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Text
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URL Address
<a href="http://doi.org/10.1016/j.bmcl.2016.09.009" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2016.09.009</a>
Pages
5350–5353
Issue
21
Volume
26
Dublin Core
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Title
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Identification of small molecules that bind to the mitochondrial protein mitoNEET.
Publisher
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Bioorganic & medicinal chemistry letters
Date
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2016
2016-11
Subject
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*Bioenergetics; *Glitazones; *Mitochondria; *Small Molecule Libraries; *Type II diabetes; Hypoglycemic Agents/chemistry/metabolism; Ligands; Mitochondrial Proteins/*metabolism; Protein Binding; Thiazolidinediones/chemistry/metabolism
Creator
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Geldenhuys Werner J; Yonutas Heather M; Morris Daniel L; Sullivan Patrick G; Darvesh Altaf S; Leeper Thomas C
Description
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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.
Identifier
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<a href="http://doi.org/10.1016/j.bmcl.2016.09.009" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2016.09.009</a>
Rights
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
*Bioenergetics
*Glitazones
*Mitochondria
*Small Molecule Libraries
*Type II diabetes
2016
Bioorganic & medicinal chemistry letters
Darvesh Altaf S
Department of Pharmaceutical Sciences
Geldenhuys Werner J
Hypoglycemic Agents/chemistry/metabolism
Leeper Thomas C
Ligands
Mitochondrial Proteins/*metabolism
Morris Daniel L
NEOMED College of Pharmacy
Protein Binding
Sullivan Patrick G
Thiazolidinediones/chemistry/metabolism
Yonutas Heather M