Structural mechanisms of QacR induction and multidrug recognition.
Publication
, Journal Article
Schumacher, MA; Miller, MC; Grkovic, S; Brown, MH; Skurray, RA; Brennan, RG
Published in: Science
December 7, 2001
The Staphylococcus aureus multidrug binding protein QacR represses transcription of the qacA multidrug transporter gene and is induced by structurally diverse cationic lipophilic drugs. Here, we report the crystal structures of six QacR-drug complexes. Compared to the DNA bound structure, drug binding elicits a coil-to-helix transition that causes induction and creates an expansive multidrug-binding pocket, containing four glutamates and multiple aromatic and polar residues. These structures indicate the presence of separate but linked drug-binding sites within a single protein. This multisite drug-binding mechanism is consonant with studies on multidrug resistance transporters.
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Published In
Science
DOI
ISSN
0036-8075
Publication Date
December 7, 2001
Volume
294
Issue
5549
Start / End Page
2158 / 2163
Location
United States
Related Subject Headings
- Staphylococcus aureus
- Rosaniline Dyes
- Rhodamines
- Repressor Proteins
- Protein Structure, Tertiary
- Protein Structure, Secondary
- Protein Conformation
- Molecular Structure
- Models, Molecular
- Hydrophobic and Hydrophilic Interactions
Citation
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MLA
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Schumacher, M. A., Miller, M. C., Grkovic, S., Brown, M. H., Skurray, R. A., & Brennan, R. G. (2001). Structural mechanisms of QacR induction and multidrug recognition. Science, 294(5549), 2158–2163. https://doi.org/10.1126/science.1066020
Schumacher, M. A., M. C. Miller, S. Grkovic, M. H. Brown, R. A. Skurray, and R. G. Brennan. “Structural mechanisms of QacR induction and multidrug recognition.” Science 294, no. 5549 (December 7, 2001): 2158–63. https://doi.org/10.1126/science.1066020.
Schumacher MA, Miller MC, Grkovic S, Brown MH, Skurray RA, Brennan RG. Structural mechanisms of QacR induction and multidrug recognition. Science. 2001 Dec 7;294(5549):2158–63.
Schumacher, M. A., et al. “Structural mechanisms of QacR induction and multidrug recognition.” Science, vol. 294, no. 5549, Dec. 2001, pp. 2158–63. Pubmed, doi:10.1126/science.1066020.
Schumacher MA, Miller MC, Grkovic S, Brown MH, Skurray RA, Brennan RG. Structural mechanisms of QacR induction and multidrug recognition. Science. 2001 Dec 7;294(5549):2158–2163.
Published In
Science
DOI
ISSN
0036-8075
Publication Date
December 7, 2001
Volume
294
Issue
5549
Start / End Page
2158 / 2163
Location
United States
Related Subject Headings
- Staphylococcus aureus
- Rosaniline Dyes
- Rhodamines
- Repressor Proteins
- Protein Structure, Tertiary
- Protein Structure, Secondary
- Protein Conformation
- Molecular Structure
- Models, Molecular
- Hydrophobic and Hydrophilic Interactions