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ChemInform Abstract: X-Ray Crystal Structure of a Bisubstrate Inhibitor Bound to the Enzyme Catechol-O-methyltransferase: A Dramatic Effect of Inhibitor Preorganization on Binding Affinity.

✍ Scribed by Christian Lerner; Armin Ruf; Volker Gramlich; Birgit Masjost; Gerhard Zuercher; Roland Jakob-Roetne; Edilio Borroni; Francois Diederich

Publisher: John Wiley and Sons
Year: 2010
Weight: 25 KB
Volume: 33
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.200208254

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## Abstract Inhibition of the enzyme catechol __O__‐methyltransferase (COMT) is of significant interest in the therapy of __Parkinson__'s disease. Described herein are structural analogs of the potent bisubstrate inhibitor (−)‐1 (__IC__~50~=9 nM; __Table 1__) for COMT, with target modifications of