A structure-based mechanism for drug binding by multidrug transporters.
Publication
, Journal Article
Zheleznova, EE; Markham, P; Edgar, R; Bibi, E; Neyfakh, AA; Brennan, RG
Published in: Trends Biochem Sci
February 2000
Multidrug transporters bind chemically dissimilar, potentially cytotoxic compounds and remove them from the cell. How these transporters carry out either of these functions is unknown. On the basis of crystal structures of the multidrug-binding domain of the transcription activator BmrR and mutagenesis studies on the bacterial multidrug transporter MdfA, we propose a possible mechanism for the binding of cationic lipophilic drugs by multidrug transporters. The key element of this mechanism includes a conformational change in the transporter that exposes a buried charged residue in the substrate-binding pocket and allows access to this site by only those drugs that are its steric and electrostatic complements.
Duke Scholars
Published In
Trends Biochem Sci
DOI
ISSN
0968-0004
Publication Date
February 2000
Volume
25
Issue
2
Start / End Page
39 / 43
Location
England
Related Subject Headings
- Trans-Activators
- Pharmaceutical Preparations
- Molecular Sequence Data
- Models, Molecular
- Membrane Transport Proteins
- Membrane Proteins
- Escherichia coli Proteins
- Drug Resistance, Multiple
- Drug Resistance, Microbial
- Developmental Biology
Citation
APA
Chicago
ICMJE
MLA
NLM
Zheleznova, E. E., Markham, P., Edgar, R., Bibi, E., Neyfakh, A. A., & Brennan, R. G. (2000). A structure-based mechanism for drug binding by multidrug transporters. Trends Biochem Sci, 25(2), 39–43. https://doi.org/10.1016/s0968-0004(99)01514-5
Zheleznova, E. E., P. Markham, R. Edgar, E. Bibi, A. A. Neyfakh, and R. G. Brennan. “A structure-based mechanism for drug binding by multidrug transporters.” Trends Biochem Sci 25, no. 2 (February 2000): 39–43. https://doi.org/10.1016/s0968-0004(99)01514-5.
Zheleznova EE, Markham P, Edgar R, Bibi E, Neyfakh AA, Brennan RG. A structure-based mechanism for drug binding by multidrug transporters. Trends Biochem Sci. 2000 Feb;25(2):39–43.
Zheleznova, E. E., et al. “A structure-based mechanism for drug binding by multidrug transporters.” Trends Biochem Sci, vol. 25, no. 2, Feb. 2000, pp. 39–43. Pubmed, doi:10.1016/s0968-0004(99)01514-5.
Zheleznova EE, Markham P, Edgar R, Bibi E, Neyfakh AA, Brennan RG. A structure-based mechanism for drug binding by multidrug transporters. Trends Biochem Sci. 2000 Feb;25(2):39–43.
Published In
Trends Biochem Sci
DOI
ISSN
0968-0004
Publication Date
February 2000
Volume
25
Issue
2
Start / End Page
39 / 43
Location
England
Related Subject Headings
- Trans-Activators
- Pharmaceutical Preparations
- Molecular Sequence Data
- Models, Molecular
- Membrane Transport Proteins
- Membrane Proteins
- Escherichia coli Proteins
- Drug Resistance, Multiple
- Drug Resistance, Microbial
- Developmental Biology