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In Situ Assembly and Screening of Enzyme Inhibitors with Surface‐Tension Microarrays
Author(s) -
Mugherli Laurent,
Burchak Olga N.,
Balakireva Larissa A.,
Thomas Aline,
Chatelain François,
Balakirev Maxim Y.
Publication year - 2009
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200901139
Subject(s) - surface tension , phenylboronic acid , in situ , protease , microarray , enzyme , chemistry , materials science , biochemistry , organic chemistry , gene , physics , gene expression , quantum mechanics , catalysis
Hundreds of reactions were conducted in parallel in droplets maintained on a glass slide through differential surface tension in a new approach to submicroliter‐scale synthesis. This “surface‐tension microarray” was applied to the in situ assembly of thousands of derivatives of phenylboronic acid and their profiling against the NS3/4A protease of the hepatitis C virus. Several potent inhibitors of the enzyme were identified.