Facile synthesis of covalent probes to capture enzymatic intermediates during E1 enzyme catalysis.

Chem Commun (Camb)

Department of Chemistry, Center for Molecular Innovation and Drug Discovery, Chemistry of Life Processes Institute, Northwestern University, Silverman Hall, 2145 Sheridan Road, Evanston, Illinois 60208, USA.

Published: February 2016

We report a facile synthetic strategy to prepare UBL-AMP electrophilic probes that form a covalent bond with the catalytic cysteine of cognate E1s, mimicking the tetrahedral intermediate of the E1-UBL-AMP complex. These probes enable the structural and biochemical study of both canonical- and non-canonical E1s.

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http://dx.doi.org/10.1039/c5cc08592fDOI Listing

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