Skip to main content
construction release_alert
Scholars@Duke will be undergoing maintenance April 11-15. Some features may be unavailable during this time.
cancel
Journal cover image

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.

Duke Scholars

Altmetric Attention Stats
Dimensions Citation Stats

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

APA
Chicago
ICMJE
MLA
NLM
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.
Journal cover image

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