Author: Schmidt, Marco Florian; Isidroâ€Llobet, Albert; Lisurek, Michael; Elâ€Dahshan, Adeeb; Tan, Jinzhi; Hilgenfeld, Rolf; Rademann, Jörg
Title: Sensitized Detection of Inhibitory Fragments and Iterative Development of Nonâ€Peptidic Protease Inhibitors by Dynamic Ligation Screening Cord-id: 7dgbc4um Document date: 2008_3_17
ID: 7dgbc4um
Snippet: A potential antiâ€SARS drug has been developed by dynamic ligation screening (DLS), by which nucleophilic fragments are directed to the protein's active site by reversible reaction with an aldehyde inhibitor. Their inhibitory effect is detected by competition with a fluorogenic enzyme substrate. With this concept, lowâ€affinity fragments binding specifically to the active site are quickly identified in a functional enzyme assay.[Image: see text]
Document: A potential antiâ€SARS drug has been developed by dynamic ligation screening (DLS), by which nucleophilic fragments are directed to the protein's active site by reversible reaction with an aldehyde inhibitor. Their inhibitory effect is detected by competition with a fluorogenic enzyme substrate. With this concept, lowâ€affinity fragments binding specifically to the active site are quickly identified in a functional enzyme assay.[Image: see text]
Search related documents:
Co phrase search for related documents- active compound and low affinity: 1
- active compound and low inhibition: 1
- active fragment and acute respiratory syndrome: 1
- active inhibitor and acute respiratory syndrome: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14
- active inhibitor and low micromolar range: 1, 2, 3
- active protease site cysteine and acute respiratory syndrome: 1, 2
- active site and acute respiratory syndrome: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25
- active site and low affinity: 1, 2, 3, 4, 5, 6
- active site and low affinity fragment: 1
- active site and low inhibition: 1, 2, 3, 4, 5, 6, 7
- active site and low micromolar range: 1, 2, 3, 4, 5, 6
- active site and low micromolar range constant: 1
- active site and low micromolar range constant inhibition: 1
- activity show and acute respiratory syndrome: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25
- activity show and additional evidence: 1, 2
- activity show and low affinity: 1
- activity show and low micromolar range: 1, 2
- acute respiratory syndrome and low micromolar range: 1, 2, 3, 4, 5, 6, 7, 8, 9, 10
- acute respiratory syndrome and low micromolar range constant: 1
Co phrase search for related documents, hyperlinks ordered by date