider bite angle of thipPS introduces some strain upon Cu(I) coordination to yield an almost 10-fold lower affinity with a
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