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Cyclosporins are natural or synthetic undecapeptides with a wide range of actual and potential pharmaceutical applications. Several members of the cyclosporin compound family have remarkably high passive membrane permeabilities that are not well-described by simple structural metrics. Here we review experimental studies of cyclosporin structure and permeability, including cyclosporin-metal complexes. We also discuss models for the conformation-dependent permeability of cyclosporins and similar compounds. Finally, we identify current knowledge gaps in the literature and provide recommendations regarding future avenues of exploration.


Karen M Corbett, Leigh Ford, Dallas B Warren, Colin W Pouton, David K Chalmers. Cyclosporin Structure and Permeability: From A to Z and Beyond. Journal of medicinal chemistry. 2021 Sep 23;64(18):13131-13151

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PMID: 34478303

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