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Back Cover: In Situ Assembly of Choline Acetyltransferase Ligands by a Hydrothiolation Reaction Reveals Key Determinants for Inhibitor Design (Angew. Chem. Int. Ed. 2/2021)
Author(s) -
Wiktelius Daniel,
Allgardsson Anders,
Bergström Tomas,
Hoster Norman,
Akfur Christine,
Forsgren Nina,
Lejon Christian,
Hedenström Mattias,
Linusson Anna,
Ekström Fredrik
Publication year - 2021
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.202015990
Subject(s) - in situ , chemistry , enzyme , active site , catalysis , combinatorial chemistry , biochemistry , stereochemistry , organic chemistry
In situ hydrothiolation solves a 50‐year SAR conundrum: In their Research article on page 813, Fredrik Ekström and co‐workers describe an in situ inhibitor assembly catalyzed by choline acetyltransferase. Using a series of prototypical arylvinylpyridinium‐based compounds previously believed to be inhibitors, they show that these compounds are actually substrates in a coenzyme A‐dependent hydrothiolation reaction that yields the active inhibitors. The reaction product within the enzyme catalytic site is illustrated.