Recent Advance in Small Molecules Targeting RhlR of Pseudomonas aeruginosa

Taehyeong Lim, So Young Ham, Sangjin Nam, Myoungsun Kim, Ki Yong Lee, Hee Deung Park, Youngjoo Byun

Research output: Contribution to journalReview articlepeer-review

8 Citations (Scopus)


Pseudomonas aeruginosa (P. aeruginosa) is an opportunistic gram-negative pathogen that can cause various infections, particularly in patients with compromised host defenses. P. aeruginosa forms biofilms and produces virulence factors through quorum sensing (QS) network, resulting in resistance to antibiotics. RhlI/RhlR, one of key QS systems in P. aeruginosa, is considered an attractive target for inhibiting biofilm formation and attenuating virulence factors. Several recent studies examined small molecules targeting the RhlI/RhlR system and their in vitro and in vivo biological activities. In this review, RhlR-targeted modulators, including agonists and antagonists, are discussed with particular focus on structure-activity relationship studies and outlook for next-generation anti-biofilm agents.

Original languageEnglish
Article number274
Issue number2
Publication statusPublished - 2022 Feb

Bibliographical note

Funding Information:
Funding: This research was funded by the National Research Foundation of Korea (2019R1A6A1A03031807).

Publisher Copyright:
© 2022 by the authors. Licensee MDPI, Basel, Switzerland.


  • Biofilm
  • Pseudomonas aeruginosa
  • RhlR

ASJC Scopus subject areas

  • Microbiology
  • Biochemistry
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Microbiology (medical)
  • Infectious Diseases
  • Pharmacology (medical)


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