Promises of anionic calix[n]arenes in life science: State of the art in 2023

Lazar, Adina-N.; Perret, Florent; Perez-Lloret, Marta; Michaud, Mickael; Coleman, Anthony W.

doi:10.1016/j.ejmech.2023.115994

European Journal of Medicinal Chemistry

2024

DOI: 10.1016/j.ejmech.2023.115994

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Promises of anionic calix[n]arenes in life science: State of the art in 2023

Adina-N. Lazar,

Florent Perret,

Marta Perez-Lloret

et al.

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Cited by 5 publications

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Anionic Calixarenes in Biomembrane Transport of Peptides

Neumann,

Hennig

2024

Israel Journal of Chemistry

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Biomembranes function as hydrophobic barriers for hydrophilic substances enabling compartmentalization in biological systems. This poses, however, a problem for the targeted introduction of cargo into cells. The result is a high demand for delivery pathways into cells with the goal to investigate biological processes or to treat diseases by improved delivery. Polycationic cell‐penetrating peptides (CPPs) are interesting as they can cross cell membranes and transport attached cargos directly into the cytosol. Their efficiency can be improved by anionic amphiphilic counterion activators, which bind to the CPPs to form charge‐neutralized counterion‐CPP complexes with sufficient hydrophobicity to cross the lipid bilayer membrane. This review summarizes recent results, which establish amphiphilic calixarenes as a new class of biocompatible and non‐cytotoxic counterion activators with very high transport activities at nanomolar concentrations. We also include a brief summary of fluorescence‐based assays with large unilamellar vesicles (LUVs) to investigate counterion‐activated transport. Current methods use liposome‐encapsulated, supramolecular host‐dye reporter pairs including calixarenes, which provide new mechanistic insights and enable rapid in vitro identification of suitable activators. Taken together, amphiphilic calixarenes are currently emerging as prime candidates for counterion activation of membrane transport, which are highly modifiable and can be specifically tailored towards different cargoes and membrane types.

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Anionic Calixarenes in Biomembrane Transport of Peptides

Neumann,

Hennig

2024

Israel Journal of Chemistry

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Utilizing the metal coordination and supramolecular chemistry of macrocycles to tackle medicinal issues

Redshaw

2025

Coordination Chemistry Reviews

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Supramolecular engineering of micellar systems: Precision control on self-assembly, polarity, and charge for enhanced nanocarrier design

Gómez-González,

Basílio,

Vaz

et al. 2024

Journal of Molecular Liquids

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Promises of anionic calix[n]arenes in life science: State of the art in 2023

Cited by 5 publications

References 124 publications

Anionic Calixarenes in Biomembrane Transport of Peptides

Anionic Calixarenes in Biomembrane Transport of Peptides

Utilizing the metal coordination and supramolecular chemistry of macrocycles to tackle medicinal issues

Supramolecular engineering of micellar systems: Precision control on self-assembly, polarity, and charge for enhanced nanocarrier design

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