Structure-Guided Synthesis of FK506 and FK520 Analogs with Increased Selectivity Exhibit In Vivo Therapeutic Efficacy against Cryptococcus

Structure-Guided Synthesis of FK506 and FK520 Analogs with Increased Selectivity Exhibit In Vivo Therapeutic Efficacy against Cryptococcus

ABSTRACT Calcineurin is an essential virulence factor that is conserved across human fungal pathogens, including Cryptococcus neoformans, Aspergillus fumigatus, and Candida albicans. Although an excellent target for antifungal drug development, the serine-threonine phosphatase activity of calcineuri...

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Bibliographic Details
Main Authors: Michael J. Hoy, Eunchong Park, Hyunji Lee, Won Young Lim, D. Christopher Cole, Nicholas D. DeBouver, Benjamin G. Bobay, Phillip G. Pierce, David Fox, Maria Ciofani, Praveen R. Juvvadi, William Steinbach, Jiyong Hong, Joseph Heitman
Format: Article
Language:English
Published: American Society for Microbiology 2022-06-01
Series:mBio
Subjects:
X-ray crystallography
antifungal
antifungal resistance
antifungal susceptibility testing
ascomycin
calcineurin
Online Access:https://journals.asm.org/doi/10.1128/mbio.01049-22

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