Mostra i principali dati dell'item
Solvent Selection for Insoluble Ligands, a Challenge for Biological Assay Development: A TNF-alpha/SPD304 Study
dc.creator | Papaneophytou, C. P. | en |
dc.creator | Mettou, A. K. | en |
dc.creator | Rinotas, V. | en |
dc.creator | Douni, E. | en |
dc.creator | Kontopidis, G. A. | en |
dc.date.accessioned | 2015-11-23T10:43:58Z | |
dc.date.available | 2015-11-23T10:43:58Z | |
dc.date.issued | 2013 | |
dc.identifier | 10.1021/ml300380h | |
dc.identifier.issn | 1948-5875 | |
dc.identifier.uri | http://hdl.handle.net/11615/31867 | |
dc.description.abstract | Many active compounds may be excluded from biological assays due to their low aqueous solubility. In this study, a simple method for the determination of the solubility of compounds containing aromatic rings is proposed. In addition to DMSO, five organic solvents for screening experiments of TNF-alpha inhibitors were explored. DMSO and PEG3350 were the most suitable for both protein stability and ligand-binding experiments. In addition, glycerol is a promising solvent for the screening of other compounds for which it might provide acceptable solubilization, due to its strong tendency to preserve the protein. Moreover, a fluorescence binding assay was developed using the TNF-alpha/SPD304 system, and a K-d of 5.36 +/- 0.21 mu M was determined. The results of this study could be used for the future screening of potential TNF-alpha inhibitors, while the protocols developed in this work could be applied to other proteins. | en |
dc.source | Acs Medicinal Chemistry Letters | en |
dc.source.uri | <Go to ISI>://WOS:000313404200034 | |
dc.subject | solvent selection | en |
dc.subject | insoluble ligands | en |
dc.subject | aqueous solubility | en |
dc.subject | protein | en |
dc.subject | stability | en |
dc.subject | fluorescence binding assay | en |
dc.subject | DRUG DISCOVERY | en |
dc.subject | TNF-ALPHA | en |
dc.subject | SOLUBILITY | en |
dc.subject | OPTIMIZATION | en |
dc.subject | Chemistry, Medicinal | en |
dc.title | Solvent Selection for Insoluble Ligands, a Challenge for Biological Assay Development: A TNF-alpha/SPD304 Study | en |
dc.type | journalArticle | en |
Files in questo item
Files | Dimensione | Formato | Mostra |
---|---|---|---|
Nessun files in questo item. |