Tetracyclines have been foundational antibacterial agents for more than 70 years. Renewed interest in tetracycline antibiotics is being driven by advancements in tetracycline synthesis and strategic scaffold modifications designed to overcome established clinical resistance mechanisms including efflux and ribosome protection. Emerging new resistance mechanisms, including enzymatic antibiotic inactivation, threaten recent progress on bringing these next-generation tetracyclines to the clinic. Here we review the current state of knowledge on the structure, mechanism, and inhibition of tetracycline-inactivating enzymes.

Original languageEnglish
Article number1058
JournalFrontiers in Microbiology
Issue numberMAY
StatePublished - May 30 2018


  • Antibiotic adjuvants
  • Antibiotic resistance
  • Enzymatic antibiotic inactivation
  • Flavin monooxygenase
  • Tetracycline destructases
  • Tetracyclines


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