Antibiotic binding releases autoinhibition of the TipA multidrug-resistance transcriptional regulator.

ABSTRACT: Investigations of bacterial resistance strategies can aid in the development of new antimicrobial drugs as a countermeasure to the increasing worldwide prevalence of bacterial antibiotic resistance. One such strategy involves the TipA class of transcription factors, which constitute minimal autoregulated multidrug resistance (MDR) systems against diverse antibiotics. However, we have insufficient information regarding how antibiotic binding induces transcriptional activation to design molecules that could interfere with this process. To learn more, we determined the crystal structure of SkgA from Caulobacter crescentus as a representative TipA protein. We identified an unexpected spatial orientation and location of the antibiotic-binding TipAS effector domain in the apo state. We observed

SUBMITTER: Jiang X 

PROVIDER: S-EPMC7762955 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature