Bioorganic & medicinal chemistry letters, 2017-06, Vol.27 (11), p.2465-2471
2017
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Details
- Autor(en) / Beteiligte
- Titel
- A calcineurin antifungal strategy with analogs of FK506
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2017-06, Vol.27 (11), p.2465-2471
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2017
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- [Display omitted] A novel antifungal strategy targeting the inhibition of calcineurin is described. To develop a calcineurin based inhibitor of pathogenic fungi, analogs of FK506 were synthesized that were able to permeate mammalian but not fungal cells. Antagonists in combination with FK506 were not immunosuppressive and retained antifungal activity in A. fumigatus. To reduce the dosage burden of the antagonist, murine oral PK was improved an order of magnitude relative to previous FK506 antagonists.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2017.04.004Titel-ID: cdi_proquest_miscellaneous_1888957281
- Format
- –
- Schlagworte
- Animals, Antifungal, Antifungal Agents - chemical synthesis, Antifungal Agents - pharmacokinetics, Antifungal Agents - pharmacology, Antifungal Agents - toxicity, Aspergillosis, Aspergillus fumigatus - drug effects, Calcineurin, Calcineurin Inhibitors - chemical synthesis, Calcineurin Inhibitors - pharmacokinetics, Calcineurin Inhibitors - pharmacology, Calcineurin Inhibitors - toxicity, Cercopithecus aethiops, FK506, FKBP12, Hep G2 Cells, Humans, Immunosuppressant, Interleukin-2 - metabolism, Jurkat Cells, Tacrolimus, Tacrolimus - analogs & derivatives, Tacrolimus - chemical synthesis, Tacrolimus - pharmacokinetics, Tacrolimus - pharmacology, Tacrolimus - toxicity, Tacrolimus Binding Protein 1A - chemistry, Vero Cells