Echinocandins: Production and applications

Tamás Emri, László Majoros, Viktória Tóth, István Pócsi

Research output: Contribution to journalReview article

50 Citations (Scopus)

Abstract

The first echinocandin-type antimycotic (echinocandin B) was discovered in the 1970s. It was followed by the isolation of more than 20 natural echinocandins. These cyclic lipo-hexapeptides are biosynthesized on non-ribosomal peptide synthase complexes by different ascomycota fungi. They have a unique mechanism of action; as non-competitive inhibitors of β-1,3-glucan synthase complex they target the fungal cell wall. Results of the structure-activity relationship experiments let us develop semisynthetic derivatives with improved properties. Three cyclic lipohiexapeptides (caspofungin, micafungin and anidulafungin) are currently approved for use in clinics. As they show good fungicidal (Candida spp.) or fungistatic (Aspergillus spp.) activity against the most important human pathogenic fungi including azole-resistant strains, they are an important addition to the antifungal armamentarium. Some evidence of acquired resistance against echinocandins has been detected among Candida glabrata strains in recent years, which enhanced the importance of data collected on the mechanism of acquired resistance developing against the echinocandins. In this review, we show the structural diversity of natural echinocandins, and we summarize the emerging data on their mode of action, biosynthesis and industrial production. Their clinical significance as well as the mechanism of natural and acquired resistance is also discussed.

Original languageEnglish
Pages (from-to)3267-3284
Number of pages18
JournalApplied Microbiology and Biotechnology
Volume97
Issue number8
DOIs
Publication statusPublished - Apr 1 2013

Keywords

  • Echinocandin resistance
  • Natural echinocandins
  • Non-ribosomal peptide synthase
  • Paradoxical growth
  • Semisynthetic echinocandins
  • β-1,3-Glucan synthase

ASJC Scopus subject areas

  • Biotechnology
  • Applied Microbiology and Biotechnology

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