Binding of thiazolidinediones to the endoplasmic reticulum protein nutrient-deprivation autophagy factor-1

Bioorg Med Chem Lett. 2019 Apr 1;29(7):901-904. doi: 10.1016/j.bmcl.2019.01.041. Epub 2019 Feb 1.

Abstract

Nutrient-deprivation autophagy factor-1 (NAF-1, miner1; gene cisd2) is part of the [2Fe-2S]-containing protein family which includes mitoNEET (gene cisd1) and MiNT (miner2; gene cisd3). These proteins are redox active and are thought to play an important role in cellular energy homeostasis with NAF-1 playing a critical role in calcium regulation and aging. To date, no studies have investigated potential ligand interaction with NAF-1. Here we show that the thiazolidinediones pioglitazone and rosiglitazone along with the mitoNEET ligand, NL-1, bind to NAF-1 with low micromolar affinities. Further, we show that overexpression of NAF-1 in hepatocellular carcinoma (HepG2) cells reduces inhibition of mitochondrial respiration by pioglitazone. Our findings support the need for further efforts of the rational design of selective NAF-1 ligands.

Keywords: CDGSH; CISD' miner1; Glitazones; Wolfram syndrome; Zinc-finger.

Publication types

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

MeSH terms

  • Hep G2 Cells
  • Humans
  • Ligands
  • Membrane Proteins / metabolism*
  • Molecular Docking Simulation
  • Pioglitazone / metabolism*
  • Protein Binding
  • Rosiglitazone / metabolism*

Substances

  • CISD2 protein, human
  • Ligands
  • Membrane Proteins
  • Rosiglitazone
  • Pioglitazone