1334176-79-2Relevant academic research and scientific papers
Synthesis and SAR study of novel peptide aldehydes as inhibitors of 20S proteasome
Ma, Yuheng,Xu, Bo,Fang, Yuan,Yang, Zhenjun,Cui, Jingrong,Zhang, Liangren,Zhang, Lihe
scheme or table, p. 7551 - 7564 (2011/11/14)
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.
