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- Title
Back Cover: Phosphono Bisbenzguanidines as Irreversible Dipeptidomimetic Inhibitors and Activity-Based Probes of Matriptase-2 (Chem. Eur. J. 25/2016).
- Authors
Häußler, Daniela; Mangold, Martin; Furtmann, Norbert; Braune, Annett; Blaut, Michael; Bajorath, Jürgen; Stirnberg, Marit; Gütschow, Michael
- Abstract
Phosphono bisbenzguanidines as dipeptidomimetic inactivators for matriptase ‐ 2 were discovered. Inhibition of this enzyme is one strategy for the treatment of iron ‐ overload diseases. Synthetic routes to new inactivators were developed. The irreversible inhibition was kinetically characterized and the binding mode was supported by docking analysis. Based on this chemotype, a fluorescent probe was designed and synthesized. Finally, by applying the first activity ‐ based probe for matriptase ‐ 2, detection of the target was demonstrated. More information can be found in the Full Paper by M. Gütschow et al. on page 8525 ff.
- Subjects
MATRIPTASE; CHEMISTRY periodicals
- Publication
Chemistry - A European Journal, 2016, Vol 22, Issue 25, p8704
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201601295