Total synthesis of the-potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology
作者:Ny Sin、Kyung Bo Kim、Mikael Elofsson、Lihao Meng、Hak Auth、Benjamin H.B. Kwok、Craig M. Crews
DOI:10.1016/s0960-894x(99)00376-5
日期:1999.8
Epoxomicin (1), a peptide alpha',beta'-epoxyketone isolated from the actinomycete strain No.Q996-17, possesses potent in vivo anti-tumor and anti-inflammatory activities. In this paper, we report the first syntheses of epoxomicin, [H-3]-epoxomicin, and a biotinylated epoxomicin analog as well as the absolute configuration of the epoxide stereocenter. The natural product and derivatives have permitted the first identification of the proteasome as the specific cellular target of epoxomicin. (C) 1999 Elsevier Science Ltd. All rights reserved.