Details
| Original language | English |
|---|---|
| Pages (from-to) | 3934-3938 |
| Number of pages | 5 |
| Journal | Angewandte Chemie - International Edition |
| Volume | 49 |
| Issue number | 23 |
| Publication status | Published - 25 May 2010 |
| Externally published | Yes |
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.
Keywords
- Cancer, Competitive binding, Ligand interactions, Nmr spectroscopy, Proteasomes
ASJC Scopus subject areas
- Chemical Engineering(all)
- Catalysis
- Chemistry(all)
Sustainable Development Goals
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In: Angewandte Chemie - International Edition, Vol. 49, No. 23, 25.05.2010, p. 3934-3938.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - Elucidation of the structure and intermolecular interactions of a reversible cyclic-peptide inhibitor of the proteasome by NMR spectroscopy and molecular modeling
AU - Stauch, Benjamin
AU - Simon, Bernd
AU - Basile, Teodora
AU - Schneider, Gisbert
AU - Malek, Nisar P.
AU - Kalesse, Markus
AU - Carlomagno, Teresa
PY - 2010/5/25
Y1 - 2010/5/25
N2 - 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.
AB - 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.
KW - Cancer
KW - Competitive binding
KW - Ligand interactions
KW - Nmr spectroscopy
KW - Proteasomes
UR - http://www.scopus.com/inward/record.url?scp=77953012647&partnerID=8YFLogxK
U2 - 10.1002/anie.201000140
DO - 10.1002/anie.201000140
M3 - Article
C2 - 20408152
AN - SCOPUS:77953012647
VL - 49
SP - 3934
EP - 3938
JO - Angewandte Chemie - International Edition
JF - Angewandte Chemie - International Edition
SN - 1433-7851
IS - 23
ER -