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Front Microbiol. 2018 Aug 20;9:1942. doi: 10.3389/fmicb.2018.01942. eCollection 2018.

Look and Outlook on Enzyme-Mediated Macrolide Resistance.

Frontiers in microbiology

Tolou Golkar, Michał Zieliński, Albert M Berghuis

Affiliations

  1. Department of Biochemistry, McGill University, Montreal, QC, Canada.
  2. Department of Microbiology & Immunology, McGill University, Montreal, QC, Canada.

PMID: 30177927 PMCID: PMC6109786 DOI: 10.3389/fmicb.2018.01942

Abstract

Since their discovery in the early 1950s, macrolide antibiotics have been used in both agriculture and medicine. Specifically, macrolides such as erythromycin and azithromycin have found use as substitutes for β-lactam antibiotics in patients with penicillin allergies. Given the extensive use of this class of antibiotics it is no surprise that resistance has spread among pathogenic bacteria. In these bacteria different mechanisms of resistance have been observed. Frequently observed are alterations in the target of macrolides, i.e., the ribosome, as well as upregulation of efflux pumps. However, drug modification is also increasingly observed. Two classes of enzymes have been implicated in macrolide detoxification: macrolide phosphotransferases and macrolide esterases. In this review, we present a comprehensive overview on what is known about macrolide resistance with an emphasis on the macrolide phosphotransferase and esterase enzymes. Furthermore, we explore how this information can assist in addressing resistance to macrolide antibiotics.

Keywords: Ere; MPH; antibiotic resistance mechanisms; erythromycin esterase; ketolides; macrolide phosphotransferase; macrolide resistance; macrolides

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