Interdomain Loop Mutation Asp190Cys of the Tetracycline Efflux Transporter TetA(B) Decreases Affinity for Substrate

Antimicrobial Agents and Chemotherapy
2007.0

Abstract

TetA(B), a tetracycline efflux protein from Tn10 with 12 predicted transmembrane α-helices and belonging to the major facilitator superfamily, uses the bacterial transmembrane proton motive force to export metal-tetracycline complexes in exchange for H⁺. Previous studies showed that the cytoplasmic interdomain loop connecting transmembrane helices 6 and 7 of TetA(B) contains residues involved in tetracycline efflux activity, and Asp190, Glu192, and Ser201 are implicated in substrate specificity. In this study, we investigated the effect of the Asp190Cys mutation on TetA(B)-mediated tetracycline efflux by transforming Escherichia coli DH5α with low-copy plasmids (pSC101 origin) carrying wild-type or mutant TetA(B), preparing everted membrane vesicles, and using [³H]tetracycline uptake assays, along with MIC determination for intact cells, Western immunoblotting to verify consistent TetA(B) protein levels in membranes, and Graphpad Prism 4 software to fit Km and Vmax values via the Michaelis-Menten equation. Results showed that the Asp190Cys mutant had an average Km value 3.8 times that of the wild type (83 ± 24 μM vs. 22 ± 6 μM) without modifying Vmax (1327 ± 187 pmol/mg protein/min vs. 1274 ± 106 pmol/mg protein/min for wild type). MIC assays revealed reduced tetracycline resistance in intact DH5 cells expressing the mutant (MIC = 11 μg/ml) compared to the wild type (MIC = 128 μg/ml). These findings indicate that the Asp190Cys mutation decreases TetA(B)'s affinity for tetracycline, likely due to the loss of the negatively charged aspartate that interacts with the positively charged metal-tetracycline complex. Furthermore, our biochemical results support that the cytoplasmic interdomain loop, previously thought to merely tether the two halves of the protein, plays an unexpected role in tetracycline transport.

Knowledge Graph

Similar Paper

Interdomain Loop Mutation Asp190Cys of the Tetracycline Efflux Transporter TetA(B) Decreases Affinity for Substrate
Antimicrobial Agents and Chemotherapy 2007.0
Molecular Requirements for the Inhibition of the Tetracycline Antiport Protein and the Effect of Potent Inhibitors on the Growth of Tetracycline-Resistant Bacteria
Journal of Medicinal Chemistry 1994.0
Selectivity of the Polyspecific Cation Transporter rOCT1 Is Changed by Mutation of Aspartate 475 to Glutamate
Molecular Pharmacology 1999.0
Site-Directed Mutagenesis Reveals Amino Acid Residues in the Escherichia coli RND Efflux Pump AcrB That Confer Macrolide Resistance
Antimicrobial Agents and Chemotherapy 2009.0
A New Tetracycline Efflux Gene, tet (40), Is Located in Tandem with tet (O/32/O) in a Human Gut Firmicute Bacterium and in Metagenomic Library Clones
Antimicrobial Agents and Chemotherapy 2008.0
Contribution of the CmeABC Efflux Pump to Macrolide and Tetracycline Resistance in Campylobacter jejuni
Antimicrobial Agents and Chemotherapy 2007.0
Inhibition of the tetracycline efflux antiport protein by 13-thio-substituted 5-hydroxy-6-deoxytetracyclines
Journal of Medicinal Chemistry 1993.0
Roles of Residues Cys69, Asn104, Phe160, Gly232, Ser237, and Asp240 in Extended-Spectrum β-Lactamase Toho-1
Antimicrobial Agents and Chemotherapy 2011.0
Single amino acid substitutions in the transmembrane domains of breast cancer resistance protein (BCRP) alter cross resistance patterns in transfectants
International Journal of Cancer 2003.0
Tat Pathway-Mediated Translocation of the Sec Pathway Substrate Protein MexA, an Inner Membrane Component of the MexAB-OprM Xenobiotic Extrusion Pump in Pseudomonas aeruginosa
Antimicrobial Agents and Chemotherapy 2010.0