Abstract
Graphical Abstract The Front Cover shows new macrocyclic plasmin inhibitors containing a C-terminal P1 benzylamine group. Their N-terminal substitution provided analogues with sub-nanomolar Ki values. Additional inhibitors containing an asymmetric linker possess Ki values close to 2 nM. For the first time, crystal structures of these macrocyclic inhibitors in complex with a Ser195Ala microplasmin mutant were determined, which explain their excellent potency and selectivity. More information can be found in the Research Article by Simon J. A. Wiedemeyer, Guojie Wu, Ruby H. P. Law, Torsten Steinmetzer et al.
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