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(−)‐FR182877 Is a Potent and Selective Inhibitor of Carboxylesterase‐1
Author(s) -
Adam Gregory C.,
Vanderwal Christopher D.,
Sorensen Erik J.,
Cravatt Benjamin F.
Publication year - 2003
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.200352576
Subject(s) - carboxylesterase , natural product , chemistry , pharmacology , computational biology , biochemistry , biology , enzyme
Activity‐based profiling and reporter‐group‐tagged compounds were used to identify carboxylesterase‐1 (CE‐1) as a specific target of the natural product (−)‐FR182877 (see scheme). Now that a target is known, specific modification of the lactone natural product may lead to even more effective inhibitors of CE‐1.