2. Academic Validation
  3. A calcineurin antifungal strategy with analogs of FK506

A calcineurin antifungal strategy with analogs of FK506

  • Bioorg Med Chem Lett. 2017 Jun 1;27(11):2465-2471. doi: 10.1016/j.bmcl.2017.04.004.
Mitchell Nambu 1,  Jonathan A Covel 2,  Mili Kapoor 2,  Xiaoming Li 2,  Molly K Moloney 2,  Mehdi M Numa 2,  Quinlyn A Soltow 2,  Michael Trzoss 2,  Peter Webb 2,  Robert R Webb 2nd 2,  Mitchell Mutz 3
Affiliations

Affiliations

  • 1 Amplyx Pharmaceuticals, 3210 Merryfield Row, San Diego, CA 92121, United States. Electronic address: mitch.nambu@yahoo.com.
  • 2 Amplyx Pharmaceuticals, 3210 Merryfield Row, San Diego, CA 92121, United States.
  • 3 Amplyx Pharmaceuticals, 3210 Merryfield Row, San Diego, CA 92121, United States. Electronic address: mutz.mitchell@gene.com.
PMID: 28412204 DOI: 10.1016/j.bmcl.2017.04.004
Abstract

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.

Keywords

Antifungal; Aspergillosis; Calcineurin; FK506; FKBP12; Immunosuppressant; Tacrolimus.

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