Gorris, Hans H. (2013) Kinetic analysis of renin and its inhibitors by detecting double-labelled peptidic substrates with an immunoassay. ANALYST, 138 (7). pp. 2104-2109. ISSN 0003-2654,
Full text not available from this repository. (Request a copy)Abstract
The proteolytic activity of renin is a key element in the regulation of blood pressure and a main target for inhibitor design. Currently, the activity of renin and its inhibitors is mainly analyzed using radioimmunoassays or FRET-substrates, which both have their limitations. Here, a novel kinetic assay is presented that combines the advantages of a homogeneous proteolytic reaction and a robust heterogeneous detection in a sandwich immunoassay format. The proteolysis in solution is not influenced by surface interactions and yields accurate kinetic values, while the specific detection of the cleavage products on a microtiter plate strongly reduces interference by concomitant substances and allows for a self-referenced signal readout. A new enzyme kinetic scheme for the inhibition of renin has been developed and validated by using the model inhibitor pepstatin. This kinetic analysis is amenable to parallelization for large-scale inhibitor screening. Furthermore, it can be easily adapted to inhibitors of other medically important proteases.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | KIDNEY RENIN; HUMAN-PLASMA; PEPSTATIN; ASSAY; ACID; ANGIOTENSINOGEN; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institut für Analytische Chemie, Chemo- und Biosensorik |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 29 Apr 2020 07:03 |
| Last Modified: | 29 Apr 2020 07:03 |
| URI: | https://pred.uni-regensburg.de/id/eprint/17456 |
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