Volume 117, Issue 42 pp. 7019-7022
Zuschrift

Regio- and Chemoselective 6′-N-Derivatization of Aminoglycosides: Bisubstrate Inhibitors as Probes To Study Aminoglycoside 6′-N-Acetyltransferases

Feng Gao

Feng Gao

Department of Chemistry, McGill University, 801 Sherbrooke Street West, Montréal, Québec, H3A 2K6, Canada, Fax: (+1) 514-398-3797

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Xuxu Yan

Xuxu Yan

Department of Chemistry, McGill University, 801 Sherbrooke Street West, Montréal, Québec, H3A 2K6, Canada, Fax: (+1) 514-398-3797

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Oliver M. Baettig

Oliver M. Baettig

Department of Biochemistry, McGill University, 801 Sherbrooke Street West, Montréal, Québec, H3A 2K6, Canada

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Albert M. Berghuis Prof.

Albert M. Berghuis Prof.

Department of Biochemistry, McGill University, 801 Sherbrooke Street West, Montréal, Québec, H3A 2K6, Canada

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Karine Auclair Prof.

Karine Auclair Prof.

Department of Chemistry, McGill University, 801 Sherbrooke Street West, Montréal, Québec, H3A 2K6, Canada, Fax: (+1) 514-398-3797

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First published: 25 October 2005
Citations: 13

This work was supported by the National Science and Engineering Research Council of Canada (NSERC), by the Canadian Institute of Health Research (CIHR), and by the Cancer Research Center (CRC). F.G., X.Y., and O.M.B. were supported by scholarship awards from the Chemical Biology Strategic Training Initiative of CIHR. The authors are grateful to G. D. Wright at McMaster University for sharing his AAC(6′)-Ii expression plasmid.

Graphical Abstract

Einfach zu komplexen nanomolaren Inhibitoren: Aminoglycosid-Coenzym-A-Derivate wurden durch eine effiziente regioselektive 6′-N-Modifizierung von Aminoglycosiden hergestellt (siehe Schema). Diese Bisubstrate sind fest bindende kompetitive Inhibitoren der Aminoglycosid-6′-N-Acetyltransferase, eines an der Antibiotikaresistenz beteiligten Enzyms.

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