1334176-84-9Relevant 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
, 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.
