MG-262[Z-Leu-Leu-Leu-B(OH)2]

Description :
MG-262 [Z-Leu-Leu-Leu-B(OH)2], a boric acid peptide, is a potent proteasome inhibitor that selectively and reversibly inhibits chymotrypsin activity of the proteasome. MG-262 is composed of a polypeptide and a boric acid moiety, which plays a role in inhibiting the proteasome. MG-262 has been reported to be able to reduce cell viability in nasal mucosal and polyp fibroblasts, induce cell growth arrest, inhibit DNA replication and retinoblastoma phosphorylation, increase the expression of cell cycle repressors p21 and p27, induce phosphorylation of c-Jun and expression of mitogen-activated protein kinase phosphatase-1 (MKP-1) through mitochondrial membrane potential depletion, activation of caspase-3 and poly(ADP-ribose) polymerase, thereby inducing cell death.