Affinity-based separation methods for the study of biological interactions: The case of peroxisome proliferator-activated receptors in drug discovery

• Published in: Methods (San Diego, Calif.) Calif.), 2018-08, Vol.146, p.12-25
• Main Authors: Temporini, Caterina, Brusotti, Gloria, Pochetti, Giorgio, Massolini, Gabriella, Calleri, Enrica
• Format: Article
• Language: English
• Subjects: Affinity chromatography; Chromatography, Affinity - methods; Drug-target interactions; Ligands; Peroxisome proliferator activated receptors; Peroxisome Proliferator-Activated Receptors - isolation & purification; Peroxisome Proliferator-Activated Receptors - metabolism; Receptor sub-types selectivity; Stereoselective interactions
• ISSN: 1046-2023; 1095-9130
• DOI: 10.1016/j.ymeth.2018.02.006

•Affinity chromatographic methods based on immobilized PPARs receptors are described.•Selection of PPARs ligands from natural and synthetic sources is discussed.•Selectivity and stereoselective interactions studies with PPARs receptors are reported.•The potential of affinity chromatography based on PPARs receptors in drug discovery is discussed. Affinity-based methods using immobilized proteins are important approaches for understanding the interactions between small molecules and biological targets. This review is intended to provide an overview of different affinity based separation methods that have been applied to the study of peroxisome proliferator activated receptors (PPARs). The screening of compound to increase screening rates for synthetic and natural ligands of PPAR are reported. Pros and cons of the approaches in ligand discovery initiatives are discussed.