Crystal structures of LeuT reveal conformational dynamics in the outward-facing states

J Biol Chem. 2021 Jan-Jun:296:100609. doi: 10.1016/j.jbc.2021.100609. Epub 2021 Apr 1.

Abstract

The neurotransmitter:sodium symporter (NSS) homolog LeuT from Aquifex aeolicus has proven to be a valuable model for studying the transport mechanism of the NSS family. Crystal structures have captured LeuT in key conformations visited during the transport cycle, allowing for the construction of a nearly complete model of transport, with much of the conformational dynamics studied by computational simulations. Here, we report crystal structures of LeuT representing new intermediate conformations between the outward-facing open and occluded states. These structures, combined with binding and accessibility studies, reveal details of conformational dynamics that can follow substrate binding at the central substrate binding site (S1) of LeuT in outward-facing states, suggesting a potential competition for direction between the outward-open and outward-occluded states at this stage during substrate transport. Our structures further support an intimate interplay between the protonation state of Glu290 and binding of Na1 that may ultimately regulate the outward-open-to-occluded transition.

Keywords: Conformational change; Membrane protein; NSS; SLC6; Structural biology; X-ray structure; monoamine transporter; tructure–function.

Publication types

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

MeSH terms

  • Aquifex / metabolism
  • Bacterial Proteins / chemistry*
  • Bacterial Proteins / metabolism*
  • Crystallography, X-Ray
  • Leucine / metabolism
  • Molecular Dynamics Simulation
  • Plasma Membrane Neurotransmitter Transport Proteins / chemistry*
  • Plasma Membrane Neurotransmitter Transport Proteins / metabolism*
  • Protein Conformation
  • Sodium / metabolism*
  • Symporters / chemistry
  • Symporters / metabolism
  • Thermodynamics

Substances

  • Bacterial Proteins
  • Plasma Membrane Neurotransmitter Transport Proteins
  • Symporters
  • Sodium
  • Leucine

Supplementary concepts

  • Aquifex aeolicus