Affinity labeling libraries with tagged leaving group
US6403324B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Mar 13, 1998 |
| Grant date | Jun 11, 2002 |
| Priority date | — |
| Expiry date | Mar 13, 2018 |
Classification
- Technology area (CPC B)Performing Operations; Transporting
- CPC primaryB01J2219/00592
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
Methods and compositions are provided for identifying compounds having affinity to a target site. The method provides for the affinity group to be a leaving group from a reactive functionality capable of forming a covalent bond to the target site. One can combine the compound comprising the target site with the library, and assay for the resulting composition of the leaving groups. The leaving groups having the highest concentration can be identified as the groups having the binding highest affinity for the target site. The selected compounds may then be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding proteins or as an enzyme inhibitor.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.