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Bioorg Med Chem Lett. 2016 Nov 1;26(21):5350-5353. doi: 10.1016/j.bmcl.2016.09.009. Epub 2016 Sep 6.

Identification of small molecules that bind to the mitochondrial protein mitoNEET.

Author information

1
Department of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, 1 Medical Center Drive, Morgantown, WV 26506, USA. Electronic address: werner.geldenhuys@hsc.wvu.edu.
2
Spinal Cord and Brain Injury Research Center, University of Kentucky, Lexington, KY 40536, USA; Anatomy and Neurobiology, University of Kentucky, Lexington, KY 40536, USA.
3
Department of Chemistry and Biochemistry, University of Akron, Akron, OH 44325, USA.
4
Department of Pharmaceutical Sciences, Northeast Ohio Medical University, Rootstown, OH 44240, USA.

Abstract

MitoNEET (CISD1) is a 2Fe-2S iron-sulfur cluster protein belonging to the zinc-finger protein family. Recently mitoNEET has been shown to be a major role player in the mitochondrial function associated with metabolic type diseases such as obesity and cancers. The anti-diabetic drug pioglitazone and rosiglitazone were the first identified ligands to mitoNEET. Since little is known about structural requirements for ligand binding to mitoNEET, we screened a small set of compounds to gain insight into these requirements. We found that the thiazolidinedione (TZD) warhead as seen in rosiglitazone was not an absolutely necessity for binding to mitoNEET. These results will aid in the development of novel compounds that can be used to treat mitochondrial dysfunction seen in several diseases.

KEYWORDS:

Bioenergetics; Glitazones; Mitochondria; Type II diabetes

PMID:
27687671
PMCID:
PMC5482219
DOI:
10.1016/j.bmcl.2016.09.009
[Indexed for MEDLINE]
Free PMC Article

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