Amine oxidases that occur in the plasma of mammals have been intensively studied in recent years (l-8). The ability of human plasma and serum to convert benzylamine to benzaldehyde has recently been demonstrated (9). Evidence has been presented to show that this enzymatic activity is different from other human plasma enzymes that catalyze the oxidation of amines (i.e. ceruloplasmin and diamine ...

Semicarbazide-sensitive amine oxidase (SSAO) is a copper-containing enzyme that catalyzes the oxidative deamination of endogenous and exogenous primary amines. SSAO exists in mammals both as a plasma-soluble and as a membrane-bound form, and its active site is able to come into contact with numerous xenobiotic, amine-containing compounds. The kinetic studies performed in this work showed that c...

A N-benzyl-4-amino-2,2-dimethylbutanoic acid-based system has been developed as a new oxidatively activated safety catch linker for reaction monitoring and optimisation on solid support. The CAN promoted oxidative debenzylation of the tertiary N-benzylamine moiety, followed by concomitant cyclisation and release of alcohols and amines has been demonstrated both in solution phase model studies a...

Amine oxidases that occur in the plasma of mammals have been intensively studied in recent years (l-8). The ability of human plasma and serum to convert benzylamine to benzaldehyde has recently been demonstrated (9). Evidence has been presented to show that this enzymatic activity is different from other human plasma enzymes that catalyze the oxidation of amines (i.e. ceruloplasmin and diamine ...

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 an asymmetric linker possess values close to 2 nM. For the first time, crystal structures of these in complex Ser195Ala microplasmin mutant were determined, which explain their excellent potency and selec...