Structure and autoregulation of a P4-ATPase lipid flippase

Nature. 2019 Jul;571(7765):366-370. doi: 10.1038/s41586-019-1344-7. Epub 2019 Jun 26.

Abstract

Type 4 P-type ATPases (P4-ATPases) are lipid flippases that drive the active transport of phospholipids from exoplasmic or luminal leaflets to cytosolic leaflets of eukaryotic membranes. The molecular architecture of P4-ATPases and the mechanism through which they recognize and transport lipids have remained unknown. Here we describe the cryo-electron microscopy structure of the P4-ATPase Drs2p-Cdc50p, a Saccharomyces cerevisiae lipid flippase that is specific to phosphatidylserine and phosphatidylethanolamine. Drs2p-Cdc50p is autoinhibited by the C-terminal tail of Drs2p, and activated by the lipid phosphatidylinositol-4-phosphate (PtdIns4P or PI4P). We present three structures that represent the complex in an autoinhibited, an intermediate and a fully activated state. The analysis highlights specific features of P4-ATPases and reveals sites of autoinhibition and PI4P-dependent activation. We also observe a putative lipid translocation pathway in this flippase that involves a conserved PISL motif in transmembrane segment 4 and polar residues of transmembrane segments 2 and 5, in particular Lys1018, in the centre of the lipid bilayer.

MeSH terms

  • Binding Sites
  • Biological Transport
  • Calcium-Transporting ATPases / antagonists & inhibitors
  • Calcium-Transporting ATPases / chemistry*
  • Calcium-Transporting ATPases / metabolism*
  • Calcium-Transporting ATPases / ultrastructure
  • Cryoelectron Microscopy*
  • Enzyme Activation
  • Lipid Bilayers / metabolism
  • Models, Biological
  • Models, Molecular
  • Phosphatidylethanolamines / metabolism
  • Phosphatidylinositol Phosphates / chemistry
  • Phosphatidylinositol Phosphates / metabolism
  • Phosphatidylserines / metabolism
  • Protein Domains
  • Saccharomyces cerevisiae / enzymology*
  • Saccharomyces cerevisiae Proteins / antagonists & inhibitors
  • Saccharomyces cerevisiae Proteins / chemistry*
  • Saccharomyces cerevisiae Proteins / metabolism*
  • Saccharomyces cerevisiae Proteins / ultrastructure

Substances

  • CDC50 protein, S cerevisiae
  • DRS2 protein, S cerevisiae
  • Lipid Bilayers
  • Phosphatidylethanolamines
  • Phosphatidylinositol Phosphates
  • Phosphatidylserines
  • Saccharomyces cerevisiae Proteins
  • phosphatidylinositol 4-phosphate
  • phosphatidylethanolamine
  • Calcium-Transporting ATPases