Significantly enhanced proteolytic activity of cyclen complexes by monoalkylation.
A simple approach towards efficient artificial proteases based on the cyclen ligand is presented. We thus achieved an increase of the proteolytic activity of two orders of magnitude when compared to the unsubstituted cyclen complex. Amphiphilic Cu(ii) and Co(iii) complexes cut BSA and myoglobin as model substrates at μM concentrations. MALDI-ToF MS is used to identify the cleavage fragments.
Institut für Chemie und Biochemie, Freie Universität Berlin, Fabeckstr. 34/36, 14195 Berlin, Germany. nora.kulak@fu-berlin.de.
Chrischani
C
Perera-Bobusch
Jan
J
Hormann
Christoph
C
Weise
Stefanie
S
Wedepohl
Jens
J
Dernedde
Nora
N
Kulak
D000072283:A549 Cells; D000478:Alkylation; D002470:Cell Survival / Q000187:drug effects; D003035:Cobalt / Q000737:chemistry / Q000494:pharmacology; D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology; D003300:Copper / Q000737:chemistry / Q000494:pharmacology; D000080027:Cyclams; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009211:Myoglobin / Q000737:chemistry; D059748:Proteolysis; D012710:Serum Albumin, Bovine / Q000737:chemistry
D056831:Coordination Complexes; D000080027:Cyclams; D006571:Heterocyclic Compounds; D009211:Myoglobin; D012710:Serum Albumin, Bovine; D003035:Cobalt; D003300:Copper; C038072:cyclen