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Selective Binding of the Fluorescent Dye 1-Anilinonaphthalene-8-sulfonic Acid to Peroxisome Proliferator-activated Receptor γ Allows Ligand Identification and Characterization by Silvia Zorrilla; Beatriz Garzón; Dolores Pérez-Sala is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Peroxisome proliferator-activated receptor c (PPARc) is a member of the nuclear receptor superfamily involved in insulin sensitization, atherosclerosis, inflammation, and carcinogenesis. PPARc transcriptional activity is modulated by specific ligands that promote conformational changes allowing interaction with coactivators. Here we show that the fluorophore 1-anilinonaphthalene-8-sulfonic acid (ANS) binds to PPARc-LBD (ligand binding domain), displaying negligible interaction with other nuclear receptors such as PPARa and retinoid X receptor a (RXRa). ANS binding is competed by PPARc agonists such as rosiglitazone, 15-deoxy-D 12,14 -prostaglandin J 2 (15d-PGJ 2 ), and 9,10-dihydro-15-deoxy-D 12,14 -prostaglandin J 2 (CAY10410). Moreover, the affinity of PPARc for these ligands, determined through ANS competition titrations, is within the range of that reported previously, thereby suggesting that ANS competition could be useful in the screening and characterization of novel PPARc agonists. In contrast, gelbased competition assays showed limited performance with noncovalently bound ligands. We applied the ANS binding assay to characterize a biotinylated analog of 15d-PGJ 2 that does

Who reads Selective Binding of the Fluorescent Dye 1-Anilinonaphthalene-8-sulfonic Acid to Peroxisome Proliferator-activated Receptor γ Allows Ligand Identification and Characterization?

Author

Silvia Zorrilla; Beatriz Garzón; Dolores Pérez-Sala

Publisher

Elsevier Science; Elsevier ; Elsevier Inc.; Elsevier BV (ISSN 0003-2697)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)