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Screening a fragment cocktail library using ultrafiltration.
| Title | Screening a fragment cocktail library using ultrafiltration. |
| Publication Type | Journal Article |
| Year of Publication | 2011 |
| Authors | Shibata, S, Zhang, Z, Korotkov, KV, Delarosa, J, Napuli, A, Kelley, AM, Mueller, N, Ross, J, Zucker, FH, Buckner, FS, Merritt, EA, Verlinde, CLMJ, Van Voorhis, WC, Hol, WGJ, Fan, E |
| Journal | Anal Bioanal Chem |
| Volume | 401 |
| Issue | 5 |
| Pagination | 1585-91 |
| Date Published | 2011 Sep |
| ISSN | 1618-2650 |
| Keywords | Binding, Competitive, Drug Discovery, Escherichia coli, Ligands, Plasmodium yoelii, Protein Binding, Proteins, Small Molecule Libraries, Trypanosoma brucei brucei, Ultrafiltration |
| Abstract | Ultrafiltration provides a generic method to discover ligands for protein drug targets with millimolar to micromolar K(d), the typical range of fragment-based drug discovery. This method was tailored to a 96-well format, and cocktails of fragment-sized molecules, with molecular masses between 150 and 300 Da, were screened against medical structural genomics target proteins. The validity of the method was confirmed through competitive binding assays in the presence of ligands known to bind the target proteins. |
| DOI | 10.1007/s00216-011-5225-7 |
| Alternate Journal | Anal Bioanal Chem |
| PubMed ID | 21750879 |
