Identification of small molecules that bind to the mitochondrial protein mitoNEET
Autor: | Thomas C. Leeper, Werner J. Geldenhuys, Patrick G. Sullivan, Altaf S. Darvesh, Daniel L. Morris, Heather M. Yonutas |
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Rok vydání: | 2016 |
Předmět: |
0301 basic medicine
Protein family medicine.drug_class Clinical Biochemistry Pharmaceutical Science Mitochondrion Ligands Biochemistry Article Mitochondrial Proteins Small Molecule Libraries 03 medical and health sciences Drug Discovery medicine Hypoglycemic Agents Thiazolidinedione Molecular Biology Mitochondrial protein Chemistry Organic Chemistry Small molecule 030104 developmental biology Molecular Medicine Thiazolidinediones Rosiglitazone Pioglitazone Function (biology) Protein Binding medicine.drug |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:5350-5353 |
ISSN: | 0960-894X |
DOI: | 10.1016/j.bmcl.2016.09.009 |
Popis: | 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. |
Databáze: | OpenAIRE |
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