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- W2007977393 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." @default.
- W2007977393 created "2016-06-24" @default.
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- W2007977393 date "2011-09-05" @default.
- W2007977393 modified "2023-10-18" @default.
- W2007977393 title "Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome" @default.
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- W2007977393 doi "https://doi.org/10.3390/molecules16097551" @default.
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