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- Title
Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome.
- Authors
Yuheng Ma; Bo Xu; Yuan Fang; Zhenjun Yang; Jingrong Cui; Liangren Zhang; Lihe Zhang
- Abstract
Based on the analysis of the crystal structure of MG101 (1) and 20S proteasomes, a new series of peptide aldehyde derivatives were designed and synthesized. Their ability to inhibit 20S proteasome was assayed. Among them, Cbz-Glu(OtBu)-Phe-Leucinal (3c), Cbz-Glu(OtBu)-Leu-Leucinal (3d), and Boc-Ser(OBzl)-Leu-Leucinal (3o) exhibited the most activity, which represented an order of magnitude enhancement compared with MG132 (2). The covalent docking protocol was used to explore the binding mode. The structure-activity relationship of the peptide aldehyde inhibitors is discussed.
- Subjects
ALDEHYDE synthesis; PEPTIDE synthesis; CRYSTAL structure; STRUCTURE-activity relationships; PROTEOLYSIS; ENZYME inhibitors
- Publication
Molecules, 2011, Vol 16, Issue 9, p7551
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules16097551