Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594126 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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 2-iminothiazolidin-4-one (ITD) compounds to establish several trends to enhance ligand development for the purpose of elucidating mitoNEET function.
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Authors
Werner J. Geldenhuys, Max O. Funk, Prabha S. Awale, Li Lin, Richard T. Carroll,