Journal
MOLECULES
Volume 16, Issue 9, Pages 7551-7564Publisher
MDPI AG
DOI: 10.3390/molecules16097551
Keywords
20S proteasome; inhibitor; peptide aldehydes; synthesis; structure-activity relationship
Funding
- National Natural Science Foundation of China [20672010]
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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.
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