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    • 9. 发明公开
    • PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER, CONTAINING ENOBLOCK AS ACTIVE INGREDIENT
    • 用于预防的药物组合物和治疗癌症与ENOBLOCK为活动
    • EP2910246A1
    • 2015-08-26
    • EP13849288.9
    • 2013-10-22
    • Gwangju Institute of Science and Technology
    • JUNG, Da-WoonKIM, Woong-HeeWILLIAMS, Darren
    • A61K31/53A61P35/00
    • A61K31/53
    • The present invention relates to ENOblock, which is a non-substrate analogue having an enolase inhibitory activity, and a pharmaceutical composition for preventing or treating cancer or enolase-associated diseases, containing the same. The ENOblock of the present invention directly binds to enolase so as to inhibit an activity thereof, and the inhibition is more effective in hypoxia than in normoxia. In addition, the ENOblock of the present invention inhibits migration, metastasis and invasion of cancer cells. Furthermore, the ENOblock of the present invention induces glucose uptake into cells, down-regulates the expression of PEPCK, and inhibits adipogenesis and foam cell formation. Therefore, a composition containing the ENOblock of the present invention can be very effectively applied to prevent or treat cancer or enolase-associated diseases.
    • 本发明涉及ENOblock,所有这些是具有烯醇的抑制活性的非底物类似物,以及用于预防或治疗癌症或烯醇化酶有关的疾病,含有它们的药物组合物。 本发明的ENOblock直接结合烯醇化酶以抑制其活性,所述抑制是比在常氧更有效缺氧。 另外,本发明的ENOblock抑制迁移,转移和癌细胞的侵袭。 进一步,本发明的ENOblock诱导的葡萄糖摄取到细胞中,下调PEPCK的表达,并抑制脂肪形成和泡沫细胞形成。 因此,含有本发明的ENOblock的组合物可非常有效地应用于预防或治疗癌症或烯醇酶相关的疾病。