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Back Cover: Phosphono Bisbenzguanidines as Irreversible Dipeptidomimetic Inhibitors and Activity‐Based Probes of Matriptase‐2 (Chem. Eur. J. 25/2016)
Author(s) -
Häußler Daniela,
Mangold Martin,
Furtmann Norbert,
Braune Annett,
Blaut Michael,
Bajorath Jürgen,
Stirnberg Marit,
Gütschow Michael
Publication year - 2016
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201601295
Subject(s) - docking (animal) , chemistry , combinatorial chemistry , fluorescence , computational biology , enzyme , cover (algebra) , stereochemistry , biochemistry , biology , medicine , engineering , physics , nursing , quantum mechanics , mechanical engineering
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.