Lactacystin is a microbial metabolite isolated from Streptomyces that is now widely used for a discriminating inhibitor of the 20 S proteasome. The molecule is a lactam, or cyclic amide.
A number of syntheses of this molecule consume embodied promulgated and in that respect are no less than 1,300 references to this natural product in the literature. Lactacystin is an organic compound naturally synthesized along bacterium of the genus Streptomyces commencement depicted in 1991. Lactacystin was first characterized by thems ability to induct specialization and subdue cell cycle progression in several tumor cell lines. Cell permeable, irreversible proteasome inhibitor.
Specifically inhibits the 20S and 26S proteasome. Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. A cell-permeable, potent and selective proteasome inhibitor. A Streptomyces metabolite that is thought to bind irreversibly to the active site N-terminal threonine residue of the catalytic β-subunit of the 20S proteasome, thereby inhibiting its chymotrypsin and trypsin-like activities. Inducts neurite growth in Neuro 2a neuroblastoma cells and consumes followed reported to get apoptosis fashionable someone monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 μM).
Thus, the effects of lactacystin are pleiotropic and depend substantially on the expression pattern of signalling proteins within the treated cell.
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