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Inhibition of tumor growth by NF-kappaB inhibitors Umezawa KCancer Sci 2006[Oct]; 97 (10): 990-5NF-kappaB is a transcription factor that induces inflammatory cytokines and anti-apoptotic proteins. NF-kappaB is often constitutively activated in human cancers and leukemias, which might increase the malignant character of neoplastic diseases. Therefore, NF-kappaB inhibitors might be useful as anticancer agents. Our research team designed a new NF-kappaB inhibitor that is based on the structure of the antibiotic epoxyquomicin C isolated from a microorganism. The designed compound, DHMEQ, inhibited the ligand-induced activation of NF-kappaB, and it also inhibited the constitutively activated NF-kappaB in cancer cells. DHMEQ is a unique inhibitor of NF-kappaB that acts at the level of the nuclear translocation. It inhibited both canonical and non-canonical NF-kappaB activating pathways. It inhibited various carcinomas and leukemias in animal models without any toxicity, and might be useful as an anticancer agent.|*Drug Design[MESH]|Animals[MESH]|Antineoplastic Agents/chemical synthesis/chemistry/*pharmacology[MESH]|Benzamides/chemistry[MESH]|Cell Proliferation/*drug effects[MESH]|Cyclohexanones/chemistry[MESH]|Humans[MESH]|NF-kappa B/*antagonists & inhibitors[MESH]|Neoplasms/*metabolism[MESH]|Quinones/chemistry[MESH]|Signal Transduction/drug effects[MESH]|Tumor Cells, Cultured[MESH] |
