Structure and function of Neisseria gonorrhoeae MtrF illuminates a class of antimetabolite efflux pumps

Cell Rep. 2015 Apr 7;11(1):61-70. doi: 10.1016/j.celrep.2015.03.003. Epub 2015 Mar 26.

Abstract

Neisseria gonorrhoeae is an obligate human pathogen and the causative agent of the sexually transmitted disease gonorrhea. The control of this disease has been compromised by the increasing proportion of infections due to antibiotic-resistant strains, which are growing at an alarming rate. N. gonorrhoeae MtrF is an integral membrane protein that belongs to the AbgT family of transporters for which no structural information is available. Here, we describe the crystal structure of MtrF, revealing a dimeric molecule with architecture distinct from all other families of transporters. MtrF is a bowl-shaped dimer with a solvent-filled basin extending from the cytoplasm to halfway across the membrane bilayer. Each subunit of the transporter contains nine transmembrane helices and two hairpins, posing a plausible pathway for substrate transport. A combination of the crystal structure and biochemical functional assays suggests that MtrF is an antibiotic efflux pump mediating bacterial resistance to sulfonamide antimetabolite drugs.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / therapeutic use
  • Bacterial Proteins / chemistry*
  • Bacterial Proteins / metabolism
  • Crystallography, X-Ray
  • Drug Resistance, Bacterial / genetics*
  • Gene Expression Regulation, Bacterial / drug effects
  • Gonorrhea / drug therapy
  • Gonorrhea / genetics
  • Gonorrhea / microbiology*
  • Humans
  • Models, Molecular
  • Neisseria gonorrhoeae / chemistry*
  • Neisseria gonorrhoeae / drug effects
  • Neisseria gonorrhoeae / genetics
  • Protein Conformation
  • Repressor Proteins / chemistry*
  • Repressor Proteins / metabolism
  • Structure-Activity Relationship
  • Sulfonamides / chemistry
  • Sulfonamides / therapeutic use

Substances

  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Repressor Proteins
  • Sulfonamides
  • mtrR protein, Neisseria gonorrhoeae

Associated data

  • PDB/4R11