Elucidation of the structure and intermolecular interactions of a reversible cyclic-peptide inhibitor of the proteasome by NMR spectroscopy and molecular modeling

authored by
Benjamin Stauch, Bernd Simon, Teodora Basile, Gisbert Schneider, Nisar P. Malek, Markus Kalesse, Teresa Carlomagno
Abstract

chemical equation presentation Complex considerations: The proteasome plays a key role in diseases and is thus an appealing drug target. A structural model (see picture) of the proteasome as a complex with argyrin, a cyclic heptapeptide with antitumoral activity, provides a rationale for the high biological activity of this natural product. The structure-activity-relationship data available for the drug are discussed on the basis of this model.

External Organisation(s)
European Molecular Biology Laboratory
ETH Zurich
Hannover Medical School (MHH)
Helmholtz Centre for Infection Research (HZI)
Type
Article
Journal
Angewandte Chemie - International Edition
Volume
49
Pages
3934-3938
No. of pages
5
ISSN
1433-7851
Publication date
25.05.2010
Publication status
Published
Peer reviewed
Yes
ASJC Scopus subject areas
Catalysis, Chemistry(all)
Sustainable Development Goals
SDG 3 - Good Health and Well-being
Electronic version(s)
https://doi.org/10.1002/anie.201000140 (Access: Unknown)