Bacterial transcription as a target for antibacterial drug development

Cong Ma, Xiao Yang, Peter J. Lewis

Research output: Journal article publicationReview articleAcademic researchpeer-review

95 Citations (Scopus)


Transcription, the first step of gene expression, is carried out by the enzyme RNA polymerase (RNAP) and is regulated through interaction with a series of protein transcription factors. RNAP and its associated transcription factors are highly conserved across the bacterial domain and represent excellent targets for broadspectrum antibacterial agent discovery. Despite the numerous antibiotics on the market, there are only two series currently approved that target transcription. The determination of the three-dimensional structures of RNAP and transcription complexes at high resolution over the last 15 years has led to renewed interest in targeting this essential process for antibiotic development by utilizing rational structure-based approaches. In this review, we describe the inhibition of the bacterial transcription process with respect to structural studies of RNAP, highlight recent progress toward the discovery of novel transcription inhibitors, and suggest additional potential antibacterial targets for rational drug design.
Original languageEnglish
Pages (from-to)139-160
Number of pages22
JournalMicrobiology and Molecular Biology Reviews
Issue number1
Publication statusPublished - 1 Mar 2016
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Biology
  • General Immunology and Microbiology


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