Issue 1, 2011
From the journal:

Chemical Communications

The natural product hybrid of Syringolin A and Glidobactin A synergizes proteasome inhibition potency with subsite selectivity†‡

Jérôme Clerc,a   Nan Li,b   Daniel Krahn,a   Michael Groll,c   André S. Bachmann,d   Bogdan I. Florea,b   Herman S. Overkleeft*b  and  Markus Kaiser*a  

* Corresponding authors

a Zentrum für Medizinische Biotechnologie, Fakultät für Biologie und Geographie, Universität Duisburg-Essen, 45117 Essen, Germany
E-mail: markus.kaiser@uni-due.de
Fax: +49 201 1833135
Tel: +49 201 1832949

b Leiden Institute of Chemistry and Netherlands Proteomics Centre, Gorlaeus Laboratories, Einsteinweg 55, 2333 CC Leiden, The Netherlands
E-mail: h.s.overkleeft@chem.leidenuniv.nl
Fax: +31 71 5274307
Tel: +31 71 5274342

c Center for Integrated Protein Science at the Department Chemie, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany

d Cancer Research Center of Hawaii, University of Hawaii at Manao, 1236 Lauhala Street, Honolulu, USA

Abstract

The preparation of a Syringolin A/Glidobactin A hybrid (SylA–GlbA) consisting of a SylA macrocycle connected to the GlbA side chain and its potent proteasome targeting of all three proteasomal subsites is reported. The influence of the syrbactin macrocycle moiety on subsite selectivity is demonstrated.

Graphical abstract: The natural product hybrid of Syringolin A and Glidobactin A synergizes proteasome inhibition potency with subsite selectivity

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Article information

DOI
https://doi.org/10.1039/C0CC02238A
Article type
Communication
Submitted
30 Jun 2010
Accepted
17 Aug 2010
First published
07 Sep 2010

Chem. Commun., 2011,47, 385-387

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The natural product hybrid of Syringolin A and Glidobactin A synergizes proteasome inhibition potency with subsite selectivity

J. Clerc, N. Li, D. Krahn, M. Groll, A. S. Bachmann, B. I. Florea, H. S. Overkleeft and M. Kaiser, Chem. Commun., 2011, 47, 385 DOI: 10.1039/C0CC02238A

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