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In Situ Click Chemistry: Enzyme‐Generated Inhibitors of Carbonic Anhydrase II
Author(s) -
Mocharla Vani P.,
Colasson Benoit,
Lee Lac V.,
Röper Stefanie,
Sharpless K. Barry,
Wong ChiHuey,
Kolb Hartmuth C.
Publication year - 2004
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.200461580
Subject(s) - carbonic anhydrase , click chemistry , enzyme , in situ , chemistry , biochemistry , combinatorial chemistry , organic chemistry
Target‐guided synthesis : Rather than making and screening thousands of compounds for lead discovery, in situ click chemistry employs the biological target itself to assemble its inhibitors by selectively binding and interconnecting reagents within the confines of its binding sites. Subnanomolar inhibitors of carbonic anhydrase II were produced by the enzyme from simple azide and acetylene precursors (see picture).