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Sancho-Vaello, E.

Publications and source records attributed to Sancho-Vaello, E..

2 recordsLinked to original sources

Seven amino acids gate transcriptional activation by a minimal MarA Helix turn-helix DNA-binding domain

Prokaryotic transcription factors (TFs) lie at the core of antimicrobial resistance, controlling genes that let bacteria survive antibiotic exposure. The AraC/XylS family of TFs is defined by a ~99-residue DNA-binding domain composed of two helix-turn-helix (HTH) motifs. While this two-motif architecture is considered the minimal functional unit, the striking sequence and structural similarity between both HTH motifs raises the question of whether it evolved from a single ancestral HTH domain. Here, we designed two C-terminal truncations of MarA, comprising a single HTH motif, differing by seven-residues (IRSRKMT). Electrophoretic-mobility shift assays reveal that both constructs specifically bind the marbox sequence as reconstituted dimers, while size-exclusion chromatography shows they exist in a monomer-dimer equilibrium in solution. Despite retaining DNA-binding capacity, the truncations diverge functionally: while MarA64 (including IRSRKMT) activates transcription and confers regular erythromycin tolerance, MarA57 (lacking IRSRKMT) yields a transcriptionally inactive complex that suppresses reporter expression below baseline, suggesting competitive promoter occupancy. Molecular dynamics simulations and AlphaFold models suggest that the IRSRKMT extension forms an -helical element stabilizing a transcriptionally productive dimer interface. Conversely, its loss disrupts quaternary assembly, alters DNA bending, and misaligns RNA polymerase-contacting residues. Furthermore, free dimers explore non-productive conformations, suggesting that functional dimerization occurs upon DNA engagement. These findings establish that a single, correctly dimerized HTH domain is sufficient for both DNA binding and transcriptional activation, providing a structural rationale for short AraC/XylS-like proteins and offering a tuneable scaffold for synthetic biology and novel anti-virulence strategies.

molecular biology↗

The N-terminal helix of MarA as a key element in the mechanism of DNA binding

Efflux is one of the mechanisms employed by Gram-negative bacteria to become resistant to routinely used antibiotics. The inhibition of efflux by targeting their regulators is a promising strategy to re-sensitise bacterial pathogens to antibiotics. AcrAB-TolC is the main Resistance-Nodulation-Division efflux pump in Enterobacteriaceae. MarA is an AraC/XylS family global regulator that regulates more than 40 genes related to the antimicrobial resistance phenotype, including acrAB. The aim of this work was to understand the role of the N-terminal helix of MarA in the mechanism of DNA binding. An N-terminal deletion of MarA showed that the N-terminal helix has a role in the recognition of the functional marboxes. By engineering two double cysteine variants of MarA, and combining in vitro electrophoretic mobility assays and in vivo measurements of acrAB transcription with molecular dynamic simulations, it was shown that the immobilization of the N-terminal helix of MarA prevents binding to DNA. This new mechanism of inhibition seems to be universal for the monomeric members of the AraC/XylS family, as suggested by additional molecular dynamics simulations of the two-domain protein Rob. These results point to the N-terminal helix of the AraC/XylS family monomeric regulators as a promising target for the development of inhibitors.

molecular biology↗