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Text
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URL Address
<a href="http://doi.org/10.1016/j.bmcl.2011.06.111" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2011.06.111</a>
Pages
5498–5501
Issue
18
Volume
21
Dublin Core
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Title
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A novel binding assay identifies high affinity ligands to the rosiglitazone binding site of mitoNEET.
Publisher
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Bioorganic & medicinal chemistry letters
Date
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2011
2011-09
Subject
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Binding Sites/drug effects; Dose-Response Relationship; Drug; Ligands; Mitochondrial Proteins/*antagonists & inhibitors/metabolism; Molecular Structure; Recombinant Proteins/antagonists & inhibitors/metabolism; Rosiglitazone; Stereoisomerism; Structure-Activity Relationship; Thiazolidinediones/chemical synthesis/chemistry/*pharmacology
Creator
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Geldenhuys Werner J; Funk Max O; Awale Prabha S; Lin Li; Carroll Richard T
Description
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A novel outer mitochondrial membrane protein containing [2Fe-2S] clusters, mitoNEET was first identified through its binding to the anti-diabetic drug pioglitazone. Pioglitazone belongs to a family of drugs that are peroxisome proliferator-activated receptor (PPAR) gamma agonists, collectively known as glitazones. With the lack of pharmacological tools available to fully elucidate mitoNEET's function, we developed a binding assay to probe the glitazone binding site with the aim of developing selective and high affinity compounds. We used multiple thiazolidine-2,4-dione (TZD), 2-thioxothiazolidin-4-one (TTD), and
Identifier
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<a href="http://doi.org/10.1016/j.bmcl.2011.06.111" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2011.06.111</a>
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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).
2011
Awale Prabha S
Binding Sites/drug effects
Bioorganic & medicinal chemistry letters
Carroll Richard T
Dose-Response Relationship
Drug
Funk Max O
Geldenhuys Werner J
Ligands
Lin Li
Mitochondrial Proteins/*antagonists & inhibitors/metabolism
Molecular Structure
Recombinant Proteins/antagonists & inhibitors/metabolism
Rosiglitazone
Stereoisomerism
Structure-Activity Relationship
Thiazolidinediones/chemical synthesis/chemistry/*pharmacology