Screening for enzyme inhibitors
US6770451B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 3, 2002 |
| Grant date | Aug 3, 2004 |
| Priority date | — |
| Expiry date | Nov 14, 2022 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2500/02
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
Systems, including methods and reagents, for identifying enzyme inhibitors. The systems employ a conjugate of a known inhibitor of a target enzyme and an enzyme donor, an enzyme acceptor that binds to the enzyme donor to form an active indicator-enzyme complex, and a detectable substrate for the indicator enzyme. The assay is performed by combining the candidate agent, the conjugate of the known inhibitor and enzyme donor, the enzyme acceptor, and the substrate under binding conditions, where the candidate compound competes with the conjugate for the target enzyme. By measuring the rate of product formation or substrate depletion catalyzed by the indicator enzyme, the inhibitory activity of the candidate compound can be determined. The methodology is particularly applicable for target enzymes that have substrates or products that are difficult to synthesize and/or detect, such as kinases and phosphatases.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.