Ribosome-Targeting Antibiotics: Modes of Action, Mechanisms of Resistance, and Implications for Drug Design

Jinzhong Lin, Dejian Zhou, Thomas A. Steitz, Yury S. Polikanov, Matthieu G. Gagnon

Research output: Contribution to journalReview articlepeer-review

54 Scopus citations


Genetic information is translated into proteins by the ribosome. Structural studies of the ribosome and of its complexes with factors and inhibitors have provided invaluable information on the mechanism of protein synthesis. Ribosome inhibitors are among the most successful antimicrobial drugs and constitute more than half of all medicines used to treat infections. However, bacterial infections are becoming increasingly difficult to treat because the microbes have developed resistance to the most effective antibiotics, creating a major public health care threat. This has spurred a renewed interest in structure-function studies of protein synthesis inhibitors, and in few cases, compounds have been developed into potent therapeutic agents against drug-resistant pathogens. In this review, we describe the modes of action of many ribosome-targeting antibiotics, highlight the major resistance mechanisms developed by pathogenic bacteria, and discuss recent advances in structure-assisted design of new molecules.

Original languageEnglish (US)
Pages (from-to)451-478
Number of pages28
JournalAnnual Review of Biochemistry
StatePublished - Jun 20 2018


  • antibiotic resistance
  • antibiotics
  • drug design
  • mechanisms of inhibition
  • protein synthesis
  • ribosome

ASJC Scopus subject areas

  • Biochemistry


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