Small-molecule inhibitor: belactosin A

Summary Structure Literature

Name

Common name: belactosin A
Other names: belactosin C; KF33955

Inhibition

History: Belactosin A was described as an antibiotic produced by Streptomyces species (Asai et al., 2000), and was later shown to be a proteasome inhibitor (Asai et al., 2004).
Peptidases inhibited: Belactosin A inhibits the chymotrypsin-like activity of the rabbit 20S proteasome (Asai et al., 2004), which is due to proteasome catalytic subunit 3.

Chemistry

ChEBI: 593046
Structure
Formula weight: 369
Related inhibitors: Belactosin C is structurally related to belactosin A (Larionov & de Meijere, 2004). A hydrophobic derivative of belactosin A, KF33955, exhibited much greater potency in a cell-based assay, presumably because of higher cell permeability. Other more potent analogues have also been described (Yoshida et al., 2009).

Properties

Synthesis: Armstrong & Scutt, 2004